Journal: Annals of Hematology

Article Title: The BET bromodomain inhibitor ZEN-3365 targets the Hedgehog signaling pathway in acute myeloid leukemia

doi: 10.1007/s00277-021-04602-z

Figure Lengend Snippet: BET inhibitor ZEN-3365 reduces GLI reporter activity in vitro. a Western blot of GLI protein levels under ZEN-3365 treatment. MV4-11, MOLM13, and OCI-AML3 were cultivated for 3 days with 100 or 200 nM ZEN-3365. b GLI promoter assays reveal the dependence of GLI expression and BRD4 regulation. MV4-11, HL-60, Kasumi-1, and OCI-AML3 were treated with different concentrations of ZEN-3365 (25 to 2500 nM) for 24 h. c Time course experiment for BRD4 inhibition with 25, 50, 250, 1000, and 2500 nM ZEN-3365 on MV4-11 cells reveals a stable inhibitory function over 4 days

Article Snippet: AML cell lines or primary AML blasts were cultured with different concentrations of the GLI inhibitor GANT-61 (2,20-[[Dihydro-2-(4-pyridinyl)-1,3(2H,4H)-pyrimidinediyl]bis(methylene)]bis[N,N-dimethylbenzenamine]; Tocris Bioscience) or the BET inhibitor ZEN-3365 (Zenith Epigenetics) either alone or in combination or dimethyl sulfoxide (DMSO, Sigma-Aldrich) as solvent control.

Techniques: Activity Assay, In Vitro, Western Blot, Expressing, Inhibition

Journal: Annals of Hematology

Article Title: The BET bromodomain inhibitor ZEN-3365 targets the Hedgehog signaling pathway in acute myeloid leukemia

doi: 10.1007/s00277-021-04602-z

Figure Lengend Snippet: Combinatorial treatment of AML reporter cell lines with ZEN-3365 and GANT-61 decreases GLI reporter activity in vitro. a MV4-11, b MOLM13, c Kasumi-1, and d HL60 reporter cell lines were treated with 2500 or 5000 nM GANT-61 and 50 nM or 100 nM ZEN-3365 for 24 h. Significance calculated against GANT-61 single treatment, * p < 0.05, ** p < 0.01, and ns = not significant

Article Snippet: AML cell lines or primary AML blasts were cultured with different concentrations of the GLI inhibitor GANT-61 (2,20-[[Dihydro-2-(4-pyridinyl)-1,3(2H,4H)-pyrimidinediyl]bis(methylene)]bis[N,N-dimethylbenzenamine]; Tocris Bioscience) or the BET inhibitor ZEN-3365 (Zenith Epigenetics) either alone or in combination or dimethyl sulfoxide (DMSO, Sigma-Aldrich) as solvent control.

Techniques: Activity Assay, In Vitro

Journal: Annals of Hematology

Article Title: The BET bromodomain inhibitor ZEN-3365 targets the Hedgehog signaling pathway in acute myeloid leukemia

doi: 10.1007/s00277-021-04602-z

Figure Lengend Snippet: ZEN-3365 and GANT-61 present antiproliferative effects. GANT-61 (5 or 10 μM) and ZEN-3365 (100 or 200 nM) inhibit cell proliferation over 7 days for a MV4-11, b HL60, c KG-1, d MOLM13, e Kasumi-1, and f OCI-AML3. g Combinatorial treatment of primary AML sample with GANT-61 (5 or 10 M) and ZEN-3365 (100 or 200 nM) leads to a decreased cell proliferation after 4 days. Significance calculated against GANT-61 treatment alone, * p <0.05, ** p <0.01, and ns=not significant

Article Snippet: AML cell lines or primary AML blasts were cultured with different concentrations of the GLI inhibitor GANT-61 (2,20-[[Dihydro-2-(4-pyridinyl)-1,3(2H,4H)-pyrimidinediyl]bis(methylene)]bis[N,N-dimethylbenzenamine]; Tocris Bioscience) or the BET inhibitor ZEN-3365 (Zenith Epigenetics) either alone or in combination or dimethyl sulfoxide (DMSO, Sigma-Aldrich) as solvent control.

Techniques:

Journal: Annals of Hematology

Article Title: The BET bromodomain inhibitor ZEN-3365 targets the Hedgehog signaling pathway in acute myeloid leukemia

doi: 10.1007/s00277-021-04602-z

Figure Lengend Snippet: The colony formation potential of AML cell lines is decreased under single or combinatorial treatment. a MV4-11, b MOLM13, c OCI-AML3, and d HL60 were treated with 5 μM GANT-61 and 0.1 μM ZEN-3365 or in combination and cultured in methocult medium for one week. Colony numbers were counted with an inverted microscope. * p <0.05, ** p <0.01, and ns=not significant

Article Snippet: AML cell lines or primary AML blasts were cultured with different concentrations of the GLI inhibitor GANT-61 (2,20-[[Dihydro-2-(4-pyridinyl)-1,3(2H,4H)-pyrimidinediyl]bis(methylene)]bis[N,N-dimethylbenzenamine]; Tocris Bioscience) or the BET inhibitor ZEN-3365 (Zenith Epigenetics) either alone or in combination or dimethyl sulfoxide (DMSO, Sigma-Aldrich) as solvent control.

Techniques: Cell Culture, Inverted Microscopy