mek inhibitor Search Results


meki  (MedChemExpress)
95
MedChemExpress meki
MEK inhibition <t>(MEKi)</t> acts by selective complete inhibition of nuclear factor kappa-light-chain-enhancer of activated B cells (NFκB) and nuclear factor of activated T cells (NFAT) and partial inhibition of activator protein 1 (AP-1) signaling. (a-c) Time course over 24 hours of reporter activity for AP-1 (MCherry fluorescent protein (mCherry)), NFκB (enhanced cyan fluorescent protein (eCFP)), and NFAT (enhanced green fluorescent protein (eGFP)) in JE6.1 triple parameter reporter (TPR) CD8+ KIF-sc1-tg Jurkat cells upon co-culture with U698M-mut mg (effector-to-target (E:T) ratio 1:1) comparing condition without (0 µM) and with 0.5 µM cobimetinib (COB). One representative of three experiments is shown. (d) Representative flow cytometry plots of mCherry, eCFP, and eGFP expression (co-culture setup described in a) with further concentrations of COB (0, 0.05, 0.5, and 1 µM). Comparison is made to an unstimulated control (unstim ctrl) condition. (e-j) Ratio of reporter activity (mCherry, eCFP, and eGFP) in conditions with MEKi compared with 0 µM MEKi after 20 hours co-culture between JE6.1 TPR CD8+ KIF-sc1-Jurkat T cells and either specific stimulation via U698M-mut mg (E:T=1:1, e–g ) or unspecific stimulation with phorbol 12-myristate 13-acetate (PMA)/ionomycin (Iono) ( h–j ) at increasing doses of five different <t>MEKi:</t> <t>selumetinib</t> (SELU), binimetinib (BINI), COB, GDC-0623 (GDC), trametinib (TRA). Mean and SD of three independent experiments are shown. (k-m) Flow cytometry-based measurement of reporter activity for AP-1 (mCherry), NFκB (eCFP), and NFAT (eGFP) in JE6.1 TPR CD8+ KIF-sc1-tg Jurkat cells on co-culture with U698M-mut mg (E:T 1:1) after 24 hours. T cells only (Tc) conditions served as unstimulated background control. Increasing doses of COB (green) were compared with dasatinib (DASA, violet). Mean and SD of experimental triplicates are depicted. (n, o) Flow cytometry-based quantification of T cell receptor (TCR)mu+ T cells after 96 hours of co-culture of KIF-sc1-tg T cells and U698M-mut mg (E:T 1:2 ( n ) or 1:4 ( o ) as indicated above graphs). Percent increase or decrease of TCR-transgenic (tg) T cells compared with conditions without inhibitor (0 µM) is depicted for COB-treated or DASA-treated conditions (concentrations in µM). Mean and SD for three biological triplicates are shown. One-way analysis of variance (ANOVA) with Tukey’s correction for multiple comparisons: **p<0.01, ***p<0.001, ****p<0.0001. (p) CellTrace Violet (CTV)-flow cytometry plots from one representative of three donors comparing increasing doses of COB and DASA with 0 µM condition without inhibitor. (q, r) Flow cytometry-based quantification of dsRed+ tumor cells after 96 hours of co-culture of KIF-sc1-tg T cells and U698M-mut mg (E:T 1:2 ( q ) or 1:4 ( r ) as indicated above graphs). Per cent killing is depicted compared with unspecific control TCR 2.5D6. Mean and SD for three biological triplicates are shown. One-way ANOVA with Tukey’s correction for multiple comparisons: ****p<0.0001. Only significant p values for comparisons with 0.05 µM COB are depicted.
Meki, supplied by MedChemExpress, used in various techniques. Bioz Stars score: 95/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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Average 95 stars, based on 1 article reviews
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m mek inhibitor pd0325901  (TargetMol)
92
TargetMol m mek inhibitor pd0325901
MEK inhibition <t>(MEKi)</t> acts by selective complete inhibition of nuclear factor kappa-light-chain-enhancer of activated B cells (NFκB) and nuclear factor of activated T cells (NFAT) and partial inhibition of activator protein 1 (AP-1) signaling. (a-c) Time course over 24 hours of reporter activity for AP-1 (MCherry fluorescent protein (mCherry)), NFκB (enhanced cyan fluorescent protein (eCFP)), and NFAT (enhanced green fluorescent protein (eGFP)) in JE6.1 triple parameter reporter (TPR) CD8+ KIF-sc1-tg Jurkat cells upon co-culture with U698M-mut mg (effector-to-target (E:T) ratio 1:1) comparing condition without (0 µM) and with 0.5 µM cobimetinib (COB). One representative of three experiments is shown. (d) Representative flow cytometry plots of mCherry, eCFP, and eGFP expression (co-culture setup described in a) with further concentrations of COB (0, 0.05, 0.5, and 1 µM). Comparison is made to an unstimulated control (unstim ctrl) condition. (e-j) Ratio of reporter activity (mCherry, eCFP, and eGFP) in conditions with MEKi compared with 0 µM MEKi after 20 hours co-culture between JE6.1 TPR CD8+ KIF-sc1-Jurkat T cells and either specific stimulation via U698M-mut mg (E:T=1:1, e–g ) or unspecific stimulation with phorbol 12-myristate 13-acetate (PMA)/ionomycin (Iono) ( h–j ) at increasing doses of five different <t>MEKi:</t> <t>selumetinib</t> (SELU), binimetinib (BINI), COB, GDC-0623 (GDC), trametinib (TRA). Mean and SD of three independent experiments are shown. (k-m) Flow cytometry-based measurement of reporter activity for AP-1 (mCherry), NFκB (eCFP), and NFAT (eGFP) in JE6.1 TPR CD8+ KIF-sc1-tg Jurkat cells on co-culture with U698M-mut mg (E:T 1:1) after 24 hours. T cells only (Tc) conditions served as unstimulated background control. Increasing doses of COB (green) were compared with dasatinib (DASA, violet). Mean and SD of experimental triplicates are depicted. (n, o) Flow cytometry-based quantification of T cell receptor (TCR)mu+ T cells after 96 hours of co-culture of KIF-sc1-tg T cells and U698M-mut mg (E:T 1:2 ( n ) or 1:4 ( o ) as indicated above graphs). Percent increase or decrease of TCR-transgenic (tg) T cells compared with conditions without inhibitor (0 µM) is depicted for COB-treated or DASA-treated conditions (concentrations in µM). Mean and SD for three biological triplicates are shown. One-way analysis of variance (ANOVA) with Tukey’s correction for multiple comparisons: **p<0.01, ***p<0.001, ****p<0.0001. (p) CellTrace Violet (CTV)-flow cytometry plots from one representative of three donors comparing increasing doses of COB and DASA with 0 µM condition without inhibitor. (q, r) Flow cytometry-based quantification of dsRed+ tumor cells after 96 hours of co-culture of KIF-sc1-tg T cells and U698M-mut mg (E:T 1:2 ( q ) or 1:4 ( r ) as indicated above graphs). Per cent killing is depicted compared with unspecific control TCR 2.5D6. Mean and SD for three biological triplicates are shown. One-way ANOVA with Tukey’s correction for multiple comparisons: ****p<0.0001. Only significant p values for comparisons with 0.05 µM COB are depicted.
