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
V69685	PTD10	2642231-19-2	PTD10 is a highly efficient PROTAC BTK degrader (DC50= 0.5 nM, KD: 2.28nM).
V76575	PZ703b hydrochloride		PZ703b HCl is a Bcl-xl PROTAC degrader that can cause apoptosis and inhibit cancer cell proliferation/growth.
V76574	PZ703b TFA		PZ703b TFA is a Bcl-xl PROTAC degrader that can cause apoptosis, inhibit cancer cell proliferation/growth, and may be used in bladder cancer research.
V37563	RAR ligand 1 (Ch55-O-C3-carbaldehyde)		RAR ligand 1 (Ch55-O-C3-carbaldehyde) is a warhead targeting RAR for degradation, used in PROTAC technology.
V83052	Roridin L2	85124-22-7	Roridin L2, a fungal metabolite and biosynthetic precursor of Satratoxin G, has little toxic activity in vitro or in vivo.
V81354	SA-PA		SA-PA is an intracellular self-assembling PROTAC based on azide and alkynes.
V81375	SA-VA		SA-VA is an intracellular self-assembling PROTAC based on azide and alkynes.
V76516	SIAIS100 TFA		SIAIS100 TFA is a potent BCR-ABL PROTAC degrader with DC50 of 2.7 nM.
V76515	SIAIS164018 hydrochloride		SIAIS164018 HCl is a PROTAC ALK and EGFR degrader with IC50s of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively.
V75492	SIM1	2719051-84-8	SIM1 is a potent von Hippel-Lindau (VHL)-based PROTAC that degrades all BET family members with preferential degradation of BRD2 (IC50=1.1 nM; Kd=186 nM).
V76510	SJ1008030 formic		SJ1008030 (compound 8) formic is a JAK2 PROTAC that selectively degrades JAK2.
V76509	SJ1008030 TFA		SJ1008030 (compound 8) TFA is a JAK2 PROTAC that selectively degrades JAK2.
V69670	SJF620 hydrochloride	2821938-05-8	SJF620 HCl is a PROTAC linked to Cereblon ligand and Btk ligand with DC50 of 7.9 nM.
V76502	SMD-3040		SMD-3040 is a potent and specific SMARCA2 degrader.
V83043	SN52	1071173-56-2	SN52 is a potent, competitive, cell-permeable (penetrable) inhibitor of NF-κB2.
V81422	SP27		SP27 is a PROTAC that selectively degrades PLK4 with DC50 of 19.5 nM.
V69149	STAT3 degrader-2	2497583-03-4	STAT3 degrader-2 is a PROTAC-based STAT3 degrader.
V37538	TD-428		TD-428 is a PROTAC protein degrader linked by Cereblon ligand and BRD4 ligand.
V75506	TD-428	2334525-50-5	TD-428 is a PROTAC linked by Cereblon ligand and BRD4 ligand.
V3487	THAL-SNS-032	2139287-33-3	THAL-SNS-032 is a novel, potent and selective CDK9 degrader baed on PROTAC technology to degrade CDK9.