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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
PROTAC Her3 Degrader-8 V83035 PROTAC Her3 Degrader-8 2103331-95-7 PROTAC Her3 Degrader-8 (Compound PP2) is a PROTAC that can degrade Her3 proteins in in vitro experiments and cell experiments and may be utilized to study diseases regulated by HER family proteins.
PROTAC IAP binding moiety 1 V37561 PROTAC IAP binding moiety 1 PROTAC IAP binding moiety 1 is a warhead targeting IAP, used in PROTAC technology.
PROTAC IAP binding moiety 2 V37562 PROTAC IAP binding moiety 2 PROTAC IAP binding moiety 2 is a warhead targeting IAP, used in PROTAC technology.
PROTAC IRAK3 degrade-1 formic V76592 PROTAC IRAK3 degrade-1 formic PROTAC IRAK3 degrade-1 (compound 23) formic is a potent and specific IRAK3 degrader (IC50 = 5 nM).
PROTAC IRAK4 degrader-3 V75061 PROTAC IRAK4 degrader-3 2374122-43-5 PROTAC IRAK4 degrader-3 is a von Hippel-Lindau based IRAK4 degrader PROTAC.
PROTAC IRAK4 degrader-4 V75068 PROTAC IRAK4 degrader-4 2360528-45-4 PROTAC IRAK4 degrader-4 is a Cereblon-based IRAK4 degrader PROTAC.
PROTAC IRAK4 degrader-5 V75071 PROTAC IRAK4 degrader-5 2360530-61-4 PROTAC IRAK4 Degrader-5 is an IRAK4 degrader based on Cereblon.
PROTAC IRAK4 degrader-6 V75069 PROTAC IRAK4 degrader-6 2360530-72-7 PROTAC IRAK4 degrader-6 is a Cereblon-based IRAK4 degrader PROTAC.
PROTAC KRAS G12C degrader-1 V76591 PROTAC KRAS G12C degrader-1 PROTAC KRAS G12C degrader-1 is a KRASG12C PROTAC degrader based on Cereblon.
PROTAC MEK1 Degrader-1 V69816 PROTAC MEK1 Degrader-1 2671004-41-2 PROTAC MEK1 Degrader-1 is a PROTAC targeting MEK1 with pIC50 of 7.0.
PROTAC MLKL Degrader-1 V81233 PROTAC MLKL Degrader-1 PROTAC MLKL Degrader-1 (Compound 36) is a PROTAC targeted degrader of MLKL with Dmax >90%.
PROTAC NSD3 degrader-1 V81234 PROTAC NSD3 degrader-1 PROTAC NSD3 degrader-1 (compound 56) is a PROTAC that targets the nuclear receptor-binding SET domain protein NSD3.
PROTAC PARP1 degrader V37546 PROTAC PARP1 degrader 2369022-68-2 PROTAC PARP1 degrader is a PARP1 degrader based on MDM2 E3 ligand.
PROTAC RAF degrader 1 V74142 PROTAC RAF degrader 1 2413035-41-1 PROTAC RAF degrader 1 (compound 512) is a PROTAC RAF degrader.
PROTAC SOS1 degrader-4 V81235 PROTAC SOS1 degrader-4 PROTAC SOS1 degrader-4 (compound 10) is a potent SOS1 degrader.
PROTAC STAT3 degrader-2 V69154 PROTAC STAT3 degrader-2 2429877-78-9 PROTAC STAT3 degrader-2 is a selective PROTAC degrader of STAT3 protein with DC50 of 3.54 μM in Molm-16 cells.
PROTAC TG2 degrader-1 V77698 PROTAC TG2 degrader-1 PROTAC TG2 degrader-1 (Compound 11) is a von Hippel-Lindau (VHL)-based PROTAC targeting tissue transglutaminase (TG2) with a KD of 68.9 μM.
PROTAC TG2 degrader-2 V81236 PROTAC TG2 degrader-2 PROTAC TG2 degrader-2 (compound 7) is a selective and competitive degrader targeting Transglutaminase 2 (TG2) with a Kd > 100 μM.
PROTAC α-synuclein degrader 3 V70183 PROTAC α-synuclein degrader 3 2412273-77-7 PROTAC α-synuclein degrader 3 (compound 5) is a potent and specific PROTAC α-synuclein degrader.
PROTAC α-synuclein degrader 5 V70184 PROTAC α-synuclein degrader 5 2781922-42-5 PROTAC α-synuclein degrader 5 is a selective small molecule degrader (PROTAC) for α-synuclein aggregates, with DC50 of 7.51 μM and a maximum degradation rate of Dmax of 89%.
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