ML-210 (CID-49766530)

Description: ML-210 (CID 49766530) is a novel, potent, selective RAS inhibitor, also a potent and covalent glutathione peroxidase 4 (GPX4) inhibitor with an EC50 of 30 nM. ML-210 binds the GPX4 selenocysteine residue. ML-210 has anti-cancer activity. ML-210 displayed nanomolar potency in the primary screening cell line while maintaining selectivity similar to previously identified probes. The probe is in a novel structural class in the field of RAS synthetically lethal compounds and will, therefore, be highly useful in identifying pathways that can potentially be used for selectively inhibiting cancer cells.

References:

1. John K. Eaton, et al. Targeting a Therapy-Resistant Cancer Cell State Using Masked Electrophiles as GPX4 Inhibitors. Biorxiv. 2018.

2. Weïwer M, 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.