M Mek Inhibitor Pd0325901, supplied by TargetMol, used in various techniques. Bioz Stars score: 92/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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m mek inhibitor pd0325901 - by Bioz Stars, 2026-03
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mek inhibitor  (Santa Cruz Biotechnology)
93
Santa Cruz Biotechnology mek inhibitor
MEK inhibition <t>(MEKi)</t> acts by selective complete inhibition of nuclear factor kappa-light-chain-enhancer of activated B cells (NFκB) and nuclear factor of activated T cells (NFAT) and partial inhibition of activator protein 1 (AP-1) signaling. (a-c) Time course over 24 hours of reporter activity for AP-1 (MCherry fluorescent protein (mCherry)), NFκB (enhanced cyan fluorescent protein (eCFP)), and NFAT (enhanced green fluorescent protein (eGFP)) in JE6.1 triple parameter reporter (TPR) CD8+ KIF-sc1-tg Jurkat cells upon co-culture with U698M-mut mg (effector-to-target (E:T) ratio 1:1) comparing condition without (0 µM) and with 0.5 µM cobimetinib (COB). One representative of three experiments is shown. (d) Representative flow cytometry plots of mCherry, eCFP, and eGFP expression (co-culture setup described in a) with further concentrations of COB (0, 0.05, 0.5, and 1 µM). Comparison is made to an unstimulated control (unstim ctrl) condition. (e-j) Ratio of reporter activity (mCherry, eCFP, and eGFP) in conditions with MEKi compared with 0 µM MEKi after 20 hours co-culture between JE6.1 TPR CD8+ KIF-sc1-Jurkat T cells and either specific stimulation via U698M-mut mg (E:T=1:1, e–g ) or unspecific stimulation with phorbol 12-myristate 13-acetate (PMA)/ionomycin (Iono) ( h–j ) at increasing doses of five different <t>MEKi:</t> <t>selumetinib</t> (SELU), binimetinib (BINI), COB, GDC-0623 (GDC), trametinib (TRA). Mean and SD of three independent experiments are shown. (k-m) Flow cytometry-based measurement of reporter activity for AP-1 (mCherry), NFκB (eCFP), and NFAT (eGFP) in JE6.1 TPR CD8+ KIF-sc1-tg Jurkat cells on co-culture with U698M-mut mg (E:T 1:1) after 24 hours. T cells only (Tc) conditions served as unstimulated background control. Increasing doses of COB (green) were compared with dasatinib (DASA, violet). Mean and SD of experimental triplicates are depicted. (n, o) Flow cytometry-based quantification of T cell receptor (TCR)mu+ T cells after 96 hours of co-culture of KIF-sc1-tg T cells and U698M-mut mg (E:T 1:2 ( n ) or 1:4 ( o ) as indicated above graphs). Percent increase or decrease of TCR-transgenic (tg) T cells compared with conditions without inhibitor (0 µM) is depicted for COB-treated or DASA-treated conditions (concentrations in µM). Mean and SD for three biological triplicates are shown. One-way analysis of variance (ANOVA) with Tukey’s correction for multiple comparisons: **p<0.01, ***p<0.001, ****p<0.0001. (p) CellTrace Violet (CTV)-flow cytometry plots from one representative of three donors comparing increasing doses of COB and DASA with 0 µM condition without inhibitor. (q, r) Flow cytometry-based quantification of dsRed+ tumor cells after 96 hours of co-culture of KIF-sc1-tg T cells and U698M-mut mg (E:T 1:2 ( q ) or 1:4 ( r ) as indicated above graphs). Per cent killing is depicted compared with unspecific control TCR 2.5D6. Mean and SD for three biological triplicates are shown. One-way ANOVA with Tukey’s correction for multiple comparisons: ****p<0.0001. Only significant p values for comparisons with 0.05 µM COB are depicted.
Mek Inhibitor, supplied by Santa Cruz Biotechnology, used in various techniques. Bioz Stars score: 93/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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Average 93 stars, based on 1 article reviews
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gdc 0623  (MedChemExpress)
93
MedChemExpress gdc 0623
MEK inhibition <t>(MEKi)</t> acts by selective complete inhibition of nuclear factor kappa-light-chain-enhancer of activated B cells (NFκB) and nuclear factor of activated T cells (NFAT) and partial inhibition of activator protein 1 (AP-1) signaling. (a-c) Time course over 24 hours of reporter activity for AP-1 (MCherry fluorescent protein (mCherry)), NFκB (enhanced cyan fluorescent protein (eCFP)), and NFAT (enhanced green fluorescent protein (eGFP)) in JE6.1 triple parameter reporter (TPR) CD8+ KIF-sc1-tg Jurkat cells upon co-culture with U698M-mut mg (effector-to-target (E:T) ratio 1:1) comparing condition without (0 µM) and with 0.5 µM cobimetinib (COB). One representative of three experiments is shown. (d) Representative flow cytometry plots of mCherry, eCFP, and eGFP expression (co-culture setup described in a) with further concentrations of COB (0, 0.05, 0.5, and 1 µM). Comparison is made to an unstimulated control (unstim ctrl) condition. (e-j) Ratio of reporter activity (mCherry, eCFP, and eGFP) in conditions with MEKi compared with 0 µM MEKi after 20 hours co-culture between JE6.1 TPR CD8+ KIF-sc1-Jurkat T cells and either specific stimulation via U698M-mut mg (E:T=1:1, e–g ) or unspecific stimulation with phorbol 12-myristate 13-acetate (PMA)/ionomycin (Iono) ( h–j ) at increasing doses of five different <t>MEKi:</t> <t>selumetinib</t> (SELU), binimetinib (BINI), COB, GDC-0623 (GDC), trametinib (TRA). Mean and SD of three independent experiments are shown. (k-m) Flow cytometry-based measurement of reporter activity for AP-1 (mCherry), NFκB (eCFP), and NFAT (eGFP) in JE6.1 TPR CD8+ KIF-sc1-tg Jurkat cells on co-culture with U698M-mut mg (E:T 1:1) after 24 hours. T cells only (Tc) conditions served as unstimulated background control. Increasing doses of COB (green) were compared with dasatinib (DASA, violet). Mean and SD of experimental triplicates are depicted. (n, o) Flow cytometry-based quantification of T cell receptor (TCR)mu+ T cells after 96 hours of co-culture of KIF-sc1-tg T cells and U698M-mut mg (E:T 1:2 ( n ) or 1:4 ( o ) as indicated above graphs). Percent increase or decrease of TCR-transgenic (tg) T cells compared with conditions without inhibitor (0 µM) is depicted for COB-treated or DASA-treated conditions (concentrations in µM). Mean and SD for three biological triplicates are shown. One-way analysis of variance (ANOVA) with Tukey’s correction for multiple comparisons: **p<0.01, ***p<0.001, ****p<0.0001. (p) CellTrace Violet (CTV)-flow cytometry plots from one representative of three donors comparing increasing doses of COB and DASA with 0 µM condition without inhibitor. (q, r) Flow cytometry-based quantification of dsRed+ tumor cells after 96 hours of co-culture of KIF-sc1-tg T cells and U698M-mut mg (E:T 1:2 ( q ) or 1:4 ( r ) as indicated above graphs). Per cent killing is depicted compared with unspecific control TCR 2.5D6. Mean and SD for three biological triplicates are shown. One-way ANOVA with Tukey’s correction for multiple comparisons: ****p<0.0001. Only significant p values for comparisons with 0.05 µM COB are depicted.
