Chk2 Inhibitor II (BML-277)

Catalog No.S8632

For research use only.

Chk2 Inhibitor II (BML-277) 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.

Chk2 Inhibitor II (BML-277) Chemical Structure

CAS No. 516480-79-8

Selleck's Chk2 Inhibitor II (BML-277) has been cited by 6 Publications

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Biological Activity

Description Chk2 Inhibitor II (BML-277) 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

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].

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].

Protocol (from reference)

Cell Research:

[2]

  • 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.

Animal Research:

[2]

  • Animal Models: SUDHL6 DLBCL xenografts (SCID mice)
  • Dosages: 1 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

DMSO 72 mg/mL
(197.91 mM)
Ethanol 21 mg/mL
(57.72 mM)
Water Insoluble

Chemical Information

Molecular Weight 363.80
Formula

C20H14ClN3O2

CAS No. 516480-79-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC(=CC=C1C2=NC3=C(N2)C=C(C=C3)C(=O)N)OC4=CC=C(C=C4)Cl

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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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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