Mirin is a potent Mre11-Rad50-Nbs1 (MRN) complex inhibitor, and inhibits Mre11-associated exonuclease activity.
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产品名称 | ATM ↓ ↑ | ATR ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Wortmannin |
++
ATM, IC50: 150 nM |
PI3K,DNA-PK,MLCK | 99%+ | ||||||||||||||||
CP-466722 |
+
ATM, IC50: 410 nM |
99%+ | |||||||||||||||||
Torin 2 |
++
ATM, EC50: 28 nM |
++
ATR, EC50: 35 nM |
mTOR,DNA-PK | 99%+ | |||||||||||||||
KU-55933 |
+++
ATM, IC50: 12.9 nM |
96% | |||||||||||||||||
ETP-46464 |
+
ATM, IC50: 545 nM |
+++
ATR, IC50: 14 nM |
mTOR,DNA-PK | 98% | |||||||||||||||
CGK733 |
++
ATM, IC50: 200 nM |
++
ATR, IC50: 200 nM |
99%+ | ||||||||||||||||
AZD0156 | ✔ | 99%+ | |||||||||||||||||
Dactolisib |
+++
ATR, IC50: 21 nM |
98+% | |||||||||||||||||
Ceralasertib |
++++
ATR, IC50: 1 nM |
99%+ | |||||||||||||||||
Berzosertib |
+++
ATR, IC50: 19 nM |
99%+ | |||||||||||||||||
VE-821 |
+++
ATR, Ki: 13 nM |
99%+ | |||||||||||||||||
AZ20 |
++++
ATR, IC50: 5 nM |
mTOR | 99%+ | ||||||||||||||||
Schizandrin B |
+
ATR, IC50: 7.25 μM |
P-gp | 98% | ||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | (Z)-Mirin functions as an inhibitor targeting the MRN complex, comprising Mre11, Rad50, and Nbs1, thereby obstructing the MRN-mediated initiation of ATM activation without influencing the kinase activity of ATM itself. It effectively suppresses the exonuclease activity associated with Mre11. The compound enhances apoptosis, induces a G2/M cell cycle arrest, and significantly diminishes the efficiency of homology-directed repair (HDR)[1].[2]. |
体外研究 | At varying concentrations (50, 100, 500 μM), (Z)-Mirin curtails the ATM-dependent phosphorylation of Nbs1 and Chk2, along with the MRN-induced autophosphorylation of ATM at Ser1981 following DNA double-strand breaks (DSBs). A concentration of 100 μM of (Z)-Mirin is noted for its capacity to inhibit the nuclease functionality of Mre11[1]. Exposure to (Z)-Mirin ranging from 10 to 100 μM for 24 hours demonstrates a median cytotoxicity threshold at 50 μM in HEK293 cells[1]. Concentrations of 50 μM and 100 μM of (Z)-Mirin are reported to induce significant G2 phase arrest[1]. Furthermore, application of (Z)-Mirin at 18 µM for a duration of 48 hours leads to an upsurge in apoptotic activity within PEO4 cells[2]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
4.54mL 0.91mL 0.45mL |
22.70mL 4.54mL 2.27mL |
45.40mL 9.08mL 4.54mL |
CAS号 | 1198097-97-0 |
分子式 | C10H8N2O2S |
分子量 | 220.248 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,Room temperature |
溶解度 |
DMSO: 30 mg/mL(136.21 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |