brd in 3

BRD-IN-3 is a highly potent PCAF bromodomain (BRD) inhibitor (IC50: 7 nM). It also exhibits activity against GCN5 and FALZ.

BRD4-Kinases-IN-3 is a dual BRD4-Kinases inhibitor that can be used as a value-added multi-targeted chemical probe for cancer therapy.

BRD PHOTAC-I-3 is a photoswitchable BET bromodomain degrader (PHOTAC, PHOtochemically TArgeting Chimera). BRD PHOTAC-I-3 comprises a ligand for an E3 ligase, a photoswitch, and the BET bromodomain targeting ligand (+)-JQ1. Exhibits cytotoxicity and degrades BRD4, BRD3 and to a lesser extent BRD2 in lymphoblast cells upon irradiation with 390 nm light, but not in the dark.

PROTAC BRD4 Degrader-3 is an efficacious degrader of PROTAC BRD4.

PARP1/BRD4-IN-3 (compound HF4) is an effective inhibitor of BRD4 and PARP1, with IC50 values of 1210 nM and 2019 nM respectively. The compound exhibits antiproliferative activity, induces apoptosis (apoptosis) and cell cycle arrest at the G0/G1 phase. Additionally, PARP1/BRD4-IN-3 causes DNA damage and reduces the expression of the Rad51 protein, demonstrating anti-tumor activity.

HDAC3/BRD4-IN-1 (compound 26n) is an inhibitor of HDAC3/BRD4, exhibiting an IC50 of 8 nM for HDAC3, while its IC50 values for HDAC1 and HDAC2 are 220 nM and 120 nM, respectively. It displays anti-tumor and anti-proliferative effects by upregulating Ac-H3 and downregulating c-Myc. The half-life of HDAC3/BRD4-IN-1 in human liver microsomes is 29.36 minutes.

BRD4-BD1-IN-3 (Compound 4g) is an inhibitor of BRD4-BD1. It is applicable in the study of inflammatory diseases.

BRD4-BD1/2-IN-3 is a highly selective BRD4 BD2 inhibitor (IC50 = 0.41 nM) that exhibits strong selectivity over BRD4 BD1 and potently suppresses LPS-induced IL-6 expression. BRD4-BD1/2-IN-3 modulates TNF and NF-κB signaling pathways, providing a valuable tool for studying BRD4 biology and for researches on inflammatory diseases.

PROTACFLT3/JAK2/BRD4 Degrader-1 is a PROTAC degrader targeting FLT3, JAK2, and BRD4, with DC50 values of 5.23 nM, 0.678 nM, and 1.17 nM, respectively. It exhibits potent antiproliferative activity against MV4;11 cells (IC50= 0.79 nM) and FLT3-mutated Ba/F3 cells. Additionally, PROTACFLT3/JAK2/BRD4 Degrader-1 induces apoptosis in MV4;11 cells and demonstrates significant antitumor efficacy in an MV4;11 xenograft model established in NOD SCID mice. This compound is applicable for research in acute myeloid leukemia (AML).

BRD7-IN-3 (compound 1-78) is a dual inhibitor of bromodomain-containing proteins BRD7 and BRD9, with half-maximal inhibitory concentrations (IC50s) of 1.6 μM for BRD7 and 2.7 μM for BRD9, respectively [1].

PROTAC BRD3/BRD4-L degrader-2, a PROTAC molecule, selectively degrades cellular BRD3 and BRD4-L with K i values of 16.91 and 2.8 nM, respectively, and exhibits robust antitumor activity in mouse xenograft models, serving as a research tool for cancer [1].

PROTAC BRD9 Degrader-3 is a bifunctional degrader targeting BRD9, used in cancer research.

Compound 21, also known as PLK1/BRD4-IN-3, acts as a selective dual inhibitor targeting both bromodomain 4 (BRD4) and polo-like kinase 1 (PLK1). It effectively inhibits BRD4-BD1, PLK1, and BRDT-BD1, exhibiting IC50 values of 0.059, 0.127, and 0.245 μM, respectively.

BRD9 Degrader-3 (compound B20) is a molecular glue for BRD9 with a DC50 of less than 1.25 nM.

PROTAC BRD4 Ligand-3 serves as a ligand for target proteins in PROTACs (Ligands for Target Protein for PROTACs). It is utilized in the synthesis process.

BTR2004 is a selective PROTAC degrader targeting the BET family (BRD2/3/4) proteins. It facilitates the formation of a ternary complex with BRD proteins and KLHL20, leading to ubiquitination and proteasomal degradation via the UPS pathway. BTR2004 shows potential for research in PC3 prostate cancer and MDA-MB-231 breast cancer cell lines.