Gdc 0623, supplied by MedChemExpress, used in various techniques. Bioz Stars score: 93/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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pd0325901  (ReproCELL)
95
ReproCELL pd0325901
MEK inhibition <t>(MEKi)</t> acts by selective complete inhibition of nuclear factor kappa-light-chain-enhancer of activated B cells (NFκB) and nuclear factor of activated T cells (NFAT) and partial inhibition of activator protein 1 (AP-1) signaling. (a-c) Time course over 24 hours of reporter activity for AP-1 (MCherry fluorescent protein (mCherry)), NFκB (enhanced cyan fluorescent protein (eCFP)), and NFAT (enhanced green fluorescent protein (eGFP)) in JE6.1 triple parameter reporter (TPR) CD8+ KIF-sc1-tg Jurkat cells upon co-culture with U698M-mut mg (effector-to-target (E:T) ratio 1:1) comparing condition without (0 µM) and with 0.5 µM cobimetinib (COB). One representative of three experiments is shown. (d) Representative flow cytometry plots of mCherry, eCFP, and eGFP expression (co-culture setup described in a) with further concentrations of COB (0, 0.05, 0.5, and 1 µM). Comparison is made to an unstimulated control (unstim ctrl) condition. (e-j) Ratio of reporter activity (mCherry, eCFP, and eGFP) in conditions with MEKi compared with 0 µM MEKi after 20 hours co-culture between JE6.1 TPR CD8+ KIF-sc1-Jurkat T cells and either specific stimulation via U698M-mut mg (E:T=1:1, e–g ) or unspecific stimulation with phorbol 12-myristate 13-acetate (PMA)/ionomycin (Iono) ( h–j ) at increasing doses of five different <t>MEKi:</t> <t>selumetinib</t> (SELU), binimetinib (BINI), COB, GDC-0623 (GDC), trametinib (TRA). Mean and SD of three independent experiments are shown. (k-m) Flow cytometry-based measurement of reporter activity for AP-1 (mCherry), NFκB (eCFP), and NFAT (eGFP) in JE6.1 TPR CD8+ KIF-sc1-tg Jurkat cells on co-culture with U698M-mut mg (E:T 1:1) after 24 hours. T cells only (Tc) conditions served as unstimulated background control. Increasing doses of COB (green) were compared with dasatinib (DASA, violet). Mean and SD of experimental triplicates are depicted. (n, o) Flow cytometry-based quantification of T cell receptor (TCR)mu+ T cells after 96 hours of co-culture of KIF-sc1-tg T cells and U698M-mut mg (E:T 1:2 ( n ) or 1:4 ( o ) as indicated above graphs). Percent increase or decrease of TCR-transgenic (tg) T cells compared with conditions without inhibitor (0 µM) is depicted for COB-treated or DASA-treated conditions (concentrations in µM). Mean and SD for three biological triplicates are shown. One-way analysis of variance (ANOVA) with Tukey’s correction for multiple comparisons: **p<0.01, ***p<0.001, ****p<0.0001. (p) CellTrace Violet (CTV)-flow cytometry plots from one representative of three donors comparing increasing doses of COB and DASA with 0 µM condition without inhibitor. (q, r) Flow cytometry-based quantification of dsRed+ tumor cells after 96 hours of co-culture of KIF-sc1-tg T cells and U698M-mut mg (E:T 1:2 ( q ) or 1:4 ( r ) as indicated above graphs). Per cent killing is depicted compared with unspecific control TCR 2.5D6. Mean and SD for three biological triplicates are shown. One-way ANOVA with Tukey’s correction for multiple comparisons: ****p<0.0001. Only significant p values for comparisons with 0.05 µM COB are depicted.
