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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
MS9715 V80843 MS9715 MS9715 is a potent and specific NSD3 PROTAC.
MS98 V70220 MS98 2376137-31-2 MS98 is an effective and selective PROTAC AKT degrader.
MZ1 V3580 MZ1 1797406-69-9 MZ 1 (MZ1; MZ-1) is a novel and potentPROTAC-based degrader of BRD4protein with anticancer activity.
MZP-54 V3583 MZP-54 2010159-47-2 MZP-54 is a novel, potent and selective PROTAC-based degrader ofBRD3/4with aKdof 4 nM for Brd4BD2.
N-Boc-piperazine 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 .
NH2-PEG2-C6-Cl 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.
NH2-PEG2-CH2-Boc 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.
NJH-2-056 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.
NR-V04 V93763 NR-V04 2766608-52-8 NR-V04 is a PROTAC degrader of NR4A1 (red: NR4A1 inhibitor, black: linker, blue: E3 ligase ligand).
Nrf2 degrader 1 V87876 Nrf2 degrader 1 3025286-00-1 Nrf2 degrader 1 (compound 1) is a PROTAC Nrf2 degrader with anticancer activity.
OICR41114 V104643 OICR41114 OICR41114 (PROTAC 4) is a PROTAC degrader targeting WDR5.
P60-L3-VHL V96714 P60-L3-VHL P60-L3-VHL is a PROTAC-type Foxp3 degrader.
PCC16 chloride V94127 PCC16 chloride PCC16 chloride is a CRBN-based cp-PCC with an IC50 value of 102 nM for DHHC3 degradation.
PF15 V69499 PF15 2892631-70-6 PF15 is a PROTAC linked by FLT3 kinase ligand and CRBN ligand.
PF15 TFA V76637 PF15 TFA PF15 TFA is a PROTAC linked by FLT3 kinase ligand and CRBN ligand.
phoBET1 V81119 phoBET1 phoBET1 is a photo-sealed PROTAC.
PhosTAC7 V81123 PhosTAC7 3016307-75-5 Similar to the ability of PROTACs to induce ternary complexes, PhosTAC7 focuses on recruiting Ser/Thr phosphatases to phosphorylated substrates to mediate their dephosphorylation.
PIK5-12d V81140 PIK5-12d PIK5-12d is a PROTAC PIKfyve degrader (DC50= 1.48 nM).
Pomalidomide-5'-PEG8-C2-COOH V83032 Pomalidomide-5'-PEG8-C2-COOH 2138440-78-3 Pomalidomide-5'-PEG8-C2-COOH is a ligand (for E3 ligase)-linker conjugate consisting of Pomalidomide and Linker.
Pomalidomide-5-C2-NH2 hydrochloride V80369 Pomalidomide-5-C2-NH2 hydrochloride Pomalidomide-5-C2-NH2 (HCl) is a linker conjugate used in the preparation /synthesis of E3 ligase ligand and PROTAC.
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