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Catalog:
SLK-S8287
Brand:
Selleck
CAS:
2095432-28-1
Overview
MDL
-
Molecular Weight
314.77
Molecular Formula
C16H15ClN4O
SMILES
N#CC1=C2NC(C3=CC=CC=C3)=C(C(C)C)C(N2N=C1)=O.[H]Cl
For research use only.
Storage
3 years,-20°C,powder 1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
1 mg
5 mg
10 mg
1 mM
3.1769 mL
15.8846 mL
31.7692 mL
5 mM
0.6354 mL
3.1769 mL
6.3538 mL
10 mM
0.3177 mL
1.5885 mL
3.1769 mL
50 mM
0.0635 mL
0.3177 mL
0.6354 mL
Description
CPI-455 HCl is a specific 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.
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.
