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CPI-455

A potent and selective KDM5A inhibitor
Catalog #: B1881

In stock

SKU-Size Size Price Qty
B1881-5 5 mg
$125.00
B1881-25 25 mg
$495.00
More Sizes Get Quote

Product Details

Alternate Name 6-Isopropyl-7-oxo-5-phenyl-4,7-dihydropyrazolo[1,5-a]pyrimidine-3-carbonitrile
Appearance White to off-white solid
CAS # 1628208-23-0 
Molecular Formula C₁₆H₁₄N₄O
Molecular Weight 278.31
Purity ≥98% by HPLC
Solubility DMSO
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
PubChem CID 78426698
Handling Protect from air and light
Storage Conditions -20°C
Shipping Conditions Gel Pack
USAGE For Research Use Only! Not For Use in Humans.

Details

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.


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