Description
CPI-455 is a specific KDM5 inhibitor with a half-maximal inhibitory concentration (IC50) of 10 ± 1 nM for full-length KDM5A in enzymatic assays, elevating global levels of H3K4 trimethylation (H3K4me3) and decreased the number of DTPs in multiple cancer cell line models treated with standard chemotherapy or targeted agents.
Product information
CAS Number: 2095432-28-1
Molecular Weight: 314.77
Formula: C16H15ClN4O
Chemical Name: 7-oxo-5-phenyl-6-(propan-2-yl)-1H,7H-pyrazolo[1,5-a]pyrimidine-3-carbonitrile hydrochloride
Smiles: Cl.CC(C)C1C(=O)N2NC=C(C#N)C2=NC=1C1C=CC=CC=1
InChiKey: SNODPNXOTKXHHH-UHFFFAOYSA-N
InChi: InChI=1S/C16H14N4O.ClH/c1-10(2)13-14(11-6-4-3-5-7-11)19-15-12(8-17)9-18-20(15)16(13)21;/h3-7,9-10,18H,1-2H3;1H
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Solubility (25°C). 10 mg/mL(31.76 mM). Insoluble.
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
CPI-455 has improved potency against KDM5A while demonstrating ~200-fold selectivity for KDM5A over KDM4C. CPI-455 inhibits KDM5A, KDM5B and KDM5C to similar extents but showed substantially weaker potency toward KDM4C and KDM7B (~200- and 770-fold, respectively) and no measurable inhibition of KDM2B, KDM3B or KDM6A. CPI-455-mediated KDM5 inhibition results in a dose-dependent increase in global H3K4me3 in HeLa cells. CPI-455 specifically alters H3K4 methylation in cells and binds at the demethylase active site.
Products are for research use only. Not for human use.
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