Home Cell Cycle Chk inhibitor - Apoptosis related inhibitor BML-277 (Chk2 Inhibitor II)

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BML-277 (Chk2 Inhibitor II) Chk inhibitor

Cat.No.S8632

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

Chemical Structure

Molecular Weight: 363.80

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Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 363.80 Formula

C20H14ClN3O2

 Storage (From the date of receipt)
CAS No. 516480-79-8 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1=CC(=CC=C1C2=NC3=C(N2)C=C(C=C3)C(=O)N)OC4=CC=C(C=C4)Cl

Solubility

In vitro
Batch:

DMSO : 72 mg/mL (197.91 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 21 mg/mL

Water : Insoluble

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Mass Concentration Volume Molecular Weight

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

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Mechanism of Action

Targets/IC50/Ki
Chk2 [1]
(Cell-free assay)
15 nM
In vitro
BML-277 (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 this compound specifically inhibit CHK2 phosphorylation at Thr68 at different time course, but not CHK1 phosphorylation. Treatment with combination of it 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), BML-277 (Chk2 Inhibitor II) (1 mg kg−1), or both ERK inhibitor and this compound for 20 days show no lethal toxicity, significant weight loss or any gross abnormalities. Both 5 mg/kg ERK inhibitor and 1 mg/kg of it modestly inhibit tumour growth but combined treatment with ERK inhibitor and BML-277 results in a statistically significant suppression of tumour growth[2].
References

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