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
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.
V86774	LHF418		LHF418 is a potent SOS1 PROTAC degrader with a DC50 value of 209.4 nM in A549 cells.
V87637	LYP-8		LYP-8 is a potent NAMPT degrader, with a maximum degradation rate of 97% for NAMPT in SKOV-3 cells at 0.5 μM.
V31651	MD-224	2136247-12-4	MD-224 is a novel, first-in-class and potent PROTAC molecule targeting human murine double minute 2 (MDM2) for degradation, it has the potential to be used as a new class of anticancer agent.
V75085	MD13	2758431-97-7	MD13 is a macrophage migration inhibitory factor (MIF)-directed PROTAC with a Ki of 71 nM.
V89698	MPD2		MPD2 is a Cereblon-binding ligand-based PROTAC that degrades MPro, the main protease of SARS-CoV-2.
V76743	MS15		MS15 is an effective and selective degrader of AKT PROTAC.
V76742	MS15 TFA		MS15 TFA is an effective and selective degrader of AKT PROTAC.
V70218	MS170	2376136-61-5	MS170 is an effective and selective PROTAC AKT degrader.
V74084	MS432	2672512-44-4	MS432 is an innovative, selective PROTAC degrader of MEK1 and MEK2 based on PD0325901 and von Hippel-Lindau ligands.
V83038	MS83	2762181-19-9	MS83 is a PROTAC molecule by linking KEAP1 ligand to BRD4/3/2 ligand.
V80842	MS83 epimer 1		MS83 epimer 1 is the epimer of MS83.
V69407	MS9427	2772613-37-1	MS9427 is a potent PROTAC EGFR degrader with Kds of 7.1 nM and 4.3 nM for wild-type EGFR and mutant EGFR L858R, respectively.
V76740	MS9427 TFA		MS9427 TFA is a potent PROTAC EGFR degrader with Kds of 7.1 nM and 4.3 nM for wild-type EGFR and mutant EGFR L858R, respectively.
V69415	MS9449	2772612-96-9	MS9449 is a potent PROTAC EGFR degrader with Kds of 17 nM and 10 nM for wild-type EGFR and mutant EGFR L858R, respectively.