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
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.
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.