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
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.
V76743	MS15		MS15 is an effective and selective degrader of AKT PROTAC.
V76742	MS15 TFA		MS15 TFA is an effective and selective degrader of AKT PROTAC.
V70218	MS170	2376136-61-5	MS170 is an effective and selective PROTAC AKT degrader.
V74084	MS432	2672512-44-4	MS432 is an innovative, selective PROTAC degrader of MEK1 and MEK2 based on PD0325901 and von Hippel-Lindau ligands.
V83038	MS83	2762181-19-9	MS83 is a PROTAC molecule by linking KEAP1 ligand to BRD4/3/2 ligand.
V80842	MS83 epimer 1		MS83 epimer 1 is the epimer of MS83.
V69407	MS9427	2772613-37-1	MS9427 is a potent PROTAC EGFR degrader with Kds of 7.1 nM and 4.3 nM for wild-type EGFR and mutant EGFR L858R, respectively.
V76740	MS9427 TFA		MS9427 TFA is a potent PROTAC EGFR degrader with Kds of 7.1 nM and 4.3 nM for wild-type EGFR and mutant EGFR L858R, respectively.
V69415	MS9449	2772612-96-9	MS9449 is a potent PROTAC EGFR degrader with Kds of 17 nM and 10 nM for wild-type EGFR and mutant EGFR L858R, respectively.
V80843	MS9715		MS9715 is a potent and specific NSD3 PROTAC.
V70220	MS98	2376137-31-2	MS98 is an effective and selective PROTAC AKT degrader.
V3580	MZ1	1797406-69-9	MZ 1 (MZ1; MZ-1) is a novel and potentPROTAC-based degrader of BRD4protein with anticancer activity.
V3583	MZP-54	2010159-47-2	MZP-54 is a novel, potent and selective PROTAC-based degrader ofBRD3/4with aKdof 4 nM for Brd4BD2.
V83046	N-Boc-piperazine	57260-71-6	N-Boc-piperazine is a PROTAC (PROteolysis TArgeting Chimera) linker of the Alkyl/ether class, may be utilized to prepare PROTAC PD-1/PD-L1 degrader-1 .
V83047	NH2-PEG2-C6-Cl	744203-60-9	NH2-PEG2-C6-Cl is a PROTAC (PROteolysis TArgeting Chimera) linker of the Polyethylene glycol (PEG) category, may be utilized to prepare PROTAC protein degraders.
V83036	NH2-PEG2-CH2-Boc	1948273-09-3	NH2-PEG2-CH2-Boc is a PROTAC (PROteolysis TArgeting Chimera) linker of the PEG category, may be utilized to prepare PROTAC protein degraders.
V74168	NJH-2-056	2858812-69-6	NJH-2-056 is a deubiquitinase-targeting chimera (DUBTAC) connecting the OTUB1 recruitment factor EN523 and the CFTR chaperone lumacaftor.
V69499	PF15	2892631-70-6	PF15 is a PROTAC linked by FLT3 kinase ligand and CRBN ligand.