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DCH36_06 Sale

目录号 : GC63627

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

DCH36_06 Chemical Structure

Cas No.:593273-05-3

规格 价格 库存 购买数量
5 mg
¥1,620.00
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10 mg
¥2,880.00
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25 mg
¥4,770.00
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50 mg
¥8,550.00
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产品描述

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].

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].

DCH36_06 (25-50 mg/kg; intraperitoneal injection; every two days; for 20 days) blocks the leukemic xenograft growth in mice[1].

[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.

Chemical Properties

Cas No. 593273-05-3 SDF
分子式 C18H13ClN2O3S 分子量 372.83
溶解度 DMSO : 125 mg/mL (335.27 mM; Need ultrasonic) 储存条件 4°C, protect from light
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1 mM 2.6822 mL 13.4109 mL 26.8219 mL
5 mM 0.5364 mL 2.6822 mL 5.3644 mL
10 mM 0.2682 mL 1.3411 mL 2.6822 mL
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Research Update

Discovery and biological evaluation of thiobarbituric derivatives as potent p300/CBP inhibitors

Bioorg Med Chem 2018 Nov 1;26(20):5397-5407.PMID:30297119DOI:10.1016/j.bmc.2018.07.048

Histone acetyltransferases (HATs) relieve transcriptional repression by preferentially acetylation of ε-amino group of lysine residues on histones. Dysregulation of HATs is strongly correlated with etiology of several diseases especially cancer, thus highlighting the utmost significance of the development of small molecule inhibitors against this potential therapeutic target. In the present study, through virtual screening and iterative optimization, we identified DCH36_06 as a bona fide, 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. Importantly, 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. Taken together, our findings suggest that DCH36_06 may serve as a qualified chemical tool to decode the acetylome code and open up new opportunities for clinical intervention.