brdt-bd2

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.

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.

ABBV-744 is a BDII-selective BET bromodomain inhibitor that inhibits BRD2 3 4. It is used in the research on inflammatory diseases, cancer, and AIDS.

RVX-297 is a BD2 selective inhibitor of BET bromodomains. RVX-297 preferentially binds to the BD2 domains of the BET bromodomain and Extra Terminal (BET) family of protein.

INCB054329, a structurally distinct bromodomain and extraterminal domain (BET) inhibitor, inhibits BRD2-BD1, BRD2-BD2, BRD3-BD1, BRD3-BD2, BRD4-BD1, BRD4-BD2, BRDT-BD1 and BRDT-BD2 with IC50 values of 44 nM, 5 nM, 9 nM, 1 nM, 28 nM, 3 nM, 119 nM and 63 nM respectively.

N-[5-[[[3-(6-Amino-4-methylpyridin-3-yl)-1-methyl-1H-indazol-5-yl]carbonyl]amino]-2-methylphenyl]-N′-methylterephthalamide had an IC50 value of 22 nM in a BD2 DEC-Tec assay.

BRD4 Inhibitor-28 (Compound 18), an orally active molecule, selectively inhibits the bromodomains of BRD4 (BRD4-BD1 and BRD4-BD2) with IC50 values of 15 and 55 nM, respectively. It also demonstrates inhibition of BRD2-BD1, BRD3-BD1, and BRDT-BD1 with IC50 values of 19, 25, and 68 nM, respectively. Furthermore, this compound exhibits anti-melanoma activity [1].

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.

GSK973 is a highly selective and orally bioavailable inhibitor that targets the second bromodomains (BD2s) of the BET family. It exhibits a pIC 50 of 7.8 and a pK d of 8.7 specifically for BRD4 BD2. Additionally, GSK973 demonstrates a remarkable selectivity of 1600-fold for BRD4 BD2 over BRD4 BD1. Moreover, it displays good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2, with pIC 50 ranging from 7.4 to 7.8 and pK d ranging from 8.3 to 8.5.

N1-[5-[[[3-(4-Amino-2-methylphenyl)-1-methyl-1H-indazol-5-yl]carbonyl]amino]-2-methylphenyl]-N4-methyl-1,4-benzenedicarboxamide is a potent, selective second bromodomain (BD2) of BRDT and BRD4 inhibitor with IC50 of 7 and 25 nM, >1,000-fold and 300-fold selectivity over BRDT-BD1 and BRD4-BD1.

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].

N1-[5-[[[3-(4-Methoxyphenyl)-1-methyl-1H-indazol-5-yl]carbonyl]amino]-2-methylphenyl]-N4-methyl-1,4-benzenedicarboxamide (ACI) in BD2 DEC-Tec assay with an affinity value of 521 nM.

N-[5-[[[3-(6-Amino-2-methylpyridin-3-yl)-1-methyl-1H-indazol-5-yl]carbonyl]amino]-2-methylphenyl]-N′-methylterephthalamide had an IC50 value of 94 nM in a BD2 DEC-Tec assay.

BET-IN-27 (compound 6C) is an orally active BET inhibitor with IC50 values of 3.3 nM (BRD4-BD2), 3.4 nM (BRD4-BD1), 4.1 nM (BRD2-BD1), 20.4 nM (BRD3-BD1), and 42.0 nM (BRDT-BD1). It also exhibits antiproliferative activity.

PLX51107 is a potent and selective BET inhibitor with Kds of 1.6, 2.1, 1.7, and 5 nM for BRD2-BD1, BRD3-BD1, BRD4-BD1, and BRDT-BD1, respectively.