Mirin

Mirin用途

米林是一种有效的Mre11-Rad50-Nbs1(MRN)复合抑制剂。Mirin在不影响ATM蛋白激酶活性的情况下阻止ATM的MRN依赖性激活(IC50=12μM),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可阻止哺乳动物细胞中因DNA双链断裂(DSB)而激活ATM,并阻断同源性定向修复(HDR)[1]。

Mirin名称

[ CAS 号 ]:
299953-00-7

[ 中文名 ]:
5-(4-羟基苯亚甲基)-2-亚氨基噻唑啉-4-酮

[ 英文名 ]:
Mirin

[英文别名 ]:

Mirin
MRN-ATM Pathway Inhibitor,Mirin
Lu AA 47070

Mirin生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 细胞周期/DNA损伤 >> ATM/ATR

信号通路 >> PI3K/Akt/mTOR 信号通路 >> ATM/ATR

[体外研究]

Mirin以66μM的IC50抑制H2AX磷酸化。Mirin还抑制下游靶点Nbs1和Chk2的ATM依赖性磷酸化,以及Ser1981对DSB的反应中ATM的MRN依赖性自磷酸化。Mirin在浓度为50μM和100μM时诱导G2期大量阻滞。Mirin(10-100μM)抑制TOSA4细胞中的同源依赖性DNA修复[1]。BRCA2缺陷细胞也对Mre11抑制剂Mirin表现出超敏反应[2]。

[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.

Mirin物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 沸点 ]:
441.6±55.0 °C at 760 mmHg

[ 分子式 ]:
C₁₀H₈N₂O₂S

[ 分子量 ]:
220.248

[ 闪点 ]:
220.8±31.5 °C

[ 精确质量 ]:
220.030655

[ PSA ]:
98.48000

[ LogP ]:
1.36

[ 外观性状 ]:
固体

[ 蒸汽压 ]:
0.0±1.1 mmHg at 25°C

[ 折射率 ]:
1.718

[ 储存条件 ]:
2-8°C

MirinMSDS

Mirin安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

[ 海关编码 ]:
2934999090

Mirin合成路线

Mirin上下游产品

Mirin上游产品

Mirin下游产品

Mirin海关

[ 海关编码 ]: 2934999090

[ 中文概述 ]:
2934999090. 其他杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Mirin文献

Productive replication of human papillomavirus 31 requires DNA repair factor Nbs1.

J. Virol. 88(15) , 8528-44, (2014)

Activation of the ATM (ataxia telangiectasia-mutated kinase)-dependent DNA damage response (DDR) is necessary for productive replication of human papillomavirus 31 (HPV31). We previously found that DN...

DNA double-strand break repair pathway choice is directed by distinct MRE11 nuclease activities.

Mol. Cell. 53(1) , 7-18, (2014)

MRE11 within the MRE11-RAD50-NBS1 (MRN) complex acts in DNA double-strand break repair (DSBR), detection, and signaling; yet, how its endo- and exonuclease activities regulate DSBR by nonhomologous en...

A central role of TRAX in the ATM-mediated DNA repair.

Oncogene 35 , 1657-70, (2016)

DNA repair is critical for the maintenance of genome stability. Upon genotoxic stress, dysregulated DNA repair may induce apoptosis. Translin-associated factor X (TRAX), which was initially identified...

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