593273-05-3

593273-05-3 structure

Name: DCH36_06
Chemical Name: DCH36_06
CAS Number: 593273-05-3
Molecular Formula: C₁₈H₁₃ClN₂O₃S
Molecular Weight: 372.83
Catalog: Signaling Pathways Apoptosis Apoptosis
Create Date: 2021-09-09 07:41:23
Modify Date: 2024-01-08 12:56:38
DCH36_06 is a potent and selective p300/CBP inhibitor with IC50s 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[1].

Name	DCH36_06

Description	DCH36_06 is a potent and selective p300/CBP inhibitor with IC50s 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[1].
Related Catalog	Signaling Pathways >> Apoptosis >> Apoptosis Research Areas >> Cancer Signaling Pathways >> Epigenetics >> Histone Acetyltransferase
In Vitro	DCH36_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[1]. 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[1]. 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[1]. Cell Cycle Analysis[1] Cell 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 Analysis[1] Cell Line: MV4-11 cells Concentration: 6.7 μM, 20 μM Incubation Time: 24 hours, 48 hours Result: Significantly induced apoptosis. Western Blot Analysis[1] Cell 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 Vivo	DCH36_06 (25-50 mg/kg; intraperitoneal injection; every two days; for 20 days) blocks the leukemic xenograft growth in mice[1]. Animal Model: MV4-11 xenograft nude mice[1] 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.
References	[1]. Wenchao Lu, et al. Discovery and biological evaluation of thiobarbituric derivatives as potent p300/CBP inhibitors. Bioorg Med Chem. 2018 Nov 1;26(20):5397-5407.

Molecular Formula	C₁₈H₁₃ClN₂O₃S
Molecular Weight	372.83

1158522-08-7	940364-43-2
134104-43-1	131615-57-1
6906-52-1	930439-75-1
1018584-77-4	1375289-11-4
1639265-82-9	2580248-64-0