Home Cell Cycle Chk inhibitor - Apoptosis related inhibitor BML-277 (Chk2 Inhibitor II) For research use only.

BML-277 (Chk2 Inhibitor II)

BML-277 (Chk2 Inhibitor II) is an ATP-competitive inhibitor of Chk2 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 apoptosis due to ionizing radiation.

BML-277 (Chk2 Inhibitor II) Chemical Structure

BML-277 (Chk2 Inhibitor II) Chemical Structure

CAS: 516480-79-8

Selleck's BML-277 (Chk2 Inhibitor II) has been cited by 13 publications

Purity & Quality Control

Batch: S863201 DMSO] 72 mg/mL] false] Ethanol] 21 mg/mL] false] Water] Insoluble] false Purity: 99.17%
99.17

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Biological Activity

Description BML-277 (Chk2 Inhibitor II) is an ATP-competitive inhibitor of Chk2 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 apoptosis due to ionizing radiation.
Targets
Chk2 [1]
(Cell-free assay)
15 nM
In vitro
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[2].
Cell Research Cell lines human DLBCLs cells
Concentrations 5 μM
Incubation Time 48 h
Method

Single-cell suspensions are obtained from lymph node biopsies of patients diagnosed with DLBCL and are treated with DMSO, ERK inhibitor and CHK2 inhibitor II alone or in combination for 48 h after which the percentage of apoptotic cells is determined by Annexin V analysis.
In Vivo
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[2].
Animal Research Animal Models SUDHL6 DLBCL xenografts (SCID mice)
Dosages 1 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 363.80 Formula

C20H14ClN3O2
CAS No. 516480-79-8 SDF Download BML-277 (Chk2 Inhibitor II) SDF
Smiles C1=CC(=CC=C1C2=NC3=C(N2)C=C(C=C3)C(=O)N)OC4=CC=C(C=C4)Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 72 mg/mL ( (197.91 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 21 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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