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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
Boc-NH-PEG7-acetic acid V83031 Boc-NH-PEG7-acetic acid 141282-29-3 Boc-NH-PEG7-acetic acid is a PROTAC (PROteolysis TArgeting Chimera) linker, which belongs to the Polyethylene glycol (PEG) category and may be utilized to prepare PROTAC protein degraders.
BRD4 degrader AT1 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.
BSJ-03-123 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).
BSJ-03-204triTFA V77183 BSJ-03-204triTFA BSJ-03-204 triTFA is a PROTAC linked by Cereblon ligand and CDK ligand.
BSJ-4-116 V2485 BSJ-4-116 2519823-34-6 BSJ-4-116 is a PROTAC protein degrader linked by Cereblon ligand and CDK ligand.
BT-PROTAC V78571 BT-PROTAC 3032848-64-6 BT-PROTAC is a bioorthogonally activated prodrug.
Bz-Ala-Arg V83053 Bz-Ala-Arg 71448-11-8 Bz-Ala-Arg is a dipeptide.
c-Kit-IN-7 V93584 c-Kit-IN-7 2941026-35-1 c-Kit-IN-7 (Compound 104) is a potent inhibitor of c-Kit with IC50 less than or equal to 10 nM.
C004019 V70083 C004019 2417159-57-8 C004019 is a small molecule PROTAC.
CaMKIIα-PHOTAC V78617 CaMKIIα-PHOTAC CaMKIIα-PHOTAC is a photochemically targeted chimera (PHOTAC) targeting Ca2+/calmodulin-dependent protein kinase II α (CaMKIIα).
CARM1 degrader-1 hydrochloride V88885 CARM1 degrader-1 hydrochloride CARM1 degrader-1 hydrochloride is the hydrochloride form of CARM1 degrader-1.
CBPD-409 V88865 CBPD-409 CBPD-409 is an orally available CBP/p300 degrader with a DC50 of 0.2–0.4 nM.
Cbz-PEG2-bromide V83030 Cbz-PEG2-bromide 2100283-00-7 Cbz-PEG2-bromide is a PROTAC (PROteolysis TArgeting Chimera) linker, which belongs to the Polyethylene glycol (PEG) category and may be utilized to prepare PROTAC protein degraders.
CCT367766 formic V77160 CCT367766 formic CCT367766 formic is a potent orally bioactive protein, a third-generation heterofunctional and Cereblon ligand-based pirin-targeted protein degradation probe (PDP, or PROTAC) that can reduce pirin protein expression at low concentrations.
CDK2 degrader 2 V101101 CDK2 degrader 2 3030271-16-7 CDK2 Degrader 2 is a PROTAC-type CDK2 degrader, whose CDK2 binding moiety (CBM) is ubiquitinated after binding to CDK2 protein, thereby degrading CDK2 through the ubiquitin-proteasome pathway (UPP).
CDK9拮抗剂-1 V37524 CDK9 Antagonist-1 CDK9 Antagonist-1
CEP1347-VHL-02 V97287 CEP1347-VHL-02 CEP1347-VHL-02 is a PROTAC targeting MLK3, which consists of PROTAC target protein ligand CEP-1347 (red part), E3 ubiquitin ligase ligand (S,R,S)-AHPC-Me (blue part) and PROTAC Linker Amino-PEG3-CH2COOH (black part). The target protein ligand activity control is CEP-1347-acid, and the E3 ubiquitin ligase ligand + Linker conjugate is (S,R,S)-AHPC-Me-CO-CH2-PEG3-NH2.
CM11 (Homo-PROTAC) V17301 CM11 (Homo-PROTAC) 2244684-49-7 Homo-PROTAC pVHL30 degrader 1 is an effective PROTAC-based pVHL30 degrader.
CP-07 V78867 CP-07 CP-07 is a potent and specific PROTAACCDK9 degrader (DC50= 43 nM).
CPD-10 V104423 CPD-10 3055471-57-0 CPD-10 is a potent CCND1 and CDK4 PROTAC degrader.
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