CPI-455

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Chemical Structure| 1628208-23-0 同义名 : -
CAS号 : 1628208-23-0
货号 : A145136
分子式 : C16H14N4O
纯度 : 98%
分子量 : 278.31
MDL号 : MFCD29921343
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(125.76 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • KDM6

    KDM5, IC50:10 nM

  • KDM5

    KDM5, IC50:10 nM

  • KDM5

    KDM5A, IC50:10 nM
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]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.59mL

0.72mL

0.36mL

17.97mL

3.59mL

1.80mL

35.93mL

7.19mL

3.59mL
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.