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CAS No.: 516480-79-8

BML-277/Chk2抑制剂II Catalog No. CSN16323

Synonyms: Chk2 Inhibitor II;C-3742;Checkpoint Kinase 2 Inhibitor II

BML-277 is a selective Chk2 (checkpoint kinase 2) inhibitor with IC50 of 15 nM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Chk2

IC50:15nM
描述Chk2 kinase is a key mediator of the DNA damage checkpoint. BML-277 is a Chk2 inhibitor with an IC50 value of 15nM. It rescued CD4+ and CD8+ cells from radiation-induced apoptosis in a dose-dependent manner with an EC₅₀ of 3-7.6µM^[2]. BML-277 at 1-10µM inhibited CHK2 phosphorylation at Thr68 at different time courses (30min, 1h, 2h, and 4h) in both Farage and SUDHL6 cells. Treatment of SUDHL4, SUDHL6, and Farage cells with 5μM BML-277 led to apoptosis of less than 30% cells. BML-277 at 1 and 5μM significantly diminished the physical interaction between ERK and CHK2 in Farage and SUDHL6 cells at 4h post-exposure. In SUDHL6, Farage, and OCI-LY3 cells, BML-277 at 1-10µM reduced CHK2 phosphorylation at Thr68 but increased ERK phosphorylation compared to the control cells. Intraperitoneal administration of BML-277 (1mg/kg) every other day for 20 days modestly inhibited tumor growth in mice bearing subcutaneous tumors of SUDHL6 cells compared to the vehicle-treated group. The combination treatment of BML-277 (1mg/kg) and ERK inhibitor (5mg/kg) for 20 days resulted in a significant reduction in Ki67 expression and tumor suppression in mice inoculated with SUDHL6 cells^[3].
作用机制BML-277 inhibits Chk2 in an ATP-competitive manner. The hydrogen bonding interactions are predicted to occur between the 5-amide group of the benzimidazole moiety and the backbone amide nitrogen and carbonyl group of MET 90^[2].
参考文献

[1] Arienti KL, Brunmark A, et al. Checkpoint kinase inhibitors: SAR and radioprotective properties of a series of 2-arylbenzimidazoles. J Med Chem. 2005 Mar 24;48(6):1873-85.
[2] Arienti KL, Brunmark A, Axe FU, et al. Checkpoint kinase inhibitors: SAR and radioprotective properties of a series of 2-arylbenzimidazoles. J Med Chem. 2005;48(6):1873-1885. doi:10.1021/jm0495935
[3] Dai B, Zhao XF, Mazan-Mamczarz K, et al. Functional and molecular interactions between ERK and CHK2 in diffuse large B-cell lymphoma. Nat Commun. 2011;2:402. Published 2011 Jul 19. doi:10.1038/ncomms1404

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.7488 mL
- 13.7439 mL
- 27.4878 mL
- 5 mM
- 0.5498 mL
- 2.7488 mL
- 5.4976 mL
- 10 mM
- 0.2749 mL
- 1.3744 mL
- 2.7488 mL

技术信息

CAS号

516480-79-8

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H14ClN3O2

运输

蓝冰

分子量

363.80

别名

Chk2 Inhibitor II;C-3742;Checkpoint Kinase 2 Inhibitor II

溶解度

DMSO	70.0 mg/mL (192.4 mM)
Water	Insoluble
Ethanol	20.0 mg/mL (55.0 mM)

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