Pd0325901, supplied by ReproCELL, used in various techniques. Bioz Stars score: 95/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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mek inhibitor  (BOC Sciences)
90
BOC Sciences mek inhibitor
MEK inhibition <t>(MEKi)</t> acts by selective complete inhibition of nuclear factor kappa-light-chain-enhancer of activated B cells (NFκB) and nuclear factor of activated T cells (NFAT) and partial inhibition of activator protein 1 (AP-1) signaling. (a-c) Time course over 24 hours of reporter activity for AP-1 (MCherry fluorescent protein (mCherry)), NFκB (enhanced cyan fluorescent protein (eCFP)), and NFAT (enhanced green fluorescent protein (eGFP)) in JE6.1 triple parameter reporter (TPR) CD8+ KIF-sc1-tg Jurkat cells upon co-culture with U698M-mut mg (effector-to-target (E:T) ratio 1:1) comparing condition without (0 µM) and with 0.5 µM cobimetinib (COB). One representative of three experiments is shown. (d) Representative flow cytometry plots of mCherry, eCFP, and eGFP expression (co-culture setup described in a) with further concentrations of COB (0, 0.05, 0.5, and 1 µM). Comparison is made to an unstimulated control (unstim ctrl) condition. (e-j) Ratio of reporter activity (mCherry, eCFP, and eGFP) in conditions with MEKi compared with 0 µM MEKi after 20 hours co-culture between JE6.1 TPR CD8+ KIF-sc1-Jurkat T cells and either specific stimulation via U698M-mut mg (E:T=1:1, e–g ) or unspecific stimulation with phorbol 12-myristate 13-acetate (PMA)/ionomycin (Iono) ( h–j ) at increasing doses of five different <t>MEKi:</t> <t>selumetinib</t> (SELU), binimetinib (BINI), COB, GDC-0623 (GDC), trametinib (TRA). Mean and SD of three independent experiments are shown. (k-m) Flow cytometry-based measurement of reporter activity for AP-1 (mCherry), NFκB (eCFP), and NFAT (eGFP) in JE6.1 TPR CD8+ KIF-sc1-tg Jurkat cells on co-culture with U698M-mut mg (E:T 1:1) after 24 hours. T cells only (Tc) conditions served as unstimulated background control. Increasing doses of COB (green) were compared with dasatinib (DASA, violet). Mean and SD of experimental triplicates are depicted. (n, o) Flow cytometry-based quantification of T cell receptor (TCR)mu+ T cells after 96 hours of co-culture of KIF-sc1-tg T cells and U698M-mut mg (E:T 1:2 ( n ) or 1:4 ( o ) as indicated above graphs). Percent increase or decrease of TCR-transgenic (tg) T cells compared with conditions without inhibitor (0 µM) is depicted for COB-treated or DASA-treated conditions (concentrations in µM). Mean and SD for three biological triplicates are shown. One-way analysis of variance (ANOVA) with Tukey’s correction for multiple comparisons: **p<0.01, ***p<0.001, ****p<0.0001. (p) CellTrace Violet (CTV)-flow cytometry plots from one representative of three donors comparing increasing doses of COB and DASA with 0 µM condition without inhibitor. (q, r) Flow cytometry-based quantification of dsRed+ tumor cells after 96 hours of co-culture of KIF-sc1-tg T cells and U698M-mut mg (E:T 1:2 ( q ) or 1:4 ( r ) as indicated above graphs). Per cent killing is depicted compared with unspecific control TCR 2.5D6. Mean and SD for three biological triplicates are shown. One-way ANOVA with Tukey’s correction for multiple comparisons: ****p<0.0001. Only significant p values for comparisons with 0.05 µM COB are depicted.
Mek Inhibitor, supplied by BOC Sciences, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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mek erk1 2 inhibitor  (Santa Cruz Biotechnology)
85
Santa Cruz Biotechnology mek erk1 2 inhibitor
MEK inhibition <t>(MEKi)</t> acts by selective complete inhibition of nuclear factor kappa-light-chain-enhancer of activated B cells (NFκB) and nuclear factor of activated T cells (NFAT) and partial inhibition of activator protein 1 (AP-1) signaling. (a-c) Time course over 24 hours of reporter activity for AP-1 (MCherry fluorescent protein (mCherry)), NFκB (enhanced cyan fluorescent protein (eCFP)), and NFAT (enhanced green fluorescent protein (eGFP)) in JE6.1 triple parameter reporter (TPR) CD8+ KIF-sc1-tg Jurkat cells upon co-culture with U698M-mut mg (effector-to-target (E:T) ratio 1:1) comparing condition without (0 µM) and with 0.5 µM cobimetinib (COB). One representative of three experiments is shown. (d) Representative flow cytometry plots of mCherry, eCFP, and eGFP expression (co-culture setup described in a) with further concentrations of COB (0, 0.05, 0.5, and 1 µM). Comparison is made to an unstimulated control (unstim ctrl) condition. (e-j) Ratio of reporter activity (mCherry, eCFP, and eGFP) in conditions with MEKi compared with 0 µM MEKi after 20 hours co-culture between JE6.1 TPR CD8+ KIF-sc1-Jurkat T cells and either specific stimulation via U698M-mut mg (E:T=1:1, e–g ) or unspecific stimulation with phorbol 12-myristate 13-acetate (PMA)/ionomycin (Iono) ( h–j ) at increasing doses of five different <t>MEKi:</t> <t>selumetinib</t> (SELU), binimetinib (BINI), COB, GDC-0623 (GDC), trametinib (TRA). Mean and SD of three independent experiments are shown. (k-m) Flow cytometry-based measurement of reporter activity for AP-1 (mCherry), NFκB (eCFP), and NFAT (eGFP) in JE6.1 TPR CD8+ KIF-sc1-tg Jurkat cells on co-culture with U698M-mut mg (E:T 1:1) after 24 hours. T cells only (Tc) conditions served as unstimulated background control. Increasing doses of COB (green) were compared with dasatinib (DASA, violet). Mean and SD of experimental triplicates are depicted. (n, o) Flow cytometry-based quantification of T cell receptor (TCR)mu+ T cells after 96 hours of co-culture of KIF-sc1-tg T cells and U698M-mut mg (E:T 1:2 ( n ) or 1:4 ( o ) as indicated above graphs). Percent increase or decrease of TCR-transgenic (tg) T cells compared with conditions without inhibitor (0 µM) is depicted for COB-treated or DASA-treated conditions (concentrations in µM). Mean and SD for three biological triplicates are shown. One-way analysis of variance (ANOVA) with Tukey’s correction for multiple comparisons: **p<0.01, ***p<0.001, ****p<0.0001. (p) CellTrace Violet (CTV)-flow cytometry plots from one representative of three donors comparing increasing doses of COB and DASA with 0 µM condition without inhibitor. (q, r) Flow cytometry-based quantification of dsRed+ tumor cells after 96 hours of co-culture of KIF-sc1-tg T cells and U698M-mut mg (E:T 1:2 ( q ) or 1:4 ( r ) as indicated above graphs). Per cent killing is depicted compared with unspecific control TCR 2.5D6. Mean and SD for three biological triplicates are shown. One-way ANOVA with Tukey’s correction for multiple comparisons: ****p<0.0001. Only significant p values for comparisons with 0.05 µM COB are depicted.
