brd41

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.

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 potent and selective inhibitor of CBP (IC50: 1.1 nM in TR-FRET assay), and also inhibits BRET and BRD4(1) with IC50 values of 12 nM and 4200 nM, respectively.

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).

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.

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].

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].

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].