BMI-1

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 is a potent and selective BMI-1 inhibitor.

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

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).

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.

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.

BMI-1026 is a cyclin-dependent kinase 1 (Cdk1) inhibitor with an IC50 of 2.3 nM. It induces cell apoptosis by blocking the G2-M phase transition.

BMI-135, a selective estrogen mimic, demonstrates agonist activity for the estrogen receptor and induces a rapid endoplasmic reticulum stress response (UPR) alongside apoptosis in breast cancer cells.

EBMI-13B is a potent and selective isozymes CA-VA and CA-VII activator.

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.

RB-3, a PRC1 inhibitor, binds to RING1B-BMI1f with a Kd of 2.8 μM.

BMIM-TFSI (compound8) is an HIV-1 integrase inhibitor that effectively suppresses both the 3'-processing (3'-P) and strand transfer (ST) steps of the integration process. It is applicable in HIV-1 research.