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].
Thalidomide-4-NH-PEG1-COO(t-Bu) is a t-Bu modified Thalidomide (HY-14658), which acts as a Cereblon ligand to recruit CRBN protein. The t-Bu protecting group at the end of Thalidomide-4-NH-PEG1-COO(t-Bu) can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-4-NH-PEG1-COO(t-Bu) is a key intermediate in the synthesis of CRBN-based PROTAC molecules.
Pomalidomide-7-NH2 is the Pomalidomide-based cereblon ligand used in the recruitment of CRBN protein. Pomalidomide-7-NH2 can be connected to the ligand for protein by a linker to form PROTACs[1].
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].
Thalidomide-5-NH-PEG1-NH2 hydrochloride is a Thalidomide (HY-14658)-based cereblon ligand that recruits CRBN proteins. Thalidomide-5-NH-PEG1-NH2 hydrochloride can be connected to the target protein ligand through a linker to form a PROTAC molecule. For example, THAL-SNS-032 (HY-123937).
ZXH-1-161 is a potent cereblon (CRBN) modulator with an IC50 value of 39 nM in MM1.S wild type cells. ZXH-1-161 has selective degradation activity towards GSPT1. ZXH-1-161 can be used for researching multiple myeloma[1].
A VHL ligand for PROTAC.
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].