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CPI-455

Chemical Structure : CPI-455

CAS No.: 1628208-23-0

CPI-455 (CPI455;CPI 455)

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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 278.3086
Formula C16H14N4O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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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-

References

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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