产品说明书

ML162

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Chemical Structure| 1035072-16-2 同义名 : -
CAS号 : 1035072-16-2
货号 : A1210811
分子式 : C23H22Cl2N2O3S
纯度 : 99%+
分子量 : 477.403
MDL号 : MFCD03450805
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(219.94 mM)，配合低频超声助溶，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：
生物活性
描述 ML162, a covalent inhibitor of glutathione peroxidase 4 (GPX4), exhibits selective toxicity towards cell lines expressing mutant RAS oncogenes[1][2]. It demonstrates nanomolar efficacy against two cell lines harboring HRASG12V, with IC50 values of 25 nM for HRASG12V-expressing cells and 578 nM for wild-type BJ fibroblasts[1]. Treatment with ML162 (8 μM for 24 hours) elevates p62 and Nrf2 levels in chemoresistant HN3R and HN3-rslR cells, deactivates Keap1, and enhances the phospho-PERK-ATF4-SESN2 signaling pathway[2]. ML162 variably induces cell death in head and neck cancer (HNC) cells, with the original HN3 cells being more susceptible, while the cisplatin-resistant HN3R and RSL3-resistant HN3-rslR cells show reduced sensitivity[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.09mL

0.42mL

0.21mL

10.47mL

2.09mL

1.05mL

20.95mL

4.19mL

2.09mL
参考文献

[1]Michel Weïwer, et al. Development of small-molecule probes that selectively kill cells induced to express mutant RAS. Bioorg Med Chem Lett. 2012 Feb 15;22(4):1822-6.

[2]Daiha Shin, et al. Nrf2 inhibition reverses resistance to GPX4 inhibitor-induced ferroptosis in head and neck cancer. Free Radic Biol Med. 2018 Dec;129:454-462.