DCH36_06 是一种选择性p300/CBP抑制剂，介导 p300/CBP 抑制导致白血病细胞中 H3K18 的低乙酰化，有抗肿瘤活性，对p300和CBP的IC50分别为 0.6 μM 和 3.2 μM。

DCH36_06 as a bona fide is a potent p300/CBP inhibitor

DCH36_06 mediated p300/CBP inhibition leading to hypoacetylation on H3K18 in leukemic cells. The suppression of p300/CBP activity retarded cell proliferation in several leukemic cell lines.In addition, DCH36_06 arrested cell cycle at G1 phase and induced apoptosis via activation of capase3, caspase9 and PARP that elucidated the molecular mechanism of its anti-proliferation activity. In transcriptome analysis, DCH36_06 altered downstream gene expression and apoptotic pathways-related genes verified by real-time PCR[1].

DCH36_06 blocked the leukemic xenograft growth in mice supporting its potential for?in vivo?use that underlies the therapeutic potential for p300/CBP inhibitors in clinical translation[1].

593273-05-3

C18H13ClN2O3S

372.83

(5E)-1-(3-chloro-4-methylphenyl)-5-[(2E)-3-(furan-2-yl)prop-2-en-1-ylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione

DMSO:120mg/mL (321.86mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years