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
V74715 (4S)-PROTAC SOS1 degrader-1 2913176-81-3
V83028 (R,S,S)-VH032 2230826-33-0
V83033 (S,R,S)-AHPC-3-methylbutanyl acetate-methanesulfonothioate-Me-C10-NH2 TFA 2417370-89-7
V83039 (S,R,S)-AHPC-3-methylbutanyl acetate-methanesulfonothioate-PEG3-NH2 TFA 2417370-48-8
V83027 (S,R,S)-AHPC-Me-C7 ester 2639528-48-4
V67622 A031 2682255-44-1
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
V67608 ARD-2051 2632305-17-8
V67602 ARD-2128 2222111-87-5
V67594 ARD-2585 2757422-79-8
V67601 ARD-266 2666951-70-6
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.
V3582 AT6 2098836-50-9 AT6 is a novel, potent and highly selective PROTAC-based BRD degrader, it isanalog of AT1.
V83051 Biotin alkyne 773888-45-2
V83031 Boc-NH-PEG7-acetic acid 141282-29-3
V3581 BRD4 degrader AT1 2098836-45-2 BRD4 degrader AT1 is a novel, potent and highly selectivePROTAC-based BRD4degrader (Kd= 44 nM for Brd4BD2in cells) with anticancer activity.
V3439 BSJ-03-123 2361493-16-3 BSJ-03-123 is a novel, potentcyclin-dependent kinase 6 (CDK6)-selective small-molecule degrader (PROTAC: proteolysis targeting chimera).
V77183 BSJ-03-204triTFA
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