Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation.E3 Ligase Binder, Linker, and Target Binder are the components of PROTACs. The Target Binder is a ligand (often a small-molecule inhibitor) for the protein of interest. When the PROTACs attach to the target protein, they can recruit E3 for target protein ubiquitination, which results in proteasome-mediated destruction of the protein. Because of this, PROTACs work by destroying the target proteins rather than blocking them, which is far more effective at overcoming resistance brought on by target mutation or overexpression. In order to overcome resistance, PROTAC technology has been used on a number of targets, including AR, ER, BTK, BET, and BCR-ABL.
Structure | Cat No. | Product Name | CAS No. | Product Description |
---|---|---|---|---|
V83057 | galactonic acid | 13382-27-9 | Galactonic acid is a sugar acid, a product of the metabolic breakdown of galactose. | |
V69656 | GBD-9 | 2864408-92-2 | GBD-9 is a dual-mechanism degrader that efficiently degrades BTK and GSPT1 by recruiting the E3 ligase cereblon (CRBN). | |
V3586 | Gefitinib-based PROTAC 3 | 2230821-27-7 | Gefitinib-based PROTAC 3 is a novel, potent and selective VHL-recruiting PROTAC that induces the degradation of EGFR and EGFR mutants with DC50 of 11.7 nM and 22.3 nM for HCC827 cell (Exon 19 del) and H3255 cell (L858R). | |
V2185 | GMB-475 | 2490599-18-1 | :GMB-475 is a novel and potent degrader of BCR-ABL1 tyrosine kinase based on PROTAC, overcoming BCR-ABL1-dependent drug resistance. | |
V75491 | GNE-987 | 2417371-71-0 | GNE-987 is a PROTAC linked to a von Hippel-Lindau ligand and a BRD4 ligand. | |
V60079 | GSK215 | 2743427-26-9 | GSK215 is a potent and selective PROTAC adhesion kinase (FAK) degrader, pDC50 The value is 8.4. | |
V79678 | GXF-111 | GXF-111 is a PROTAC molecule that promotes the selective degradation of cellular BRD3 and BRD4-L. | ||
V31459 | Homo-PROTAC cereblon degrader 1 | 2244520-98-5 | Homo-PROTAC cereblon degrader 1 (compound 15a) is a highly potent and efficient cereblon (CRBN) degrader with only minimal effects on IKZF1 and IKZF3. | |
V83054 | Imidazole-d4 (imidazole-d4; isopyrazole-d4; metazolin-d4) | 6923-01-9 | Imidazole-d4 is the deuterated form of Imidazole. | |
V70216 | INY-03-041 | 2503017-97-6 | INY-03-041 is a specific PROTAC-based pan-AKT degrader, consisting of the ATP-competitive AKT inhibitor Ipatasertib combined with Lenalidomide (Cereblon ligand). | |
V76888 | INY-03-041 trihydrochloride | INY-03-041 tri HCl is a specific PROTAC-based pan-AKT degrader, consisting of the ATP-competitive AKT inhibitor Ipatasertib combined with Lenalidomide (Cereblon ligand). | ||
V80396 | IR808-TZ | IR808-TZ is an effective BRD4 BT-PROTAC protein degrader. | ||
V80437 | JET-209 | JET-209 is a potent PROTAC CBP/p300 degrader with DC50s of 0.05 nM and 0.2 nM for CBP and p300. | ||
V76858 | JPS016 TFA | JPS016 TFA is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolytic targeting chimera (PROTAC). | ||
V75053 | KTX-951 | 2573298-36-7 | KTX-951 is a PROTAC that targets IRAK4 degradation (DC50= 18 nM). | |
V83045 | L-Azidohomoalanine hydrochloride | 942518-29-8 | L-Azidohomoalanine HCl is a PROTAC (PROteolysis TArgeting Chimera) linker and belongs to the alkyl chain class, may be utilized to prepare PROTAC molecules. | |
V83056 | L-Threonine-13C4,15N,d5 (L-Threonine 13C4,15N,d5) | 2378755-51-0 | L-Threonine-13C4,15N,d5 is L-Threonine with 13C, 15N and deuterated labels. | |
V83055 | L-Valine-1-13C,15N (L-Valine 1-13C,15N) | 87019-54-3 | L-Valine-1-13C,15N is L-Valine with 13C mark and 15N mark. | |
V83049 | Legumain inhibitor 1 | 2361157-34-6 | Legumain inhibitor 1 is a potent and specific Legumain inhibitor (antagonist) with IC50 of 3.6 nM. | |
V83048 | Lenalidomide-Br | 2093387-36-9 | Lenalidomide-Br (Compound 41) is an analogue of the cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligases and is used for recruitment of CRBN proteins. |