PTC-209 --- BMI-1 Inhibitor

Bioss

PTC-209 --- BMI-1 Inhibitor [315704-66-6]

16

Research Use Only

98.0

PTC-209 is a novel potent and selective BMI-1 inhibitor, targeting the BMI-1 self-renewal machinery with an IC50 of ~0.5 microM. Tumor formation and, more specifically, human colorectal cancer-initiating cells (CIC) are dependent on the canonical self-renewal regulator BMI-1. Down-regulation of BMI-1 inhibits the ability of colorectal CICs to self-renew, resulting in the abrogation of their tumorigenic potential. Treatment of primary colorectal cancer xenografts with the small-molecule BMI-1 inhibitor PTC-209 resulted in colorectal CIC loss with long-term and irreversible impairment of tumor growth. Targeting the BMI-1 self-renewal machinery represents a promising approach to the elimination of many cancer stem (and initiating) cells.

-20°C

51202000