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首页-小分子抑制剂&激动剂-Epigenetics-Histone Demethylase-CPI-455
CPI-455

Chemical Structure : CPI-455

CAS No.: 1628208-23-0

CPI-455 (CPI455;CPI 455)

货号: PC-42148Not For Human Use, Lab Use Only.

CPI-455 is a potent, specific histone demethylase pan-KDM5 inhibitor with biochemical IC50 of 10, 3 and 14 nM for KDM5A, KDM5B and KDM5C, respectively.

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25 mg ¥1680 In stock
50 mg ¥2580 In stock
100 mg ¥3980 In stock
250 mg Get quote

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

CPI-455 is a potent, specific histone demethylase pan-KDM5 inhibitor with biochemical IC50 of 10, 3 and 14 nM for KDM5A, KDM5B and KDM5C, respectively.
CPI-455 shows substantially weaker potency toward KDM4C and KDM7B (200- and 770-fold, respectively) and no inhibition of KDM2B, KDM3B or KDM6A.
CPI-455 dose-dependently increases in H3K4 methylation in multiple cell lines, decreases the number of drug-tolerant persister cancer cells (DTPs) in multiple cancer cell line models treated with standard chemotherapy or targeted agents.

物理化学性质&存储条件

分子量 278.3086
分子式 C16H14N4O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: ≥ 34 mg/mL

Chemical Name/SMILES

Pyrazolo[1,5-a]pyrimidine-3-carbonitrile, 4,7-dihydro-6-(1-methylethyl)-7-oxo-5-phenyl-

参考文献

1. Vinogradova M, et al. Nat Chem Biol. 2016 Jul;12(7):531-8.

2. Banelli B, et al. Oncotarget. 2017 May 23;8(21):34896-34910.

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