Mirin 是一种有效的Mre11-Rad50-Nbs1 (MRN)复合物抑制剂。Mirin 可在不影响 ATM 蛋白激酶活性的情况下,抑制ATM 的 MRN 依赖性激活(IC50=12 μM),并抑制 Mre11 相关的核酸外切酶活性。与其靶向 MRN 复合物的能力一致,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。
产品描述
Mirin is a potent Mre11-Rad50-Nbs1 (MRN) complex inhibitor. Mirin prevents MRN-dependent activation of ATM (IC 50 =12 μM) without affecting ATM protein kinase activity, and it inhibits Mre11-associated exonuclease activity. Consistent with its ability to target the MRN complex, Mirin abolishes the G2/M checkpoint and homology-dependent repair in mammalian cells [1].
体外活性
Mirin inhibits the phosphorylation of H2AX with an IC 50 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].
Cas No.
299953-00-7
分子式
C10H8N2O2S
分子量
220.25
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years