|6-异丙基-7-氧代-5-苯基-4,7-二氢吡唑并[1,5-a]嘧啶-3-腈盐酸盐|CsnPharm

CAS No.: 2095432-28-1

CPI-455盐酸 Catalog No. CSN19243

Synonyms: CPI-455 hydrochloride

CPI-455 HCl is an inhibitor of KDM5. It can elevate global levels of H3K4 trimethylation (H3K4me3) and decrease the number of DTPs in multiple cancer cell line models.

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400-920-2911

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 KDM5A

IC50:10nM
描述CPI-455 Hydrochloride is the hydrochloride form of CPI-455. CPI-455 is a specific KDM5 inhibitor with IC50 value of 10nM for inhibition of full-length KDM5A in enzymatic assays. CPI-455-mediated KDM5 inhibition resulted in a dose-dependent increase in global H3K4me3 in HeLa cells. Also it induced a time-dependent increase in H3K4me3 that was detected only after 2 or more days of treatment. The elevation of H3K4 trimethylation mediated by this inhibition of KDM5 by CPI-455 decreased the number of drug-tolerant state in multiple cancer cell line models treated with standard chemotherapy or targeted agents^[2].
作用机制The nitrile of CPI-455 makes a single interaction with the active-site metal ion of KDM5. The position occupied by CPI-455 completely overlaps the binding site of 2-OG, demonstrating a competitive mode of action.^[1]
动物研究
剂量
Mice: 50 mg/kg, 70 mg/kg^[2] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 50 mg/kg, 70 mg/kg^[2] (i.p.)
给药途径	i.p.

[1] Vinogradova M, Gehling VS, et al. An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells. Nat Chem Biol. 2016 Jul;12(7):531-8.
[2] Vinogradova M, Gehling VS, Gustafson A, Arora S, Tindell CA, Wilson C, Williamson KE, Guler GD, Gangurde P, Manieri W, Busby J, Flynn EM, Lan F, Kim HJ, Odate S, Cochran AG, Liu Y, Wongchenko M, Yang Y, Cheung TK, Maile TM, Lau T, Costa M, Hegde GV, Jackson E, Pitti R, Arnott D, Bailey C, Bellon S, Cummings RT, Albrecht BK, Harmange JC, Kiefer JR, Trojer P, Classon M. An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells. Nat Chem Biol. 2016 Jul;12(7):531-8. doi: 10.1038/nchembio.2085. Epub 2016 May 23. PMID: 27214401.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.1769 mL
- 15.8846 mL
- 31.7693 mL
- 5 mM
- 0.6354 mL
- 3.1769 mL
- 6.3539 mL
- 10 mM
- 0.3177 mL
- 1.5885 mL
- 3.1769 mL

技术信息

CAS号

2095432-28-1

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H15ClN4O

运输

蓝冰

分子量

314.77

别名

CPI-455 hydrochloride

溶解度

DMSO	100.0 mg/mL (317.7 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+water	2 mg/mL	clear
PO	0.5% CMC-Na	45 mg/mL	suspension

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CPI-455盐酸 Catalog No. CSN19243

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