bd 2

PBRM1-BD2-IN-7, a selective and cell-active inhibitor targeting the polybromo-1 (PBRM1) bromodomain, demonstrates inhibitory efficacy against PBRM1-BD2 with an IC50 value of 0.29 μM. This compound is utilized in cancer research.

PBRM1-BD2-IN-2, a selective and cell-active inhibitor of the polybromo-1 (PBRM1) bromodomain, exhibits binding affinity and inhibitory activity specifically targeting the PBRM1-BD2 domain, with Kd and IC50 values of 9.3 μM and 1.0 μM, respectively. This compound is utilized in cancer research.

PBRM1-BD2-IN-8 (compound 34) is a potent PBRM1 Bromodomain inhibitor with PBRM1-BD2 Kd of 4.4 μM, PBRM1-BD2 IC50 of 0.16 μM, and PBRM1-BD5 Kd of 25 μM; PBRM1-BD2-IN-8 shows anti-cancer activity.

PBRM1-BD2-IN-3 (compound 12) is a potent PBRM1-BD2 inhibitor with an IC50 of 1.1 μM, used in anticancer research.

PBRM1-BD2-IN-5 is a potent inhibitor of the PBRM1 Bromodomain, with dissociation constant (Kd) values of 1.5 μM and 3.9 μM for PBRM1-BD2 and PBRM1-BD5 respectively, and an inhibitory concentration 50 (IC50) value of 0.26 μM for PBRM1-BD2. This compound effectively diminishes the interaction between full-length PBRM1 and acetylated histone peptide within the PBAF complex in cell lysates, making it a promising candidate for anticancer research.

Pan-BET/BD2-IN-1 (compound 6b) is a selective BET protein inhibitor with BRDT-1Ki of 1.05 μM and BRD4-1Ki of 0.68 μM. It effectively inhibits the growth of MM.1S cancer cells with an IC50 value of 2.6 μM.

PBRM1-BD2-IN-1 is a selective and cell-active inhibitor of the polybromo-1 (PBRM1) bromodomain, exhibiting a binding affinity (Kd) of 0.7 μM and an inhibitory efficacy (IC50) of 0.2 μM, and is used in cancer research.

PBRM1-BD2-IN-6, a potent inhibitor of the PBRM1 bromodomain, exhibits an IC50 value of 0.22 µM and demonstrates antiproliferative activity. It holds potential for research in PBRM1-dependent cancer treatment.

BET BD2-IN-1 (compound 45) is a potent and selective BET BD2 inhibitor with an IC50 value of 1.6 nM. It suppresses Th17 cell differentiation by reducing the activation of STAT3 and NF-κB, making it relevant for psoriasis and inflammatory bowel disease (IBD) research [1].

BY27, a potent and selective BET BD2 inhibitor (Ki: 3.1 nM) with anticancer activity, inhibits BD1/BD2 of BRD2, BRD3, BRD4, and BRDT, and suppresses tumor growth.

GS-626510 is an orally bioavailable inhibitor of BET family bromodomains (Kd: 0.59-3.2 nM for BRD2/3/4; IC50: 83 nM and 78 nM for BD1 and BD2).

ZL0454 is an effective and selective Bromodomain-containing protein 4 inhibitors (IC50: 49 and 32 nM for BD1 and BD2).

Apabetalone (RVX000222) , an effective BET bromodomain inhibitor, has been investigated for the treatment of diabetes, atherosclerosis, and coronary artery disease.

CDD-1132 showed high affinity in BD2 DEC-Tec assay with an IC50 value of 13 nM.

CDD-1498 showed weak affinity for BRDT-BD1 with IC50 values >10 μM.

CDD-1154 had an IC50 value of 139 nM in the BD2 DEC-Tec assay.

CDD-1128 in BD2 DEC-Tec assay with an affinity value of 521 nM.

CDD-1349 had an IC50 value of 22 nM in a BD2 DEC-Tec assay.

CDD-1147 had an IC50 value of 94 nM in a BD2 DEC-Tec assay.

GSK046 (iBET-BD2) is a potent, selective, and orally active BD2 bromodomain inhibitor of the BET proteins, with IC50 values of 264 nM [BRD2 BD2], 98 nM [BRD3 BD2], 49 nM [BRD4 BD2], and 214 nM [BRDT BD2], respectively. It exhibits immunomodulatory activity.

CF53 is a highly potent, selective, and orally active inhibitor of BET protein, with a Ki of <1 nM, Kd of 2.2 nM, and an IC50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, being very selective over non-BET bromodomain-containing proteins. CF53 exhibits potent anti-tumor activity both in vitro and in vivo.

ZEN-3411 is an orally available and potent BET inhibitor that inhibits BRD4(BD1), BRD4(BD2), and BRD4(BD1BD2) and suppresses the growth of tumor cells overproducing BET proteins.

ZEN-3219 is a BET inhibitor, which has inhibitory effect on BRD4(BD1), BRD4(BD2) and BRD4(BD1BD2). ZEN-3219 has inhibitory effect on BRD4(BD1), The IC50 values of BRD4(BD2) and BRD4(BD1BD2) were 0.48, 0.16 and 0.47 μM, respectively. ZEN-3219 is a component of PROTAC molecule and can induce BRD4 degradation.

MS417 (GTPL7512) is an inhibitor of BET-specific BRD4(BRD4-BD1 and BRD4-BD2 with IC50s of 30, 46 nM and Kds of 36.1, 25.4 nM, respectively), with weak selectivity at CBP BRD with IC50 of 32.7 μM.