[CAS NO. 516480-79-8] Chk2 Inhibitor II (BML-277)

Name: Chk2 Inhibitor II (BML-277)
Brand: Arctom Scientific
SKU: SLK-S8632

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PRODUCTS SPECIFICATIONS [516480-79-8]

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Catalog

SLK-S8632

Brand

Selleck

CAS

516480-79-8

DESCRIPTION [516480-79-8]

Overview

MDL	MFCD08276917
Molecular Weight	363.80
Molecular Formula	C20H14ClN3O2
SMILES	O=C(C1=CC=C2C(NC(C3=CC=C(OC4=CC=C(Cl)C=C4)C=C3)=N2)=C1)N

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

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.7488 mL	13.7438 mL	27.4876 mL
5 mM	0.5498 mL	2.7488 mL	5.4975 mL
10 mM	0.2749 mL	1.3744 mL	2.7488 mL
50 mM	0.0550 mL	0.2749 mL	0.5498 mL

Description

Chk2 Inhibitor II (BML-277) is an ATP-competitive inhibitor of with IC50 of 15 nM. It is 1000-fold more selective toward Chk2 serine/threonine kinase than for Chk1 and Cdk1/B kinases. Chk2 Inhibitor II (BML-277) dose dependently protects human CD4(+) and CD8(+) T-cells from due to ionizing radiation.

Targets

Chk2 ^[1]
(Cell-free assay)

15 nM

In vitro

The CHK2 Inhibitor II shows 1,000-fold greater selectivity for the CHK2 serine/threonine kinase than for the Cdk1/B and CK1 kinases and was first discovered to be a potent, selective small molecule showing radioprotection towards human T cells. Different doses of CHK2 inhibitor II specifically inhibit CHK2 phosphorylation at Thr68 at different time course, but not CHK1 phosphorylation. Treatment with combination of CHK2 inhibitor II and ERK inhibitor results in substantially more apoptosis compared with treatment of either drug alone.

In vivo

SUDHL6 DLBCL xenografts mice treated every other day intraperitoneally with either vehicle, ERK inhibitor (5 mg kg−1), CHK2 inhibitor II (1 mg kg−1), or both ERK inhibitor and CHK2 inhibitor II for 20 days show no lethal toxicity, significant weight loss or any gross abnormalities. Both 5 mg/kg ERK inhibitor and 1 mg/kg CHK2 inhibitor II modestly inhibit tumour growth but combined treatment with ERK inhibitor and CHK2 inhibitor II results in a statistically significant suppression of tumour growth.

References

[1] Arienti KL, et al. J Med Chem. 2005, 48(6):1873-85.
[2] Dai B, et al. Nat Commun. 2011, 2:402.