tcsc3024 PTC-209 (hydrobromide)

PTC-209 hydrobromide is a specific BMI-1 inhibitor with IC₅₀ of 0.5 μM in both GEMS reporter and ELISA assays.

IC50 & Target: IC50: 0.5 μM (BMI-1, in HT1080 tumor cells)^[1]

In Vitro: PTC-209 is a recently developed inhibitor of BMI1, in biliary tract cancer (BTC) cells. PTC-209 reduces overall viability in BTC cell lines in a dose-dependent fashion (0.04-20 μM). Treatment with PTC-209 leads to slightly enhanced caspase activity and stop of cell proliferation. Cell cycle analysis reveals that PTC-209 causes cell cycle arrest at the G1/S checkpoint^[2]. PTC-209(100, 200, or 500nM) decreases BMI1 and increases p16 protein expression in canine OSA cell lines. Compare to vehicle control, BMI1 protein expression decreases by 40% and 25% in the Abrams and D17 cell lines, respectively, following 500 nM PTC-209 treatment. In the Moresco cell line, BMI1 protein expression decreases by 16% and 39% following 200nM and 500nM PTC-209 treatment, respectively, as compared to vehicle control. Increases in p16 protein levels could be observed in all cell lines beginning at 100nM PTC-209 and are highest at the 500nM PTC-209 dose for Abrams (120% increase) and Moresco (200% increase), but appeared to top out at 200 nM for the D17 cell line (54% increase)^[3].

In Vivo: Pharmacokinetic analysis demonstrates that PTC-209 (60 mg/kg, subcutaneously once a day) effectively inhibits BMI-1 production in tumor tissue in vivo. Inhibition of BMI-1 with PTC-209 halts growth of preestablished tumors in vivo^[1].