ML162 is a covalent glutathione peroxidase 4 (GPX4) inhibitor. ML162 has a selective lethal effect on mutant RAS oncogene-expressing cell lines

Product information

CAS Number: 1035072-16-2

Molecular Weight: 477.40

Formula: C23H22Cl2N2O3S

Chemical Name: 2-[2-chloro-N-(3-chloro-4-methoxyphenyl)acetamido]-N-(2-phenylethyl)-2-(thiophen-2-yl)acetamide

Smiles: COC1=CC=C(C=C1Cl)N(C(C1=CC=CS1)C(=O)NCCC1C=CC=CC=1)C(=O)CCl

InChiKey: UNVKYJSNMVDZJE-UHFFFAOYSA-N

InChi: InChI=1S/C23H22Cl2N2O3S/c1-30-19-10-9-17(14-18(19)25)27(21(28)15-24)22(20-8-5-13-31-20)23(29)26-12-11-16-6-3-2-4-7-16/h2-10,13-14,22H,11-12,15H2,1H3,(H,26,29)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 100 mg/mL (209.47 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

ML162 (compound 1a) shows nanomolar potencies against two HRASG12V 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.

Products are for research use only. Not for human use.