brd41

PNZ5, an isoxazole-based pan-BET inhibitor, demonstrates potent activity and high selectivity comparable to the established (+)-JQ1, exhibiting a dissociation constant (KD) of 5.43 nM for BRD4(1).

GNE-049 is a highly selective and potent inhibitor designed to target the CREB-binding protein (CBP) with high affinity, exhibiting an IC50 of 1.1 nM for the suppression of BRET and BRD4 activity, which consequently blocks prostate cancer cell proliferation in both in vitro and in vivo models.

Y06137 is an effective and selective BET inhibitor with a Kd of 81 nM for BRD4(1) bromodomain. Y06137 can be used for research on the treatment of castration-resistant prostate cancer.

GNE-781 is a highly potent and selective inhibitor of CBP (IC50: 0.94 nM in TR-FRET assay). GNE-781 also inhibits BRET and BRD4(1) (IC50s: 6.2 nM and 5100 nM, respectively).

GNE-207 is a selective and orally bioavailable inhibitor of the bromodomain of CBP (IC50: 1 nM). It has a selective index of >2500-fold against BRD4 (1). GNE-207 displays excellent CBP potency (EC50: 18 nM for MYC expression in MV-4-11 cells).

Bromodomain inhibitor-10 (compound 128) is a highly potent bromodomain activity inhibitor, exhibiting strong binding affinity with Kd values of 15.0 nM and 2500 nM for BRD4-1 and BRD4-2, respectively. It also effectively inhibits the production of IL12p40 [1].

Bromodomain inhibitor-9 is an inhibitor of Bromodomains that selectively inhibits the activity of BRD4-1 with a Kd value of 12 nM. Bromodomain inhibitor-9 can be used in studies of diseases related to systemic or lipid metabolism, tissue inflammation, fibrosis, or chronic autoimmune diseases.

NC-III-49-1 is a potent bivalent bromodomain and extraterminal domain (BET) inhibitor with significant affinity for various BRD4 and BRDT isoforms, as demonstrated by its Kd values of 0.095 nM for BRD4-1, 0.32 nM for BRD4-2, 0.29 nM for BRD4-T, 0.089 nM for BRDT-1, 5.5 nM for BRDT-2, and 0.058 nM for BRDT-T. Additionally, NC-III-49-1 exhibits antiproliferative effects and reduces the expression of c-Myc [1].

GXH-II-052 is a potent bivalent inhibitor targeting the bromodomain and extraterminal domain (BET), exhibiting significant binding affinity to various BET proteins, including BRD4-1, BRD4-2, BRD4-T, BRDT-1, BRDT-2, and BRDT-T, with dissociation constants (Kd) of 28, 9.1, 4.8, 0.6, 8.4, and 2.6 nM, respectively. Additionally, GXH-II-052 demonstrates antiproliferative effects and reduces the expression of c-Myc [1].