Mirin

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Mirin  纯度: 98.02%

Mirin 一种有效的 Mre11-Rad50-Nbs1 (MRN) 复合物抑制剂。Mirin 在不影响 ATM 蛋白激酶活性的情况下阻止 ATM (ataxia-telangiectasia mutated) 的 MRN 依赖性激活 (IC50=12 μM)，并抑制 Mre11 相关的核酸外切酶活性。Mirin 可消除哺乳动物细胞中的 G2/M 检查点和同源性依赖性修复。Mirin 在哺乳动物细胞中阻止 ATM 因 DNA 双链断裂 (DSBs) 而激活并阻断同源性定向修复 (HDR)。

Mirin

Mirin Chemical Structure

CAS No. : 299953-00-7

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生物活性

Mirin is a potent Mre11-Rad50-Nbs1 (MRN) complex inhibitor. Mirin prevents MRN-dependent activation of ATM (IC50=12 μM) without affecting ATM protein kinase activity, and it inhibits Mre11-associated exonuclease activity. Mirin abolishes the G2/M checkpoint and homology-dependent repair in mammalian cells. Mirin prevents ATM activation in response to DNA double-strand breaks (DSBs) and blocks homology-directed repair (HDR) in mammalian cells[1].

体外研究
(In Vitro)

Mirin inhibits H2AX phosphorylation with an IC50 of 66 μM. Mirin also inhibits the ATM-dependent phosphorylation of the downstream targets Nbs1 and Chk2 and the MRN-dependent autophosphorylation of ATM at Ser1981 in response to DSBs. Mirin induces a substantial G2 arrest at concentrations of 50 μM and 100 μM. Mirin (10-100 μM) inhibits homology-dependent DNA repair in TOSA4 cells[1].
BRCA2-deficient cells also showed hypersensitivity to the Mre11 inhibitor Mirin[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

220.25

Formula

C10H8N2O2S
CAS 号

299953-00-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶解性数据
In Vitro: 

DMSO : 83.33 mg/mL (378.34 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.5403 mL 22.7015 mL 45.4030 mL
5 mM 0.9081 mL 4.5403 mL 9.0806 mL
10 mM 0.4540 mL 2.2701 mL 4.5403 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Dupré A, et al. A forward chemical genetic screen reveals an inhibitor of the Mre11-Rad50-Nbs1 complex. Nat Chem Biol. 2008;4(2):119-125.

    [2]. Ying S, et al. Mre11-dependent degradation of stalled DNA replication forks is prevented by BRCA2 and PARP1. Cancer Res. 2012;72(11):2814-2821.

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