BD2 Inhibitor

GS-626510 is a potent, and orally active BET family bromodomains inhibitor, with K_d values of 0.59-3.2 nM for BRD2/3/4, with IC₅₀ values of 83 nM and 78 nM foe BD1 and BD2, respectively.

BRD4-BD1/2-IN-3 (Compound B6) is a selective BRD4 BD2 inhibitor with an IC₅₀ of 0.41  nM for BRD4 BD2 over BRD4 BD1. BRD4-BD1/2-IN-3 significantly inhibits the LPS (HY-D1056)-induced expression of IL-6. BRD4-BD1/2-IN-3 shows anti-inflammatory activities by modulating the TNF and NF-κB signaling pathway. BRD4-BD1/2-IN-3 can be used for inflammatory diseases research.

GSK040 is a potent and highly selective BET BD2 inhibitor, with a pIC₅₀ of 8.3. GSK040 shows more than 5000-fold selectivity for BET BD2 over BET BD1 (pIC₅₀=4.6). GSK040 can be used for the research of oncology and immunology diseases.

BRD4 Inhibitor-31 (Example 136) is a BRD4 inhibitor (K_is: 0.234 μM and 0.295 μM for BRD4 BD1 and BRD4 BD2 respectively). BRD4 Inhibitor-31 can be used for research of inflammatory diseases, cancer, and AIDS.

BET-IN-26 (compound 13a) is a potent, selective and orally active BD1 inhibitor with IC₅₀ values of 0.0055, 9.0 µM for BD1, BD2, respectively. BET-IN-26 decreases LPS (HY-D1056) induced serum levels of IL-6 and MCP-1.

SRX3212 is a potent PI3Kα/BRD4 inhibitor with human IC₅₀ values of 22 nM, 3.7 nM, and 32 nM for PI3Kα, BRD4_BD1, and BRD4_BD2, respectively. SRX3212 inhibits PI3K kinase activity and blocks acetyllysine binding function of BRD4_BD1 and BRD4_BD2. SRX3212 can be used for the research of mantle cell lymphoma, colon carcinoma, neuroblastoma, prostate cancer^[1].

CDK4/6/BRD4-IN-1 (B15) is an inhibitor of CDK4, CDK6 and BRD4, with IC₅₀ values of 220 nM, 146 nM, 106 nM and 85 nM for BRD4-BD2, BRD4-BD1, CDK6 and CDK4, respectively. CDK4/6/BRD4-IN-1 (B15) can be used in the study of NSCLC (Non-Small Cell Lung Cancer). CDK4/6/BRD4-IN-1 (B15) induces cell cycle arrest and apoptosis.

PBRM1-BD2-IN-4 is a PBRM1-BD2 inhibitor with an IC₅₀ of 0.2 μM, and its K_d values for PBRM1-BD2 and PBRM1-BD5 are 5.5 μM and 11.1 μM, respectively. PBRM1-BD2-IN-4 selectively inhibits the proliferation of PBRM1-dependent prostate cancer cells. PBRM1-BD2-IN-4 can be used in studies related to prostate cancer.

BRD4 Inhibitor-27 (compound 6) is a BRD4 inhibitor with IC₅₀ of 9.6 and 11.3 μM for BRD4 BD1 and BRD4 BD2, respectively. BRD4 Inhibitor-27 has the potential to study cancer.