E3 ligase Ligand 4 is a ligand of E3 ligase, used in PROTAC technology.
Thalidomide-5-propargyne-NH2 hydrochloride is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5-propargyne-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs[1].
Thalidomide 5-fluoride is Thalidomide-based cereblon ligand that incorporates to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1.
Homo-PROTAC pVHL30 degrader 1 is a potent pVHL30 degrader based on PROTAC[1].
Pomalidomide-C5-Dovitinib (compound 2) is a PROTAC containing Pomalidomide, Dovitinib and connected with CRBN. Pomalidomide-C5-Dovitinib shows enhanced antiproliferative effects against FLT3-ITD+ AML cells. Pomalidomide-C5-Dovitinib induces the degradation of the FLT3-ITD and KIT proteins in a ubiquitin-proteasome-dependent manner and completely blocks their downstream signaling pathway. Pomalidomide-C5-Dovitinib has the potential for the research of FLT3-ITD+ acute myeloid leukemia[1].
Thalidomide D4 is a deuterium labeled Thalidomide. Thalidomide is initially promoted as a sedative, inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ~250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties[1][2].
Pomalidomide-CO-C5-azide (Compound PA) is a ligand for E3 ligase bearing a bioorthogonal group azide. Pomalidomide-CO-C5-azide can be used to synthesize PROTACs with anticancer activity[1].
ALV1 is a potent Ikaros and Helios degrader. ALV1 potently reduces the protein abundance of IKZF1-4, CK1α (casein kinase 1α, CSNK1A1) and ribosomal protein RPL4. ALV1 shows similar degradation activity towards IKZF1/2/3. ALV1 induced Helios/CRBN dimerization. ALV1 promoted IL-2 secretion to a great extent[1].