CPI-455 | B1881

CPI-455 is a potent and selective KDM5A inhibitor (IC₅₀ ~10 nM). It inhibits KDM5A, KDM5B and KDM5C to similar extents but shows substantially weaker potency toward KDM4C and KDM7B (~200- and 770-fold, respectively) and no detectable inhibition of KDM2B, KDM3B or KDM6A. It specifically alters H3K4 methylation in cells and binds at the demethylase active site. CPI-455-mediated KDM5 inhibition leads to a dose-dependent increase in global H3K4me3 in HeLa cells, and the removal of CPI-455 resulted in a rapid reversal of H3K4me3 increases in HeLa cells.

CPI-455 is a potent and selective KDM5A inhibitor (IC₅₀ ~10 nM). It inhibits KDM5A, KDM5B and KDM5C to similar extents but shows substantially weaker potency toward KDM4C and KDM7B (~200- and 770-fold, respectively) and no detectable inhibition of KDM2B, KDM3B or KDM6A. It specifically alters H3K4 methylation in cells and binds at the demethylase active site. CPI-455-mediated KDM5 inhibition leads to a dose-dependent increase in global H3K4me3 in HeLa cells, and the removal of CPI-455 resulted in a rapid reversal of H3K4me3 increases in HeLa cells.

B1881 | CPI-455 DataSheet

Alternate Name/Synonyms: 6-Isopropyl-7-oxo-5-phenyl-4,7-dihydropyrazolo[1,5-a]pyrimidine-3-carbonitrile

Appearance: White to off-white solid

Formulation: N/A

CAS Number: 1628208-23-0

Structure Available?: Yes

Peptide sequence: N/A

Salt Form: No

Molecular Formula: C₁₆H₁₄N₄O

Molecular Weight: 278.31

Cell-Permeable?: Yes

Purity: ≥98% by HPLC

Solubilities: DMSO

Handling: Protect from air and light

Country of Origin: USA

Tag Line: A potent and selective KDM5A inhibitor

MDL Number: N/A

PubChem CID: 78426698

SMILES: CC(C)C1=C(N=C2C(=CNN2C1=O)C#N)C3=CC=CC=C3

InChi: InChI=1S/C16H14N4O/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

InChi Key: VGXRQCOVGLGFIM-UHFFFAOYSA-N