ML162 is a covalent glutathione peroxidase 4 (GPX4) inhibitor. ML162 has a selective lethal effect on mutant RAS oncogene-expressing cell lines
体外研究
ML162 (compound 1a) shows nanomolar potencies against two HRAS expressing cell lines, with IC50 values of 25 nM and 578 nM for HRASG12V-expressing and wild-type BJ fibroblasts, respectively.
ML162 (8 μM; 24 hours) treatment increases the expression of p62 and Nrf2 in chemoresistant HN3R and HN3-rslR cells, inactivates Keap1, and increases expression of the phospho-PERK-ATF4-SESN2 pathway.
ML162 induces the head and neck cancer (HNC) cell death to varying degrees, with parental HN3 cells more sensitive and cisplatin-resistant (HN3R) and acquired RSL3-resistant (HN3-rslR) cells less sensitive.
Western Blot Analysis
Cell Line:
HN3R cells
Concentration:
8 μM
Incubation Time:
24 hours
Result:
Increased the expression of p62 and Nrf2 in chemoresistant HN3R and HN3-rslR cells.
分子式
C23H22Cl2N2O3S
分子量
477.40
CAS号
1035072-16-2
运输条件
Room temperature in continental US; may vary elsewhere.