fmoc hydrazide  (Chem Impex International)

Journal: Cell

Article Title: CD36-mediated endocytosis of proteolysis-targeting chimeras.

doi: 10.1016/j.cell.2025.03.036

Figure Lengend Snippet: Figure 2. PROTACs depend on CD36-mediated endocytosis for their cellular uptake, activity, and biological properties (A and B) Immunoblotting assays showing shCD36 reverses BRD4 and AR degradation by SIM1-Me (A) and ARV-110 (B), respectively, in LNCaP cells under indicated conditions. (C and D) Metabolomic assays comparing the intracellular drug concentrations of SIM1-Me (C) and ARV-110 (D) in shLuc- or shCD36-LNCaP cells after treatment with SIM1-Me and ARV-110, respectively. Compound concentrations were examined by UPLC-MS after shLuc- or shCD36-LNCaP cells were treated with compounds under indicated conditions, washed with PBS, and lysed by radio-immunoprecipitation assay (RIPA) buffer. Compound concentrations were normalized to the corresponding density of total protein levels by bicinchoninic acid (BCA) assays. Data are mean ± SEM, n = 3. Statistical significance was determined using unpaired t tests; *p % 0.05, ****p % 0.0001. (E and F) Immunoblotting assays showing increasing expression of HA-tagged CD36 protein in shCD36-LNCaP cells restores BRD4 and AR degradation by SIM1-Me (E) and ARV-110 (F), respectively, in LNCaP cells under indicated conditions. (G–J) Viability of shEEA1+Vec-, shLuc+Vec-, shCD36+Vec-, shCD36+CD36-LNCaP cells determined by MTT assays after incubation with increasing concen- trations of SIM1-Me (G), ARV-110 (H), MZ1 (I), or paclitaxel (J). Data are mean ± SEM, n = 3. (K–M) Anti-colony formation effects of SIM-Me (K), ARV-110 (L), or paclitaxel (M) to shLuc- or shCD36-LNCaP cells. (N) Tumor volume after vehicle or ARV-110 treatment (5 mg/kg i.p., every other day [q.o.d.]) for 2 weeks in mice with shLuc, shCD36#1-, and shCD36#2-LNCaP cell xenografts. Data are mean ± SEM, n = 5 mice/group. Statistical significance was determined using two-way ANOVA with Tukey’s multiple-comparisons test; **p % 0.01; ns, not significant.

Article Snippet: REAGENT or RESOURCE SOURCE IDENTIFIER Antibodies Mouse monoclonal anti-a-Tubulin (DM1A) Cell Signaling Technology Cat# 3873; RRID: AB_1904178 Mouse monoclonal anti-b-actin (AC-15) Sigma-Aldrich Cat# A5441; RRID: AB_476744 Mouse Monoclonal Anti- AR (441) Santa Cruz Biotechnology Cat# sc-7305; RRID: AB_626671 Mouse Monoclonal Anti- BRD4 (A-7) Santa Cruz Biotechnology Cat# sc-518021; RRID: AB_2861151 Mouse Monoclonal Anti-EEA1 BD Biosciences Cat# 610457; RRID: AB_397830 Rabbit Monoclonal Anti-AR (ER179(2)) Abcam Cat# ab108341; RRID: AB_10865716 Rabbit Monoclonal Anti-BRD4 (EPR5150(2)) Abcam Cat# ab128874; RRID: AB_11145462 Rabbit onoclonal anti-CD36 (EPR6573) Abcam Cat# ab133625; RRID: AB_2716564 Rabbit monoclonal anti-CD36 (EPR22509-40) Abcam Cat# ab252922; RRID: AB_2922821 Rabbit polyclonal anti- GAPDH (D16H11) Cell Signaling Technology Cat# 5174; RRID: AB_10622025 Rabbit monoclonal anti-Rab5A Cell Signaling Technology Cat# 2143; RRID: AB_823625 Biological samples Prostate cancer tissue microarray TissueArray Cat# PR1921c Chemicals, peptides, and recombinant proteins BDP FL NHS ester Lumiprobe Cat# 61420 Birinapant (CAS # 1260251-31-7) MedChemExpress Cat# HY-16591 Cell proliferation reagent WST-1 Roche Cat# 05015944001 Clarity max western ECL substrate kit BIO-RAD Cat# 1705062 D-(+)-Biotin (CAS # 58-85-5) Thermo Fisher Scientific Cat# BP232-1 D-(+)-Biotin NHS (CAS # 35013-72-0) Combi-Blocks Cat# QA-1959 Doxorubicin (CAS # 23214-92-8) Selleckchem Cat# E2516 Dynabeads MyOne streptavidin T1 Thermo Fisher Scientific Cat# 65601 Human recombinant CD36 protein, ECD, His Tag (HPLC verified) Sino Biological Cat# 10752-H08H Human recombinant CD36 protein, ECD, His Tag (HPLC verified) ACRO Biosystems Cat# CD6-H5221 Lipofectamine RNAiMAX Invitrogen Cat# 13778150 Magic dynabeads MyOne streptavidin T1 Thermo Fisher Scientific Cat# 65601 Mem-PER plus membrane protein extraction kit Thermo Fisher Scientific Cat# 89842 Navitoclax (CAS # 923564-51-6) APExBIO Cat# A3007 NE-PER nuclear and cytoplasmic extraction reagents Thermo Fisher Scientific Cat# 78833 Paclitaxel (CAS # 33069-62-4) Selleckchem Cat# S1150 Polybrene Sigma-Aldrich Cat# TR1003 ProlongGold Life Technologies Cat# P36930 Prostate adenocarcinoma tissue microarray TissueArray Cat# PR1921c Protease inhibitor cocktail Roche Cat# 04693132001 Rapalink-1 (CAS # 1887095-82-0) MedChemExpress Cat# HY-111373 Rapamycin (CAS # 53123-88-9) MedChemExpress Cat# HY-10219 Thiazolyl blue tetrazolium bromide Sigma-Aldrich Cat# M5655 (Continued on next page) e1 Cell 188, 1–19.e1–e6, June 12, 2025

