NSC-743380

NSC-743380 (also known as oncrasin-72) is a small molecule indole-3-carbinol analog with potent preclinical anticancer activity. Originally identified through synthetic lethality screening against KRAS-mutant cell lines, its mechanism of action involves the inhibition of the JAK2/STAT3 signaling pathway and the suppression of RNA polymerase II C-terminal domain phosphorylation, which leads to the inhibition of transcription and translation. It has also been shown to rapidly activate Tyrosine kinase 2 (Tyk2), p38, and JNK, ultimately inducing caspase-dependent apoptosis. NSC-743380 has demonstrated efficacy in various xenograft models, including renal and lung cancers, and is noted for its oral bioavailability. It is particularly effective in cells expressing SULT1A1.

Other names

1-[(3-chlorophenyl)-methyl]-1H-indole-3-carbinol