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
V88151	PROTAC TEAD degrader-1		PROTAC TEAD degrader-1 (Compound 27) is a PROTAC degrader of the transcription enhancer associated domain (TEAD).
V77698	PROTAC TG2 degrader-1	3033465-55-0	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.
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.
V88894	PROTAC TYK2 degrader-1	2770470-20-5	PROTAC TYK2 degrader-1 (CPD-155) is a PROTAC targeted degrader of TYK2 with Dmax >60%.
V92034	PROTAC VHL-type degrader-1	2821804-13-9	PROTAC VHL-type degrader-1 is a VHL-type PROTAC degrader.
V101158	PROTAC Vif degrader-1		PROTAC Vif degrader-1 (compound L15) is a Vif PROTAC degrader.
V97244	PROTAC YAP degrader-1		PROTAC YAP degrader-1 (compound YZ-6) is a PROTAC that targets YAP and also inhibits the nuclear localization of YAP.
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.
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%.
V69685	PTD10	2642231-19-2	PTD10 is a highly efficient PROTAC BTK degrader (DC50= 0.5 nM, KD: 2.28nM).
V97363	PTOTAC HSD17B13 degrader 1	3046195-01-8	PTOTAC HSD17B13 Degrader 1 (Compound 1) is a PROTAC targeting 17β-HSD 13 (HSD17B13).
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.
V96878	QS-57		QS-57 is a PROTAC targeting BRD4.
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.
V104620	SD-436	2497585-50-7	SD-436 is a highly selective and efficient STAT3 PROTAC degrader (DC50 is 0.5 μM) with IC50 of 19 nM, 270 nM, 360 nM, >10 μM and >10 μM for STAT3, STAT1, STAT4, STAT5 and STAT6, respectively.
V91783	SIAIS039	2570251-69-1	SIAIS039 is an orally active c-ros oncogene 1 (ROS1)-specific PROTAC with DC50 of 154.46 nM, 126.47 nM, and 143.69 nM in HCC78 cells, Ba/F3 expressing CD74-ROS1 fusion, and Ba/F3 expressing SDC4-ROS1 fusion, respectively.