Thalidomide-O-C6-Amine HCl is a functionalized cereblon ligand used for PROTAC research. It incorporates an E3 ligase ligand and a C6 alkyl linker to conjugate to a target protein.
N-(2-(2-Aminoethoxy)ethyl)-2-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)acetamide is an E3 ligase ligand-linker conjugate used in PROTAC dTAG-13 as a degrader of FKBP12, F36V, and BET proteins.
MS4078 is a heterobifunctional linker that binds to protein targets and delivers cytotoxic agents. It has a selective binding affinity for tumor cells and has shown minimal toxicity in pre-clinical studies.
GMB-475 acts as a degrader of BCR-ABL 1 tyrosine kinase and as a recruiter of the E3 ligase Von Hippel Lindau (VHL) resulting in ubiquitination and subsequent degradation of oncogenic fusion proteins.
ARV-771 is a BET PROTAC based on E3 ligase von Hippel-Lindau with Kds of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1) and BRD4(2), respectively.
BETd-260 is a PROTAC connected by ligands for Cereblon and BET proteins. It potently suppresses cell viability and induces apoptosis in hepatocellular carcinomca (HCC) cells.
THAL-SNS-032 is a selective CDK9 degrader PROTAC composed of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN).