Techniques: Activity Assay, Western Blot, Radio Immunoprecipitation, Expressing, Incubation

Journal: Cell

Article Title: CD36-mediated endocytosis of proteolysis-targeting chimeras.

doi: 10.1016/j.cell.2025.03.036

Figure Lengend Snippet: Figure 5. ShCD36 reverses the cytotoxicity of representative bRo5 drugs in HCC1806 TNBC cells and 22Rv1 PCa cells (A–G) Structures of rapalink-1 (A), rapamycin (B), navitoclax (C), birinapant (D), tubacin (E), doxorubicin (F), and paclitaxel (G). (H–P) Viability of shLuc+Vec-, shCD36+Vec-, shCD36+CD36-HCC1806 cells determined by MTT assays after incubation with increasing concentrations of SIM1- Me (H), SIM (I), rapalink-1 (J), rapamycin (K), navitoclax (L), birinapant (M), tubacin (N), doxorubicin (O), and paclitaxel (P) for 6 days. Data are mean ± SEM, n = 3. (Q–Y) Viability of shLuc+Vec-, shCD36+Vec-, shCD36+CD36-22Rv1 cells determined by MTT assays after incubation with increasing concentrations of SIM1-Me (Q), ARV-110 (R), rapalink-1 (S), rapamycin (T), navitoclax (U), birinapant (V), tubacin (W), doxorubicin (X), and paclitaxel (Y) for 6 days. Data are mean ± SEM, n = 3. See also Figure S2.

Article Snippet: REAGENT or RESOURCE SOURCE IDENTIFIER Antibodies Mouse monoclonal anti-a-Tubulin (DM1A) Cell Signaling Technology Cat# 3873; RRID: AB_1904178 Mouse monoclonal anti-b-actin (AC-15) Sigma-Aldrich Cat# A5441; RRID: AB_476744 Mouse Monoclonal Anti- AR (441) Santa Cruz Biotechnology Cat# sc-7305; RRID: AB_626671 Mouse Monoclonal Anti- BRD4 (A-7) Santa Cruz Biotechnology Cat# sc-518021; RRID: AB_2861151 Mouse Monoclonal Anti-EEA1 BD Biosciences Cat# 610457; RRID: AB_397830 Rabbit Monoclonal Anti-AR (ER179(2)) Abcam Cat# ab108341; RRID: AB_10865716 Rabbit Monoclonal Anti-BRD4 (EPR5150(2)) Abcam Cat# ab128874; RRID: AB_11145462 Rabbit onoclonal anti-CD36 (EPR6573) Abcam Cat# ab133625; RRID: AB_2716564 Rabbit monoclonal anti-CD36 (EPR22509-40) Abcam Cat# ab252922; RRID: AB_2922821 Rabbit polyclonal anti- GAPDH (D16H11) Cell Signaling Technology Cat# 5174; RRID: AB_10622025 Rabbit monoclonal anti-Rab5A Cell Signaling Technology Cat# 2143; RRID: AB_823625 Biological samples Prostate cancer tissue microarray TissueArray Cat# PR1921c Chemicals, peptides, and recombinant proteins BDP FL NHS ester Lumiprobe Cat# 61420 Birinapant (CAS # 1260251-31-7) MedChemExpress Cat# HY-16591 Cell proliferation reagent WST-1 Roche Cat# 05015944001 Clarity max western ECL substrate kit BIO-RAD Cat# 1705062 D-(+)-Biotin (CAS # 58-85-5) Thermo Fisher Scientific Cat# BP232-1 D-(+)-Biotin NHS (CAS # 35013-72-0) Combi-Blocks Cat# QA-1959 Doxorubicin (CAS # 23214-92-8) Selleckchem Cat# E2516 Dynabeads MyOne streptavidin T1 Thermo Fisher Scientific Cat# 65601 Human recombinant CD36 protein, ECD, His Tag (HPLC verified) Sino Biological Cat# 10752-H08H Human recombinant CD36 protein, ECD, His Tag (HPLC verified) ACRO Biosystems Cat# CD6-H5221 Lipofectamine RNAiMAX Invitrogen Cat# 13778150 Magic dynabeads MyOne streptavidin T1 Thermo Fisher Scientific Cat# 65601 Mem-PER plus membrane protein extraction kit Thermo Fisher Scientific Cat# 89842 Navitoclax (CAS # 923564-51-6) APExBIO Cat# A3007 NE-PER nuclear and cytoplasmic extraction reagents Thermo Fisher Scientific Cat# 78833 Paclitaxel (CAS # 33069-62-4) Selleckchem Cat# S1150 Polybrene Sigma-Aldrich Cat# TR1003 ProlongGold Life Technologies Cat# P36930 Prostate adenocarcinoma tissue microarray TissueArray Cat# PR1921c Protease inhibitor cocktail Roche Cat# 04693132001 Rapalink-1 (CAS # 1887095-82-0) MedChemExpress Cat# HY-111373 Rapamycin (CAS # 53123-88-9) MedChemExpress Cat# HY-10219 Thiazolyl blue tetrazolium bromide Sigma-Aldrich Cat# M5655 (Continued on next page) e1 Cell 188, 1–19.e1–e6, June 12, 2025

