Chemical Structure : CPI-455
CAS No.: 1628208-23-0
Catalog No.: 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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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.
M.Wt | 278.3086 | |
Formula | C16H14N4O | |
Appearance | Solid | |
Storage |
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Solubility |
DMSO: ≥ 34 mg/mL |
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Chemical Name/SMILES |
Pyrazolo[1,5-a]pyrimidine-3-carbonitrile, 4,7-dihydro-6-(1-methylethyl)-7-oxo-5-phenyl- |
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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