Mek Erk1 2 Inhibitor, supplied by Santa Cruz Biotechnology, used in various techniques. Bioz Stars score: 85/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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arry-886  (Array BioPharma)
90
Array BioPharma arry-886
MEK inhibition <t>(MEKi)</t> acts by selective complete inhibition of nuclear factor kappa-light-chain-enhancer of activated B cells (NFκB) and nuclear factor of activated T cells (NFAT) and partial inhibition of activator protein 1 (AP-1) signaling. (a-c) Time course over 24 hours of reporter activity for AP-1 (MCherry fluorescent protein (mCherry)), NFκB (enhanced cyan fluorescent protein (eCFP)), and NFAT (enhanced green fluorescent protein (eGFP)) in JE6.1 triple parameter reporter (TPR) CD8+ KIF-sc1-tg Jurkat cells upon co-culture with U698M-mut mg (effector-to-target (E:T) ratio 1:1) comparing condition without (0 µM) and with 0.5 µM cobimetinib (COB). One representative of three experiments is shown. (d) Representative flow cytometry plots of mCherry, eCFP, and eGFP expression (co-culture setup described in a) with further concentrations of COB (0, 0.05, 0.5, and 1 µM). Comparison is made to an unstimulated control (unstim ctrl) condition. (e-j) Ratio of reporter activity (mCherry, eCFP, and eGFP) in conditions with MEKi compared with 0 µM MEKi after 20 hours co-culture between JE6.1 TPR CD8+ KIF-sc1-Jurkat T cells and either specific stimulation via U698M-mut mg (E:T=1:1, e–g ) or unspecific stimulation with phorbol 12-myristate 13-acetate (PMA)/ionomycin (Iono) ( h–j ) at increasing doses of five different <t>MEKi:</t> <t>selumetinib</t> (SELU), binimetinib (BINI), COB, GDC-0623 (GDC), trametinib (TRA). Mean and SD of three independent experiments are shown. (k-m) Flow cytometry-based measurement of reporter activity for AP-1 (mCherry), NFκB (eCFP), and NFAT (eGFP) in JE6.1 TPR CD8+ KIF-sc1-tg Jurkat cells on co-culture with U698M-mut mg (E:T 1:1) after 24 hours. T cells only (Tc) conditions served as unstimulated background control. Increasing doses of COB (green) were compared with dasatinib (DASA, violet). Mean and SD of experimental triplicates are depicted. (n, o) Flow cytometry-based quantification of T cell receptor (TCR)mu+ T cells after 96 hours of co-culture of KIF-sc1-tg T cells and U698M-mut mg (E:T 1:2 ( n ) or 1:4 ( o ) as indicated above graphs). Percent increase or decrease of TCR-transgenic (tg) T cells compared with conditions without inhibitor (0 µM) is depicted for COB-treated or DASA-treated conditions (concentrations in µM). Mean and SD for three biological triplicates are shown. One-way analysis of variance (ANOVA) with Tukey’s correction for multiple comparisons: **p<0.01, ***p<0.001, ****p<0.0001. (p) CellTrace Violet (CTV)-flow cytometry plots from one representative of three donors comparing increasing doses of COB and DASA with 0 µM condition without inhibitor. (q, r) Flow cytometry-based quantification of dsRed+ tumor cells after 96 hours of co-culture of KIF-sc1-tg T cells and U698M-mut mg (E:T 1:2 ( q ) or 1:4 ( r ) as indicated above graphs). Per cent killing is depicted compared with unspecific control TCR 2.5D6. Mean and SD for three biological triplicates are shown. One-way ANOVA with Tukey’s correction for multiple comparisons: ****p<0.0001. Only significant p values for comparisons with 0.05 µM COB are depicted.
Arry 886, supplied by Array BioPharma, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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mek inhibitor u0126  (Blackwell Science Ltd)
90
Blackwell Science Ltd mek inhibitor u0126
MEK inhibition <t>(MEKi)</t> acts by selective complete inhibition of nuclear factor kappa-light-chain-enhancer of activated B cells (NFκB) and nuclear factor of activated T cells (NFAT) and partial inhibition of activator protein 1 (AP-1) signaling. (a-c) Time course over 24 hours of reporter activity for AP-1 (MCherry fluorescent protein (mCherry)), NFκB (enhanced cyan fluorescent protein (eCFP)), and NFAT (enhanced green fluorescent protein (eGFP)) in JE6.1 triple parameter reporter (TPR) CD8+ KIF-sc1-tg Jurkat cells upon co-culture with U698M-mut mg (effector-to-target (E:T) ratio 1:1) comparing condition without (0 µM) and with 0.5 µM cobimetinib (COB). One representative of three experiments is shown. (d) Representative flow cytometry plots of mCherry, eCFP, and eGFP expression (co-culture setup described in a) with further concentrations of COB (0, 0.05, 0.5, and 1 µM). Comparison is made to an unstimulated control (unstim ctrl) condition. (e-j) Ratio of reporter activity (mCherry, eCFP, and eGFP) in conditions with MEKi compared with 0 µM MEKi after 20 hours co-culture between JE6.1 TPR CD8+ KIF-sc1-Jurkat T cells and either specific stimulation via U698M-mut mg (E:T=1:1, e–g ) or unspecific stimulation with phorbol 12-myristate 13-acetate (PMA)/ionomycin (Iono) ( h–j ) at increasing doses of five different <t>MEKi:</t> <t>selumetinib</t> (SELU), binimetinib (BINI), COB, GDC-0623 (GDC), trametinib (TRA). Mean and SD of three independent experiments are shown. (k-m) Flow cytometry-based measurement of reporter activity for AP-1 (mCherry), NFκB (eCFP), and NFAT (eGFP) in JE6.1 TPR CD8+ KIF-sc1-tg Jurkat cells on co-culture with U698M-mut mg (E:T 1:1) after 24 hours. T cells only (Tc) conditions served as unstimulated background control. Increasing doses of COB (green) were compared with dasatinib (DASA, violet). Mean and SD of experimental triplicates are depicted. (n, o) Flow cytometry-based quantification of T cell receptor (TCR)mu+ T cells after 96 hours of co-culture of KIF-sc1-tg T cells and U698M-mut mg (E:T 1:2 ( n ) or 1:4 ( o ) as indicated above graphs). Percent increase or decrease of TCR-transgenic (tg) T cells compared with conditions without inhibitor (0 µM) is depicted for COB-treated or DASA-treated conditions (concentrations in µM). Mean and SD for three biological triplicates are shown. One-way analysis of variance (ANOVA) with Tukey’s correction for multiple comparisons: **p<0.01, ***p<0.001, ****p<0.0001. (p) CellTrace Violet (CTV)-flow cytometry plots from one representative of three donors comparing increasing doses of COB and DASA with 0 µM condition without inhibitor. (q, r) Flow cytometry-based quantification of dsRed+ tumor cells after 96 hours of co-culture of KIF-sc1-tg T cells and U698M-mut mg (E:T 1:2 ( q ) or 1:4 ( r ) as indicated above graphs). Per cent killing is depicted compared with unspecific control TCR 2.5D6. Mean and SD for three biological triplicates are shown. One-way ANOVA with Tukey’s correction for multiple comparisons: ****p<0.0001. Only significant p values for comparisons with 0.05 µM COB are depicted.
