BRD4 Inhibitor

FL-411 is a potent and selective BRD4 inhibitor with an IC₅₀ of 0.43±0.09 μM for BRD4(1).

MS402 is a BD1-selective BET BrD inhibitor with K_is of 77 nM, 718 nM, 110 nM, 200 nM, 83 nM, and 240 nM for BRD4(BD1), BRD4(BD2), BRD3(BD1), BRD3(BD2), BRD2(BD1) and BRD2(BD2), respectively. MS402 blocks Th17 cell differentiation and ameliorates colitis in mice.

CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a K_i of <1 nM, K_d 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, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo.

BRD4 Inhibitor-10 is a potent BRD4-BD1 inhibitor with an IC₅₀ of 8 nM. BRD4 Inhibitor-10 interferes with the recognition of acetylated histone marks by the BRD4 bromodomain through inhibiting the interaction between BRD4-BD1 and tetra-acetylated histone H4 peptide. BRD4 Inhibitor-10 is used for research on BRD4-mediated epigenetic regulation and cancer.

BRD4/NAMPT-IN-1 (Compound A2) shows strong inhibitory effects on NAMPT and BRD4 (IC₅₀=35 nM (NAMPT) and 58 nM (BRD4)). BRD4/NAMPT-IN-1 inhibits the growth and migration of hepatocellular carcinoma cells and promotes apoptosis. BRD4/NAMPT-IN-1 also shows potent anticancer effects in HCCLM3 xenograft mouse model, with no obvious toxic effects.

(Z)-JQ1-TCO is a derivative of JQ1 (HY-13030), an inhibitor of BET. (Z)-JQ1-TCO is suitable for click chemistry and can be used as molecular probes in vitro and in vivo.

CBP/p300-IN-8 is a potent inhibitor of the CBP/P300 family of bromodomains. CBP/p300-IN-8 inhibits CBP (IC₅₀=0.01-0.1 µΜ) and BRD4 (IC₅₀=1-1000 µΜ) activity.

GAL-02-221 is a BRD4 PROTAC degrader with blood-brain barrier permeability, with a DC₅₀ of 0.009 μM (Jurkat BRD4-HiBiT). GAL-02-221 induces proteasome-catalyzed BRD4 degradation, binds to VHL to trigger BRD4 ubiquitination, and recruits the VHL E3 ligase complex to participate in protein degradation. GAL-02-221 degrades BRD4 in breast cancer cells as well as mouse liver and brain tissues. GAL-02-221 is applicable to research related to breast cancer.

BET bromodomain inhibitor 1 is an orally active, selective bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC₅₀ of 2.6 nM for BRD4. BET bromodomain inhibitor 1 binds to BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with high affinities (K_d values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, 2.1 nM, respectively). bromodomain inhibitor 1 has anti-cancer activity.

UMB298 is a potent and selective CBP/P300 bromodomain inhibitor.

BRD4 Inhibitor-20 is a potent orally active bromodomain protein 4 (BRD4) inhibitor. BRD4 Inhibitor-20 has inhibitory activity for BRD4 (BD1) and BRD4 (BD2) with IC₅₀ values of 19 nM and 28 nM, respectively. BRD4 Inhibitor-20 also has anti-proliferation activities in cancer cell lines. BRD4 Inhibitor-20 can be used for the research of kinds of cancer, such as colon cancer.

BETd-246 is a BRD2/3/4 PROTAC degrader targeting the BET family. BETd-246 induces ubiquitination and proteasomal degradation of BRD2, BRD3 and BRD4 by recruiting the CUL4-RBX1-DDB1-CRBN E3 ubiquitin ligase complex; it also inhibits TRAT1 expression and depletes BET proteins. BETd-246 suppresses cancer cell proliferation and invasion, disrupts the cell cycle and induces apoptosis. BETd-246 is applicable to research related to triple-negative breast cancer and T-cell acute lymphoblastic leukemia.

PROTAC BET degrader-2 is a BET PROTAC degrader. PROTAC BET degrader-2 induces dose-dependent degradation of BRD2, BRD3 and BRD4 proteins in leukemia cells. PROTAC BET degrader-2 inhibits the growth of acute leukemia cells. PROTAC BET degrader-2 can be used for the research of acute leukemia.

OARV-771 is a VHL-based BET degrader (PROTAC) with improved cell permeability. OARV-771 shows DC₅₀s of 6, 1, and 4 nM for Brd4, Brd2 and Brd3, respectively.

BRD4/CK2-IN-1 is the first highly effective and oral active dual-target inhibitor of BRD4/CK2 (bromodomain-containing protein 4/casein kinase 2), with IC₅₀s of 180 nM and 230 nM for BRD4 and CK2, respectively. BRD4/CK2-IN-1 has strong anticancer activity without obvious toxicities. BRD4/CK2-IN-1 induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC)

Y06036 is a potent and selective BET inhibitor, which binds to the BRD4(1) bromodomain with K_d value of 82 nM. Antitumor activity.

dBET23 is a highly potent and selective BRD4 PROTAC degrader, with a DC_50/5h of approximately 50 nM against the BRD4BD1 protein. dBET23 induces the formation of a ternary complex consisting of CRBN, itself, and BRD4BD1, thereby mediating the degradation of BRD4BD1. dBET23 causes downregulation of BRD4 expression in cancer cells. dBET23 can be used for research on malignant tumors.

PROTAC BRD4 Degrader-2 is a PROTAC connected by ligands for Cereblon and BRD4 with an IC₅₀ of 14.2 nM against BRD4 BD1.

Zavabresib (OPN-2853; PLX2853; BET-IN-16) is an orally active inhibitor of the BET family of proteins. Zavabresib blocks bromodomain-mediated interactions, reduces BRD4 enrichment at the regulatory regions of transcription factors in T cells, exerts tumor growth inhibitory effects, and enhances the efficacy of immunotherapy. Zavabresib is applicable to research on chronic lymphocytic leukemia, castration-resistant prostate cancer, diffuse large B-cell lymphoma, colon adenocarcinoma, and myelofibrosis.

XD14 is a potent BET inhibitor with antitumor effect. It binds to BRD2, BRD3, and BRD4 with K_ds of 170, 380, and 160 nM, respectively.