BMI-1

PTC-209 is a potent and selective BMI-1 inhibitor.

PRT4165 (NSC600157) is a potent PRC1-mediated H2A ubiquitylation inhibitor.

Unesbulin (PTC596) is an orally active, selective inhibitor of B-cell-specific Moloney murine leukemia virus integration site 1 (BMI-1).

PTC-028 selectively suppresses cancer cells whereas normal cells remain unaffected. PTC-028 is an orally bioavailable inhibitor of stem cell factor BMI-1 in ovarian cancer. The depletion of BMI-1 by PTC-028 causes caspase-mediated apoptosis.

XMD8-92 is an effective and specific BMK1 ERK5 inhibitor (Kd: 80 nM).

PTC-209 hydrobromide (PTC-209 HBr) is the hydrobromide salt of PTC-209, which is a potent and selective BMI-1 inhibitor with IC50 of 0.5 μM, and results in irreversible reduction of cancer-initiating cells (CICs).

APD-94 is a dual inhibitor targeting tubulin and Bmi-1. It disrupts the normal polymerization of tubulin and suppresses the expression of Bmi-1. This compound induces cell cycle arrest at the G2/M phase and triggers apoptosis, thereby inhibiting cancer cell proliferation. Additionally, APD-94 inhibits the growth of HT29 cell xenograft tumors in NOD/SCID mice and is applicable to colorectal cancer research.

1,6,7-Trihydroxyxanthone has anti-cancer activity ,at least in part, through the activation of miR-218 and suppression of Bmi-1 expression; can suppress cell growth and induce apoptosis in liver cancer cells.

QW24 down-regulates BMI-1, exhibits potent antitumour effects and is used as an effective therapeutic agent in the treatment of clinical colorectal cancer.

SH498 is a novel Bmi-1-mediated anti-tumor agent with significant anti-proliferative effects.