[CAS NO. 2095432-28-1]  CPI-455 HCl

Ships within Stock Price Qty Total
$0.00
$0.00
Please click "REQUEST A QUOTE" button if you need other sizes or custom synthesis
request a quote
If there is no stock, or you need other sizes or custom synthesis, please:

PRODUCTS SPECIFICATIONS [2095432-28-1]

Catalog
SLK-S8287
Brand
Selleck
CAS
2095432-28-1

DESCRIPTION [2095432-28-1]

Overview

MDL-
Molecular Weight314.77
Molecular FormulaC16H15ClN4O
SMILESN#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 mg5 mg10 mg
1 mM3.1769 mL15.8846 mL31.7692 mL
5 mM0.6354 mL3.1769 mL6.3538 mL
10 mM0.3177 mL1.5885 mL3.1769 mL
50 mM0.0635 mL0.3177 mL0.6354 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.

Targets

KDM5A [1]
(Cell-free assay)
10 nM

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.