Chk2 Inhibitor II (BML-277)
For research use only.
CAS No. 516480-79-8
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.
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|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.|
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.|
|In vitro||DMSO||72 mg/mL (197.91 mM)|
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|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
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Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
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