ML-210 is a selective 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 [1] [2]. ML-210 exhibits cell-killing activity across a panel of 821 cancer cell lines (WM88, LOX-IMVI, CJM, U257, CAKI2, A498, HT1080, MC38, PANC02).

2023年6月5日 · The glutathione peroxidase 4 (GPX4) is an antioxidative enzyme and a major regulator of ferroptosis. Targeting GPX4 has become a promising strategy for cancer therapy. Here in this article, we designed and synthesized a series of …

ML210, a molecule with a nitro isoxazole structure, is widely used for inducing ferroptosis [27]. Researchers have explored the antitumor molecular mechanism of ML210 to inhibit GPX4 and reported...

2023年4月10日 · ML210 is a selective covalent inhibitor of GPX4 by targeting structurally distinct masked nitrile oxides suited for engaging the GPX4 active-site selenocysteine [88]. Genome-wide identification of the mechanism of action of small-molecule compounds also revealed that the Food and Drug Administration (FDA)-approved anticancer agent altretamine ...

2019年4月8日 · Cells were exposed to ML210 treatment for 4, 6, or 8 days before being cultured in drug-free media for recovery and expansion for 24 h.

2023年6月5日 · Based on our previous experiences of RSL3-based GPX4 degraders, we focused our research of ML210-based degraders on the design and optimization of linkers with semi-rigid rings. We found for the first time that ML210 and its related degraders have obvious degradation activity of GPX4 protein.

ML 210 has been used as a glutathione peroxidase 4 (GPX4) inhibitor to induce ferroptosis in cancer cells. [1] [2] It has also been used as a GPX4 inhibitor to examine whether pharmacological inhibition of GPX4 altered prominin2 expression and impacted ferroptosis in adherent MCF10A and Hs578t cells. [3]

2025年1月6日 · ML210, a GPX4 inhibitor, is expected to induce ferroptosis. In this study, low concentrations of ML210 promoted lipid peroxidation and suppressed EMT in pancreatic cancer cells; however, ML210 did not cause cell death at doses up to 10 μM (Figure 4A). In conclusion, ML210 inhibits migration without causing ferroptosis in pancreatic cancer cells.