DCH36_06 (C09-1125-747)

DCH36_06 is a potent and selective p300/CBP inhibitor with IC 50 s of 0.6 μM and 3.2 μM for p300 and CBP , respectively. DCH36_06 mediated p300/CBP inhibition leading to hypoacetylation on H3K18 in leukemic cells. Anti-tumor activity.In VitroDCH36_06 (6.7-20 μM; 24-48 hours) treatment arrests cell cycle at G1 phase and induces apotosis in a dose-dependent manner in leukemic cells. DCH36_06 (5-10 μM; 24 hours) treatment significantly activates the cleavage of pro-caspase 3, pro-caspase 9 and PARP1 at dose-dependent manner. DCH36_06 shows potent antiproliferative activity against tested leukemia cell lines (CEM, MOLT3, MOLT4, Jurkat, MV4-11, THP-1, RS4; 11, KOPN8, Kasumi-1 and K562 cells) in a dose-dependent manner with IC50 values at single-digit micromolar range. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Cycle AnalysisCell Line: MV4-11 cells Concentration: 6.7 μM, 20 μM Incubation Time: 24 hours, 48 hours Result: Dose-dependently arrested cell cycle at G1 phase. Apoptosis AnalysisCell Line: MV4-11 cells Concentration: 6.7 μM, 20 μM Incubation Time: 24 hours, 48 hours Result: Significantly induced apoptosis. Western Blot AnalysisCell Line: MV4-11 cells Concentration: 5 μM, 10 μM Incubation Time: 24 hours Result: Significantly activated the cleavage of pro-caspase 3, pro-caspase 9 and PARP1 at dose-dependent manner.In VivoDCH36_06 (25-50 mg/kg; intraperitoneal injection; every two days; for 20 days) blocks the leukemic xenograft growth in mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: MV4-11 xenograft nude mice Dosage: 25 mg/kg, 50 mg/kg Administration: Intraperitoneal injection; every two days; for 20 days Result: The tumor growth rate showed significant reduction in dose-dependent manner.Form:Solid. Specifications and Purity: 99%. Molecular Formula: C18H13ClN2O3S. Molecular Weight: 372.83. PubChem CID: 1797299. Isomeric SMILES: CC1=C(C=C(C=C1)N2C(=O)/C(=C/C=C/C3=CC=CO3)/C(=O)NC2=S)Cl.