CBP/p300-IN-19

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CBP/p300-IN-19 

CBP/p300-IN-19 是一种有效的 p300/CBP HAT 抑制剂，p300-HAT, CBP-HAT, PCAF, Myst3 的 IC50s 分别为 1.4, 2.2, >100, > 100 µM。CBP/p300-IN-19 显示出抗肿瘤活性。

CBP/p300-IN-19

CBP/p300-IN-19 Chemical Structure

CAS No. : 2592638-13-4

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生物活性

CBP/p300-IN-19 is a potent p300/CBP HAT inhibitor with IC50s of 1.4, 2.2, >100, >100 µM for p300-HAT, CBP-HAT, PCAF, Myst3, respectively. CBP/p300-IN-19 shows antitumor activity[1].

IC50 & Target[1]

p300

1.4 μM (IC50)

PCAF

2.2 μM (IC50)

CBP

>100 μM (IC50)

Myst3

>100 μM (IC50)

体外研究
(In Vitro)

CBP/p300-IN-19 (compound 29) shows antiproliferative activity with EC50s of 5.3, 8.5, 6.2, 4.4, 1.2, 4.3, 3.6, 8.7, 6.4 µM for MCF-7, MDA-MB231, LNCaP, PC-3, PANC-1, MDA-PANC-28, Molm-13, MV4;11, RPMI-8226 cells, respectively[1].
CBP/p300-IN-19 (0, 5, 10 µM; 12 h) dose-dependenly inhibits the acetylation of H3K18, H3K9 and K27[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: Kasumi-1 leukemia cells
Concentration: 0, 5, 10 µM
Incubation Time: 12 h
Result: Dose-dependently inhibited the acetylation of H3K18, H3K9 and K27.

分子量

477.55

Formula

C30H27N3O3
CAS 号

2592638-13-4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Nie S, et al. Structure-activity relationship and antitumor activity of 1,4-pyrazine-containing inhibitors of histone acetyltransferases P300/CBP. Eur J Med Chem. 2022 Jul 5;237:114407.

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