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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

Structure Cat No. Product Name CAS No. Product Description
(4S)-PROTAC SOS1 degrader-1 V74715 (4S)-PROTAC SOS1 degrader-1 2913176-81-3 (4S)-PROTAC SOS1 degrader-1 is a potent PROTAC SOS1 degrader.
(R,S,S)-VH032 V83028 (R,S,S)-VH032 2230826-33-0 (R,S,S)-VH032 is Ligand for E3 Ligase used in the synthesis/preparation of PROTACs.
(S,R,S)-AHPC-3-methylbutanyl acetate-methanesulfonothioate-Me-C10-NH2 TFA 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.
(S,R,S)-AHPC-3-methylbutanyl acetate-methanesulfonothioate-PEG3-NH2 TFA 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.
(S,R,S)-AHPC-Me-C7 ester 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.
A031 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.
ACBI1 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.
ACBI1 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
AD4 V58319 AD4 2918262-09-4 AD4 is an artemisinin analogue that is a proteolytic targeting chimera (PROTAC) targeting PCLAF.
AK-1690 V94378 AK-1690 2984505-88-4 AK-1690 is a potent and selective STAT6 PROTAC degrader.
AP-1 V104710 AP-1 3027918-96-0
ARD-2051 V67608 ARD-2051 2632305-17-8 ARD-2051 is a potent, orally bioactive, proteolytically targeted chimeric degrader of the androgen receptor (AR).
ARD-2128 V67602 ARD-2128 2222111-87-5 ARD-2128 is a potent PROTAC androgen receptor (AR) degrader.
ARD-2585 V67594 ARD-2585 2757422-79-8 ARD-2585 is a potent, orally bioactive androgen receptor PROTAC protein degrader.
ARD-266 V67601 ARD-266 2666951-70-6 ARD-266 is a highly efficient von Hippel-Lindau E3 ligase-based androgen receptor (AR) PROTAC degrader.
ARM165 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.
ARV-393 V86806 ARV-393 2851885-95-3 ARV-393 is an orally available PROTAC that utilizes the ubiquitin proteasome system to target BCL6 for degradation.
ARV-771 V3579 ARV-771 1949837-12-0 ARV-771 (ARV771) is a novel and potent PROTAC-based degrader of bromodomain and extra-terminal (BET) proteins with the potential to be usedin the treatment of cancers such as CRPC.
AT6 V3582 AT6 2098836-50-9 AT6 is a novel, potent and highly selective PROTAC-based BRD degrader, it isanalog of AT1.
Biotin alkyne V83051 Biotin alkyne 773888-45-2 Biotin alkyne is a PROTAC (PROteolysis TArgeting Chimera) linker and belongs to the PEG (Polyethylene glycol) class, may be utilized to prepare PROTAC molecules.
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