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

CAS No.: 1628208-23-0

6-Isopropyl-7-oxo-5-phenyl-4,7-dihydropyrazolo[1,5-a]pyrimidine-3-carbonitrile Catalog No. CSN16898

Synonyms: CPI-455

CPI-455 is a selective inhibitor of KDM5 demethylases and can reduce survival of drug-tolerant cancer cells.

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技术信息

生物活性

描述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.^[2]
参考文献

[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
- 3.5931 mL
- 17.9657 mL
- 35.9313 mL
- 5 mM
- 0.7186 mL
- 3.5931 mL
- 7.1863 mL
- 10 mM
- 0.3593 mL
- 1.7966 mL
- 3.5931 mL

技术信息

CAS号

1628208-23-0

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H14N4O

运输

蓝冰

分子量

278.31

别名

CPI-455

溶解度

DMSO	34.0 mg/mL (122.2 mM)

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6-Isopropyl-7-oxo-5-phenyl-4,7-dihydropyrazolo[1,5-a]pyrimidine-3-carbonitrile Catalog No. CSN16898

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