Techniques: Incubation

Journal: Pharmaceutics

Article Title: Solubilization of Paclitaxel with Natural Compound Rubusoside toward Improving Oral Bioavailability in a Rodent Model

doi: 10.3390/pharmaceutics16081104

Figure Lengend Snippet: Composition of paclitaxel formulations for oral and intravenous administration.

Article Snippet: Paclitaxel (PTX; 33069-62-4; purity 99%) was obtained from LC Laboratories (Woburn, MA, USA).

Techniques: Formulation

Journal: Pharmaceutics

Article Title: Solubilization of Paclitaxel with Natural Compound Rubusoside toward Improving Oral Bioavailability in a Rodent Model

doi: 10.3390/pharmaceutics16081104

Figure Lengend Snippet: Particle size (nm) distribution detected in a 10% w / v RUB-solubilized paclitaxel (Nano-PTX) nanoparticle dispersion. ( a ): Size distribution by frequency. ( b ): Cumulative distribution.

Article Snippet: Paclitaxel (PTX; 33069-62-4; purity 99%) was obtained from LC Laboratories (Woburn, MA, USA).

Techniques: Dispersion

Journal: Pharmaceutics

Article Title: Solubilization of Paclitaxel with Natural Compound Rubusoside toward Improving Oral Bioavailability in a Rodent Model

doi: 10.3390/pharmaceutics16081104

Figure Lengend Snippet: Paclitaxel formulations for oral and intravenous administration.

Article Snippet: Paclitaxel (PTX; 33069-62-4; purity 99%) was obtained from LC Laboratories (Woburn, MA, USA).

Techniques: Solvent, Concentration Assay

Journal: Pharmaceutics

Article Title: Solubilization of Paclitaxel with Natural Compound Rubusoside toward Improving Oral Bioavailability in a Rodent Model

doi: 10.3390/pharmaceutics16081104

Figure Lengend Snippet: Time–concentration curves of Taxol ® (solid circle) and Nano-PTX (open circle) orally dosed at 20 mg/kg to Sprague Dawley rats. Taxol ® was diluted from the liquid drug with water and used as the PTX control. Nano-PTX formulation was prepared by reconstituting water-soluble powder with water and then diluted with water at the time of oral gavage. Each data point represents the mean of six replicates (n = 6). Vertical bars across each data point represent one standard error.

Article Snippet: Paclitaxel (PTX; 33069-62-4; purity 99%) was obtained from LC Laboratories (Woburn, MA, USA).

Techniques: Concentration Assay, Control, Formulation

Journal: Pharmaceutics

Article Title: Solubilization of Paclitaxel with Natural Compound Rubusoside toward Improving Oral Bioavailability in a Rodent Model

doi: 10.3390/pharmaceutics16081104

Figure Lengend Snippet: Time–concentration curves of two paclitaxel formulations intravenously administered at 2 mg/kg dose to Sprague Dawley rats. Taxol ® (solid circles) was diluted from the liquid drug and used as the control. Nano-PTX formulation (open circles) was prepared by reconstituting water-soluble powder with water and then diluted with saline at the time of injection via the pre-installed cannulation. Each data point represents the mean of six replicates. Vertical bars across each data point represent one standard error.

Article Snippet: Paclitaxel (PTX; 33069-62-4; purity 99%) was obtained from LC Laboratories (Woburn, MA, USA).

Techniques: Concentration Assay, Control, Formulation, Saline, Injection