protac bet degrader1

PROTAC BET Degrader-1 is a potent BET degrader utilizing the PROTAC mechanism.

PROTACBET Degrader-12 (Compound 8b) is a PROTAC degrader targeting proteins with bromodomains and extraterminal (BET) domains, facilitating the degradation of BRD3 and BRD4 in a DCAF11-dependent manner. It inhibits the viability of KBM7 cells with a DC50 of 305.2 nM.

PROTACBET Degrader-13 (Compound 34) is a TRIM21-based PROTAC (TRIMTAC) degrader that targets BET proteins. It effectively degrades the PML-eGFP-BRD4 fusion protein, causing a near-complete loss of EGFP+ nuclear foci with an EC50 of 1.4 μM.

PROTACBET Degrader-14 is a potent PROTAC compound designed to target BET (bromodomain and extraterminal domain) proteins. It effectively degrades all family members of BET, including BRD2, BRD3, and BRD4. The compound demonstrates significant efficacy in degrading BET proteins in the U2OS osteosarcoma cell line (BRD4 DC50 = 130 nM) and the KYSE180 esophageal squamous cell carcinoma cell line (DC50 = 40 nM). Its mechanism of degradation relies on the ubiquitin-proteasome system. Furthermore, PROTACBET Degrader-14 reduces the expression levels of BET-regulated gene products such as c-Myc, RUNX2, and KRT14, making it a valuable tool for osteosarcoma research.

PROTAC BET Degrader-10 (WO2017007612A1, example 37) is a highly efficient and selective small molecule compound designed to degrade BET protein BRD4. PROTAC BET Degrader-10 functions by utilizing specific ligands that connect Cereblon and BRD4, with a DC 50 value of 49 nM.