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
V74715	(4S)-PROTAC SOS1 degrader-1	2913176-81-3	(4S)-PROTAC SOS1 degrader-1 is a potent PROTAC SOS1 degrader.
V83028	(R,S,S)-VH032	2230826-33-0	(R,S,S)-VH032 is Ligand for E3 Ligase used in the synthesis/preparation of PROTACs.
V122034	(Rac)-P1D-34	2957895-04-2	(Rac)-P1D-34 is a PROTAC-based PIN1 degrader (pink: PIN1 ligand, blue: cereblon ligand thalidomide, black: linker).
V122161	(S)-dHTC1	3081383-46-9	(S)-dHTC1 is a molecular glue degrader that targets the transcriptional coactivator ENL.
V83033	(S,R,S)-AHPC-3-methylbutanyl acetate-methanesulfonothioate-Me-C10-NH2 TFA	2417370-89-7	(S,R,S)-AHPC-3-methylbutanyl acetate-methanesulfonothioate-Me-C10-NH2 TFA is a synthetic E3 ligase (e.g. CRBN) ligand-linker conjugate containing (S,R,S)-AHPC ligand body and may be utilized in PROTAC studies.
V83039	(S,R,S)-AHPC-3-methylbutanyl acetate-methanesulfonothioate-PEG3-NH2 TFA	2417370-48-8	(S,R,S)-AHPC-3-methylbutanyl acetate-methanesulfonothioate-PEG3-NH2 TFA is a ligand (for E3 ligase )-linker conjugate containing (S,R,S)-AHPC-based ligands.
V83027	(S,R,S)-AHPC-Me-C7 ester	2639528-48-4	(S,R,S)-AHPC-Me-C7 ester is an E3 ligase-connexin conjugate used in the preparation /synthesis of BCL-XL PROTAC protein degrader.
V127135	5-Norbornene-2-methylamine-C10-NH2		5-Norbornene-2-methylamine-C10-NH2 is a hydrophobic tag (HyT)-linker conjugate targeting Keap1, comprising a HyT and a linker.
V67622	A031	2682255-44-1	A031 is a highly efficient PROTAC androgen receptor (AR) degrader that degrades AR protein with IC50 of less than 0.25 μM.
V127998	AA-BR-157		AA-BR-157 is a metallothionein 2A (MT2A) PROTAC degrader.
V37523	ACBI1		ACBI1 is a novel and potent PROTAC-based degrader of BAF ATPase subunits SMARCA2 and SMARCA4, it also degrades the polybromo-associated BAF (PBAF) complex member PBRM1
V41715	ACBI1	2375564-55-7	ACBI1 (ACBI-1) is PROTAC degrader of BAF ATPase subunits SMARCA2 and SMARCA4 (DC50 = 6 nM, 11 nM and 32 nM for SMARCA2, SMARCA4 and PBRM1 in MV-4-11 cells) with anticancer activity.
V58319	AD4	2918262-09-4	AD4 is an artemisinin analogue that is a proteolytic targeting chimera (PROTAC) targeting PCLAF.
V94378	AK-1690	2984505-88-4	AK-1690 is a potent and selective STAT6 PROTAC degrader.
V104710	AP-1	3027918-96-0	AP-1 is a PROTAC targeting anaplastic lymphoma kinase (ALK).
V67608	ARD-2051	2632305-17-8	ARD-2051 is a potent, orally bioactive, proteolytically targeted chimeric degrader of the androgen receptor (AR).
V67602	ARD-2128	2222111-87-5	ARD-2128 is a potent PROTAC androgen receptor (AR) degrader.
V67594	ARD-2585	2757422-79-8	ARD-2585 is a potent, orally bioactive androgen receptor PROTAC protein degrader.
V67601	ARD-266	2666951-70-6	ARD-266 is a highly efficient von Hippel-Lindau E3 ligase-based androgen receptor (AR) PROTAC degrader.
V101624	ARM165		ARM165 is a heterobifunctional molecule that can degrade the protein PIK3CG and inhibit the PI3Kγ-Akt signaling pathway, thereby exerting an anti-leukemia effect.