Mek Inhibitor U0126, supplied by Blackwell Science Ltd, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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mek inhibitor u0126 - by Bioz Stars, 2026-03
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erk inhibitor pd98059  (Funakoshi ltd)
90
Funakoshi ltd erk inhibitor pd98059
MEK inhibition <t>(MEKi)</t> acts by selective complete inhibition of nuclear factor kappa-light-chain-enhancer of activated B cells (NFκB) and nuclear factor of activated T cells (NFAT) and partial inhibition of activator protein 1 (AP-1) signaling. (a-c) Time course over 24 hours of reporter activity for AP-1 (MCherry fluorescent protein (mCherry)), NFκB (enhanced cyan fluorescent protein (eCFP)), and NFAT (enhanced green fluorescent protein (eGFP)) in JE6.1 triple parameter reporter (TPR) CD8+ KIF-sc1-tg Jurkat cells upon co-culture with U698M-mut mg (effector-to-target (E:T) ratio 1:1) comparing condition without (0 µM) and with 0.5 µM cobimetinib (COB). One representative of three experiments is shown. (d) Representative flow cytometry plots of mCherry, eCFP, and eGFP expression (co-culture setup described in a) with further concentrations of COB (0, 0.05, 0.5, and 1 µM). Comparison is made to an unstimulated control (unstim ctrl) condition. (e-j) Ratio of reporter activity (mCherry, eCFP, and eGFP) in conditions with MEKi compared with 0 µM MEKi after 20 hours co-culture between JE6.1 TPR CD8+ KIF-sc1-Jurkat T cells and either specific stimulation via U698M-mut mg (E:T=1:1, e–g ) or unspecific stimulation with phorbol 12-myristate 13-acetate (PMA)/ionomycin (Iono) ( h–j ) at increasing doses of five different <t>MEKi:</t> <t>selumetinib</t> (SELU), binimetinib (BINI), COB, GDC-0623 (GDC), trametinib (TRA). Mean and SD of three independent experiments are shown. (k-m) Flow cytometry-based measurement of reporter activity for AP-1 (mCherry), NFκB (eCFP), and NFAT (eGFP) in JE6.1 TPR CD8+ KIF-sc1-tg Jurkat cells on co-culture with U698M-mut mg (E:T 1:1) after 24 hours. T cells only (Tc) conditions served as unstimulated background control. Increasing doses of COB (green) were compared with dasatinib (DASA, violet). Mean and SD of experimental triplicates are depicted. (n, o) Flow cytometry-based quantification of T cell receptor (TCR)mu+ T cells after 96 hours of co-culture of KIF-sc1-tg T cells and U698M-mut mg (E:T 1:2 ( n ) or 1:4 ( o ) as indicated above graphs). Percent increase or decrease of TCR-transgenic (tg) T cells compared with conditions without inhibitor (0 µM) is depicted for COB-treated or DASA-treated conditions (concentrations in µM). Mean and SD for three biological triplicates are shown. One-way analysis of variance (ANOVA) with Tukey’s correction for multiple comparisons: **p<0.01, ***p<0.001, ****p<0.0001. (p) CellTrace Violet (CTV)-flow cytometry plots from one representative of three donors comparing increasing doses of COB and DASA with 0 µM condition without inhibitor. (q, r) Flow cytometry-based quantification of dsRed+ tumor cells after 96 hours of co-culture of KIF-sc1-tg T cells and U698M-mut mg (E:T 1:2 ( q ) or 1:4 ( r ) as indicated above graphs). Per cent killing is depicted compared with unspecific control TCR 2.5D6. Mean and SD for three biological triplicates are shown. One-way ANOVA with Tukey’s correction for multiple comparisons: ****p<0.0001. Only significant p values for comparisons with 0.05 µM COB are depicted.
Erk Inhibitor Pd98059, supplied by Funakoshi ltd, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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erk inhibitor pd98059 - by Bioz Stars, 2026-03
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trametinib (mek inhibitor, #16292, (tr)  (Cayman Chemical)
90
Cayman Chemical trametinib (mek inhibitor, #16292, (tr)
MEK inhibition <t>(MEKi)</t> acts by selective complete inhibition of nuclear factor kappa-light-chain-enhancer of activated B cells (NFκB) and nuclear factor of activated T cells (NFAT) and partial inhibition of activator protein 1 (AP-1) signaling. (a-c) Time course over 24 hours of reporter activity for AP-1 (MCherry fluorescent protein (mCherry)), NFκB (enhanced cyan fluorescent protein (eCFP)), and NFAT (enhanced green fluorescent protein (eGFP)) in JE6.1 triple parameter reporter (TPR) CD8+ KIF-sc1-tg Jurkat cells upon co-culture with U698M-mut mg (effector-to-target (E:T) ratio 1:1) comparing condition without (0 µM) and with 0.5 µM cobimetinib (COB). One representative of three experiments is shown. (d) Representative flow cytometry plots of mCherry, eCFP, and eGFP expression (co-culture setup described in a) with further concentrations of COB (0, 0.05, 0.5, and 1 µM). Comparison is made to an unstimulated control (unstim ctrl) condition. (e-j) Ratio of reporter activity (mCherry, eCFP, and eGFP) in conditions with MEKi compared with 0 µM MEKi after 20 hours co-culture between JE6.1 TPR CD8+ KIF-sc1-Jurkat T cells and either specific stimulation via U698M-mut mg (E:T=1:1, e–g ) or unspecific stimulation with phorbol 12-myristate 13-acetate (PMA)/ionomycin (Iono) ( h–j ) at increasing doses of five different <t>MEKi:</t> <t>selumetinib</t> (SELU), binimetinib (BINI), COB, GDC-0623 (GDC), trametinib (TRA). Mean and SD of three independent experiments are shown. (k-m) Flow cytometry-based measurement of reporter activity for AP-1 (mCherry), NFκB (eCFP), and NFAT (eGFP) in JE6.1 TPR CD8+ KIF-sc1-tg Jurkat cells on co-culture with U698M-mut mg (E:T 1:1) after 24 hours. T cells only (Tc) conditions served as unstimulated background control. Increasing doses of COB (green) were compared with dasatinib (DASA, violet). Mean and SD of experimental triplicates are depicted. (n, o) Flow cytometry-based quantification of T cell receptor (TCR)mu+ T cells after 96 hours of co-culture of KIF-sc1-tg T cells and U698M-mut mg (E:T 1:2 ( n ) or 1:4 ( o ) as indicated above graphs). Percent increase or decrease of TCR-transgenic (tg) T cells compared with conditions without inhibitor (0 µM) is depicted for COB-treated or DASA-treated conditions (concentrations in µM). Mean and SD for three biological triplicates are shown. One-way analysis of variance (ANOVA) with Tukey’s correction for multiple comparisons: **p<0.01, ***p<0.001, ****p<0.0001. (p) CellTrace Violet (CTV)-flow cytometry plots from one representative of three donors comparing increasing doses of COB and DASA with 0 µM condition without inhibitor. (q, r) Flow cytometry-based quantification of dsRed+ tumor cells after 96 hours of co-culture of KIF-sc1-tg T cells and U698M-mut mg (E:T 1:2 ( q ) or 1:4 ( r ) as indicated above graphs). Per cent killing is depicted compared with unspecific control TCR 2.5D6. Mean and SD for three biological triplicates are shown. One-way ANOVA with Tukey’s correction for multiple comparisons: ****p<0.0001. Only significant p values for comparisons with 0.05 µM COB are depicted.
