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 |
---|---|---|---|---|
V83050 | Thalidomide-5-OH | 64567-60-8 | Thalidomide-5-OH is a Thalidomide-based cereblon (E3 ligase) ligand that recruits CRBN protein. | |
V83037 | Thalidomide-5-PEG4-NH2 hydrochloride | 2743434-24-2 | Thalidomide-5-PEG4-NH2 HCl is a ligand (for E3 ligase )-linker conjugate composed of Thalidomide (ligand for E3 ligase cereblon/CRBN) and a linker. | |
V53077 | Thalidomide-O-amido-C11-COOH | 2473270-96-9 | Thalidomide-O-amido-C11-COOH (compound IMiD acid 1) is an E3 ligase ligand and linker CRBN (Cereblon) conjugate. | |
V83040 | Thalidomide-Piperazine-Piperidine hydrochloride | 2599846-44-1 | Thalidomide-Piperazine-Piperidine HCl is a ligand (for E3 ligase )-linker conjugate. | |
V82338 | Toralactone (cassia lactone) | 41743-74-2 | Toralactone, extracted from Cassia obtusifolia, mediates liver protection through an Nrf2-dependent antioxidant mechanism. | |
V81671 | UNC7096 | UNC7096 is a potent and specific NSD2-PWWP1 inhibitor (antagonist) with a Kd of 46 nM. | ||
V83044 | V-9302 hydrochloride | 2416138-42-4 | V-9302 HCl is a competitive antagonist of transmembrane glutamine flux. | |
V67644 | Vepdegestrant (ARV-471) | 2229711-68-4 | Vepdegestrant (ARV-471) is an oral estrogen receptor PROTAC protein degrader for breast cancer. | |
V76341 | YD23 | YD23 is a SMARCA2 PROTAC. | ||
V81765 | YN14 | YN14 is a KRASG12C proteolysis targeting chimera (PROTAC). | ||
V3577 | ZXH-3-26 | 2243076-67-5 | ZXH-3-26 is a novel, potent and selectivedegrader of BRD4with aDC50/5h(half-maximal degradation after 5 hours of treatment) of ~ 5 nM. | |
V71335 | α1A-AR Degrader 9c | 2863635-02-1 | α1A-AR Degrader 9c (Compound 9c) is a specific, reversible α1A-AR (adrenergic receptor) PROTAC degrader with DC50 of 2.86 μM. |