PRLX 93936

PRLX 93936 is a small molecule structural analogue of erastin with potential antineoplastic activity. It was developed to improve upon the pharmaceutical properties of erastin and demonstrates robust and selective toxicity in a wide variety of tumor cell lines. In preclinical models, it caused complete tumor regression in mouse xenograft models of fibrosarcoma, pancreatic cancer, ovarian cancer, colon cancer, and melanoma. Mechanistically, PRLX 93936 inhibits mitochondrial outer membrane proteins voltage-dependent anion channels (VDACs) 2 and 3—leading to oxidative stress-induced non-apoptotic cell death (ferroptosis). It also acts as an inhibitor/modulator of synaptic Ras GTPase activating protein 1 (SYNGAP1), modulates ion channels including VDACs, inhibits the activated Ras pathway (including RAS-mutant cancers), and can induce caspase-dependent apoptosis as well as necrosis and cell cycle arrest. The drug was investigated for use in solid tumors and multiple myeloma but development has been discontinued[1][2][3][5][6][8].

Brand names

PRLX 93936PRLX93936PRLX-93936

Other names

Erastin analoguePRLX 82845PRLX82845PRLX-82845