Trametinib (Mek Inhibitor, #16292, (Tr), supplied by Cayman Chemical, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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Average 90 stars, based on 1 article reviews
trametinib (mek inhibitor, #16292, (tr) - by Bioz Stars, 2026-03
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mek inhibitors  (Rauscher GmbH)
90
Rauscher GmbH mek inhibitors
MEK inhibition <t>(MEKi)</t> acts by selective complete inhibition of nuclear factor kappa-light-chain-enhancer of activated B cells (NFκB) and nuclear factor of activated T cells (NFAT) and partial inhibition of activator protein 1 (AP-1) signaling. (a-c) Time course over 24 hours of reporter activity for AP-1 (MCherry fluorescent protein (mCherry)), NFκB (enhanced cyan fluorescent protein (eCFP)), and NFAT (enhanced green fluorescent protein (eGFP)) in JE6.1 triple parameter reporter (TPR) CD8+ KIF-sc1-tg Jurkat cells upon co-culture with U698M-mut mg (effector-to-target (E:T) ratio 1:1) comparing condition without (0 µM) and with 0.5 µM cobimetinib (COB). One representative of three experiments is shown. (d) Representative flow cytometry plots of mCherry, eCFP, and eGFP expression (co-culture setup described in a) with further concentrations of COB (0, 0.05, 0.5, and 1 µM). Comparison is made to an unstimulated control (unstim ctrl) condition. (e-j) Ratio of reporter activity (mCherry, eCFP, and eGFP) in conditions with MEKi compared with 0 µM MEKi after 20 hours co-culture between JE6.1 TPR CD8+ KIF-sc1-Jurkat T cells and either specific stimulation via U698M-mut mg (E:T=1:1, e–g ) or unspecific stimulation with phorbol 12-myristate 13-acetate (PMA)/ionomycin (Iono) ( h–j ) at increasing doses of five different <t>MEKi:</t> <t>selumetinib</t> (SELU), binimetinib (BINI), COB, GDC-0623 (GDC), trametinib (TRA). Mean and SD of three independent experiments are shown. (k-m) Flow cytometry-based measurement of reporter activity for AP-1 (mCherry), NFκB (eCFP), and NFAT (eGFP) in JE6.1 TPR CD8+ KIF-sc1-tg Jurkat cells on co-culture with U698M-mut mg (E:T 1:1) after 24 hours. T cells only (Tc) conditions served as unstimulated background control. Increasing doses of COB (green) were compared with dasatinib (DASA, violet). Mean and SD of experimental triplicates are depicted. (n, o) Flow cytometry-based quantification of T cell receptor (TCR)mu+ T cells after 96 hours of co-culture of KIF-sc1-tg T cells and U698M-mut mg (E:T 1:2 ( n ) or 1:4 ( o ) as indicated above graphs). Percent increase or decrease of TCR-transgenic (tg) T cells compared with conditions without inhibitor (0 µM) is depicted for COB-treated or DASA-treated conditions (concentrations in µM). Mean and SD for three biological triplicates are shown. One-way analysis of variance (ANOVA) with Tukey’s correction for multiple comparisons: **p<0.01, ***p<0.001, ****p<0.0001. (p) CellTrace Violet (CTV)-flow cytometry plots from one representative of three donors comparing increasing doses of COB and DASA with 0 µM condition without inhibitor. (q, r) Flow cytometry-based quantification of dsRed+ tumor cells after 96 hours of co-culture of KIF-sc1-tg T cells and U698M-mut mg (E:T 1:2 ( q ) or 1:4 ( r ) as indicated above graphs). Per cent killing is depicted compared with unspecific control TCR 2.5D6. Mean and SD for three biological triplicates are shown. One-way ANOVA with Tukey’s correction for multiple comparisons: ****p<0.0001. Only significant p values for comparisons with 0.05 µM COB are depicted.
