PROTACs

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PROTACs

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.

PROTACs related products

Cat No.	Product Name	CAS No.	Product Description
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.