CBP/p300-IN-5

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-5 

P300/CBP-IN-5 是一种有效的 p300/CBP 组蛋白乙酰转移酶 (histone acetyltransferase) 抑制剂,其 IC50 值为 18.8 nM。详细信息请参考专利文献 WO2016044770A1 中的 Example 715。

CBP/p300-IN-5

CBP/p300-IN-5 Chemical Structure

CAS No. : 1889284-33-6

规格 是否有货
5 mg 询价

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生物活性

P300/CBP-IN-5 is a potent p300/CBP histone acetyltransferase inhibitor extracted from patent WO2016044770A1, Example 715, has an IC50 of 18.8 nM[1].

IC50 & Target

IC50: 18.8 nM (p300/CBP)[1]

体外研究
(In Vitro)

P300/CBP-IN-5 inhibits p300 LnCap-FGC cellls proliferation with an IC50 of 14.8 nM. P300/CBP-IN-5 inhibits H3K27Ac with an IC50 value of 4.6 nM in PC-3 cells[1].

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

体内研究
(In Vivo)

The effect of P300/CBP-IN-5 (Example 715) on tumor growth is evaluated in subcutaneous, SuDHL-8 (B-cell lymphoma) and 22RV1 (prostate) xenograft tumors implanted in SCID female mice. Human cancer cells are inoculated subcutaneously into the right hind flank of female SCID mice on study day 0. Administration of P300/CBP-IN-5 (7.5 mg/kg/day) is initiated at the time of size match. P300/CBP-IN-5 induces significant tumor growth inhibition in multiple xenograft tumor models (the tumor growth inhibition of 62% in SuDHL-8 xenograft tumor model; 48% in 22RV1 xenograft tumor model)[1].

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

分子量

618.55

Formula

C29H27F5N6O4

CAS 号

1889284-33-6

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]. Michael Michaelides, et al. Spirocyclic hat inhibitors and methods for their use. WO2016044770A1.

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