Mek Inhibitors, supplied by Rauscher GmbH, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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Average 90 stars, based on 1 article reviews
mek inhibitors - by Bioz Stars, 2026-03
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Image Search Results


MEK inhibition (MEKi) acts by selective complete inhibition of nuclear factor kappa-light-chain-enhancer of activated B cells (NFκB) and nuclear factor of activated T cells (NFAT) and partial inhibition of activator protein 1 (AP-1) signaling. (a-c) Time course over 24 hours of reporter activity for AP-1 (MCherry fluorescent protein (mCherry)), NFκB (enhanced cyan fluorescent protein (eCFP)), and NFAT (enhanced green fluorescent protein (eGFP)) in JE6.1 triple parameter reporter (TPR) CD8+ KIF-sc1-tg Jurkat cells upon co-culture with U698M-mut mg (effector-to-target (E:T) ratio 1:1) comparing condition without (0 µM) and with 0.5 µM cobimetinib (COB). One representative of three experiments is shown. (d) Representative flow cytometry plots of mCherry, eCFP, and eGFP expression (co-culture setup described in a) with further concentrations of COB (0, 0.05, 0.5, and 1 µM). Comparison is made to an unstimulated control (unstim ctrl) condition. (e-j) Ratio of reporter activity (mCherry, eCFP, and eGFP) in conditions with MEKi compared with 0 µM MEKi after 20 hours co-culture between JE6.1 TPR CD8+ KIF-sc1-Jurkat T cells and either specific stimulation via U698M-mut mg (E:T=1:1, e–g ) or unspecific stimulation with phorbol 12-myristate 13-acetate (PMA)/ionomycin (Iono) ( h–j ) at increasing doses of five different MEKi: selumetinib (SELU), binimetinib (BINI), COB, GDC-0623 (GDC), trametinib (TRA). Mean and SD of three independent experiments are shown. (k-m) Flow cytometry-based measurement of reporter activity for AP-1 (mCherry), NFκB (eCFP), and NFAT (eGFP) in JE6.1 TPR CD8+ KIF-sc1-tg Jurkat cells on co-culture with U698M-mut mg (E:T 1:1) after 24 hours. T cells only (Tc) conditions served as unstimulated background control. Increasing doses of COB (green) were compared with dasatinib (DASA, violet). Mean and SD of experimental triplicates are depicted. (n, o) Flow cytometry-based quantification of T cell receptor (TCR)mu+ T cells after 96 hours of co-culture of KIF-sc1-tg T cells and U698M-mut mg (E:T 1:2 ( n ) or 1:4 ( o ) as indicated above graphs). Percent increase or decrease of TCR-transgenic (tg) T cells compared with conditions without inhibitor (0 µM) is depicted for COB-treated or DASA-treated conditions (concentrations in µM). Mean and SD for three biological triplicates are shown. One-way analysis of variance (ANOVA) with Tukey’s correction for multiple comparisons: **p<0.01, ***p<0.001, ****p<0.0001. (p) CellTrace Violet (CTV)-flow cytometry plots from one representative of three donors comparing increasing doses of COB and DASA with 0 µM condition without inhibitor. (q, r) Flow cytometry-based quantification of dsRed+ tumor cells after 96 hours of co-culture of KIF-sc1-tg T cells and U698M-mut mg (E:T 1:2 ( q ) or 1:4 ( r ) as indicated above graphs). Per cent killing is depicted compared with unspecific control TCR 2.5D6. Mean and SD for three biological triplicates are shown. One-way ANOVA with Tukey’s correction for multiple comparisons: ****p<0.0001. Only significant p values for comparisons with 0.05 µM COB are depicted.

Journal: Journal for Immunotherapy of Cancer

Article Title: Tempered signal strength via low-dose MEK inhibition optimizes therapeutic performance of engineered T cells

doi: 10.1136/jitc-2025-012800

Figure Lengend Snippet: MEK inhibition (MEKi) acts by selective complete inhibition of nuclear factor kappa-light-chain-enhancer of activated B cells (NFκB) and nuclear factor of activated T cells (NFAT) and partial inhibition of activator protein 1 (AP-1) signaling. (a-c) Time course over 24 hours of reporter activity for AP-1 (MCherry fluorescent protein (mCherry)), NFκB (enhanced cyan fluorescent protein (eCFP)), and NFAT (enhanced green fluorescent protein (eGFP)) in JE6.1 triple parameter reporter (TPR) CD8+ KIF-sc1-tg Jurkat cells upon co-culture with U698M-mut mg (effector-to-target (E:T) ratio 1:1) comparing condition without (0 µM) and with 0.5 µM cobimetinib (COB). One representative of three experiments is shown. (d) Representative flow cytometry plots of mCherry, eCFP, and eGFP expression (co-culture setup described in a) with further concentrations of COB (0, 0.05, 0.5, and 1 µM). Comparison is made to an unstimulated control (unstim ctrl) condition. (e-j) Ratio of reporter activity (mCherry, eCFP, and eGFP) in conditions with MEKi compared with 0 µM MEKi after 20 hours co-culture between JE6.1 TPR CD8+ KIF-sc1-Jurkat T cells and either specific stimulation via U698M-mut mg (E:T=1:1, e–g ) or unspecific stimulation with phorbol 12-myristate 13-acetate (PMA)/ionomycin (Iono) ( h–j ) at increasing doses of five different MEKi: selumetinib (SELU), binimetinib (BINI), COB, GDC-0623 (GDC), trametinib (TRA). Mean and SD of three independent experiments are shown. (k-m) Flow cytometry-based measurement of reporter activity for AP-1 (mCherry), NFκB (eCFP), and NFAT (eGFP) in JE6.1 TPR CD8+ KIF-sc1-tg Jurkat cells on co-culture with U698M-mut mg (E:T 1:1) after 24 hours. T cells only (Tc) conditions served as unstimulated background control. Increasing doses of COB (green) were compared with dasatinib (DASA, violet). Mean and SD of experimental triplicates are depicted. (n, o) Flow cytometry-based quantification of T cell receptor (TCR)mu+ T cells after 96 hours of co-culture of KIF-sc1-tg T cells and U698M-mut mg (E:T 1:2 ( n ) or 1:4 ( o ) as indicated above graphs). Percent increase or decrease of TCR-transgenic (tg) T cells compared with conditions without inhibitor (0 µM) is depicted for COB-treated or DASA-treated conditions (concentrations in µM). Mean and SD for three biological triplicates are shown. One-way analysis of variance (ANOVA) with Tukey’s correction for multiple comparisons: **p<0.01, ***p<0.001, ****p<0.0001. (p) CellTrace Violet (CTV)-flow cytometry plots from one representative of three donors comparing increasing doses of COB and DASA with 0 µM condition without inhibitor. (q, r) Flow cytometry-based quantification of dsRed+ tumor cells after 96 hours of co-culture of KIF-sc1-tg T cells and U698M-mut mg (E:T 1:2 ( q ) or 1:4 ( r ) as indicated above graphs). Per cent killing is depicted compared with unspecific control TCR 2.5D6. Mean and SD for three biological triplicates are shown. One-way ANOVA with Tukey’s correction for multiple comparisons: ****p<0.0001. Only significant p values for comparisons with 0.05 µM COB are depicted.

Article Snippet: To compare different MEKi, we performed analyses comprising five different MEKi (all MedChem Express): selumetinib (SELU) (catalog HY-50706), binimetinib (BINI) (catalog HY-15202), COB, GDC-0623 (GDC) (catalog HY-15610), trametinib (catalog HY-10999).

Techniques: Inhibition, Activity Assay, Co-Culture Assay, Flow Cytometry, Expressing, Comparison, Control, Transgenic Assay