BRD3 Degrader

Pomalidomide-C5-Dovitinib is a heterobifunctional PROTAC that recruits KEAP1 E3 ligase to degrade BRD4 and BRD3, but not BRD2.

PROTAC BRD4 Degrader-22 is a BRD4 PROTAC degrader with a DC₅₀ of 0.59 nM. At high concentrations, PROTAC BRD4 Degrader-22 induces partial degradation of BRD3 and BRD2, but exhibits selectivity for IKZF3. PROTAC BRD4 Degrader-22 can be used in leukemia-related research.

PROTAC BET Degrader-14 is a highly efficient PROTAC targeting BET (bromodomain and extra-terminal domain). PROTAC BET Degrader-14 can degrade all BET (BRD2, BRD3, BRD4) family proteins. PROTAC BET Degrader-14 potently degrades BET proteins in U2OS osteosarcoma cell lines (BRD4 DC₅₀ = 130 nM) and KYSE180 esophageal squamous cell carcinoma cell lines (DC₅₀ = 40 nM). PROTAC BET Degrader-14’s dependence on the ubiquitin-proteasome system. PROTAC BET Degrader-14 decreases levels of BET-regulated gene products c-Myc, RUNX2, and KRT14. PROTAC BET Degrader-14 can be used for the study of osteosarcoma.

AB3067 is a PROTAC degrader of BET that simultaneously recruits the E3 ligase activities of CRBN and VHL. The DC₅₀ values of AB3067 against BRD2, BRD3, BRD4^Short and BRD4^Long are 15 nM, 1.6 nM, 2.1 nM and 2.3 nM, respectively. AB3067 induces additive protein ubiquitination and proteasomal degradation, and minimizes the cross-degradation of E3 ligases. AB3067 can be used in colon cancer-related studies.

ARV-771 (Standard) is the analytical standard of ARV-771 (HY-100972). This product is intended for research and analytical applications. ARV-771 is a BET PROTAC degrader, with K_d values of 34, 4.7, 8.3, 7.6, 9.6 and 7.6 nM against BRD2 (1), BRD2 (2), BRD3 (1), BRD3 (2), BRD4 (1) and BRD4 (2) , respectively. ARV-771 inhibits the transcription of AR/AR-v7 and its downstream target genes. By degrading BRD4 protein, ARV-771 enhances the sensitivity of prostate cancer cells to ferroptosis, suppresses cancer cell viability, and induces apoptosis. ARV-771 downregulates the levels of BRD4, c-MYC and AR-V7 in tumor tissues and inhibits tumor tissue growth. ARV-771 can be used in prostate cancer-related research.