PTC-209

PTC-209 is a first-in-class small molecule inhibitor of the polycomb group protein **BMI-1**, a key component of the Polycomb Repressive Complex 1 (PRC1) involved in the regulation of gene expression through chromatin remodeling. PTC-209 inhibits BMI-1 transcription, leading to downregulation of BMI-1 protein and associated histone modifications, such as H2AK119 ubiquitination, which in turn impedes PRC1-mediated gene repression[1][3][5]. This mechanism induces apoptosis and cell cycle arrest in various cancer types, including multiple myeloma, colon, breast, lung, and glioblastoma cells[1][2][3][4]. PTC-209 has shown to reduce CSC (cancer stem cell) properties, inhibit cell proliferation and migration, and enhance the efficacy of other anti-cancer agents (e.g., cisplatin, camptothecin, BET inhibitors)[1][2][6]. It has also been shown to inhibit the STAT3 signaling pathway by decreasing gp130 levels, contributing to anti-tumor activity[2]. The compound was originally developed using gene expression modulation screening technology. PTC-209 is for research use and preclinical studies only; it is not approved for clinical use.

Other names

BMI-1 Expression InhibitorBMI1 Expression InhibitorBMI 1 Expression InhibitorFLVI2/BMI1 Expression InhibitorMGC12685 Expression InhibitorMGC-12685 Expression InhibitorMGC 12685 Expression InhibitorPCGF4 Expression InhibitorPCGF-4 Expression InhibitorPCGF 4 Expression InhibitorRNF51 Expression InhibitorRNF-51 Expression InhibitorRNF 51 Expression Inhibitor