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
V87978	PROTAC ERα Degrader-8	3025533-68-7	PROTAC ERα Degrader-8 (compound ii-56) is a potent Erα PROTAC degrader with a DC50 of 0.
V37539	PROTAC ER α Degrader-1		PROTAC ER α Degrader-1 is a PROTAC degrader
V81229	PROTAC EZH2 Degrader-2		PROTAC EZH2 Degrader-2 (compound E-3P-MDM2), an EZH2 inhibitor, is a PROTAC consisting of Tazemetostat (EPZ6438) and an E3 ligase system ligand.
V88028	PROTAC FAK degrader 2		PROTAC FAK degrader 2 (Compound F2) is a PROTAC degrader of focal adhesion kinase (FAK) with DC50 of 27.72 and 60.1 nM for total FAK and phosphorylated p-FAK, respectively.
V88049	PROTAC FLT3/CDKs degrader-1		PROTAC FLT3/CDKs degrader-1 (Compound C3) is a degrader of cyclin-dependent kinases (DC50 of CDK2 is 18.73 nM) and FMS-like tyrosine kinase 3 (FLT3).
V81231	PROTAC GDI2 Degrader-1		PROTAC GDI2 Degrader-1 (Compound 21) is an effective PROTAC GDI2 degrader.
V96902	PROTAC GSPT1 degrader-1	3034310-17-0	PROTAC GSPT1 Degrader-1 (Compound F) is a PROTAC degrader that degrades G1 to S phase transition protein 1 (GSPT1) with degradation rates of 95% (1 μM) GSPT1 and 86% (0.1 μM).
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.
V87080	PROTAC HPK1 Degrader-1	3034182-97-0	PROTAC HPK1 Degrader-1 (Compound B1) is a potent HPK1 degrader with a DC50 value of 1.8 nM.
V87082	PROTAC HPK1 Degrader-2	2893885-31-7	PROTAC HPK1 Degrader-2 (compound 3) is a PROTAC degrader of HPK1 with a DC50 of 23 nM in human PBMC.
V97306	PROTAC HPK1 Degrader-3		PROTAC PD-L1 degrader-2 (compound C3) is an orally active PROTAC targeting HPK1 (DC50 = 21.26 nM).
V37561	PROTAC IAP binding moiety 1		PROTAC IAP binding moiety 1 is a warhead targeting IAP, used in PROTAC technology.
V37562	PROTAC IAP binding moiety 2		PROTAC IAP binding moiety 2 is a warhead targeting IAP, used in PROTAC technology.
V76592	PROTAC IRAK3 degrade-1 formic		PROTAC IRAK3 degrade-1 (compound 23) formic is a potent and specific IRAK3 degrader (IC50 = 5 nM).
V86888	PROTAC IRAK4 degrader-10	3033829-95-4	PROTAC IRAK4 degrader-10 (compound 10) is an orally active Cereblon ligand-based PROTAC that induces a maximum degradation rate of 95.94% for IRAK4 in HEK293 cells with a DC50 value of 7.68 nM (Structural notes: (blue: Cereblon ligand, black: linker; pink: IRAK4 inhibitor).
V86887	PROTAC IRAK4 degrader-11		PROTAC IRAK4 degrader-11 (compound 15) is a Cereblon ligand-based PROTAC that induces a maximum degradation rate of 96.25% for IRAK4 in HEK293 cells with a DC50 value of 2.29 nM (Structural notes: (blue: Cereblon ligand, black: linker; pink: IRAK4 inhibitor).
V93346	PROTAC IRAK4 degrader-12	2919995-09-6	PROTAC IRAK4 degrader-12 is a Cereblon ligand-based PROTAC that induced a maximum degradation rate of IRAK4 of 108.46% in K562 cells with an IC50 value of 4.87 nM.
V75061	PROTAC IRAK4 degrader-3	2374122-43-5	PROTAC IRAK4 degrader-3 is a von Hippel-Lindau based IRAK4 degrader PROTAC.
V75068	PROTAC IRAK4 degrader-4	2360528-45-4	PROTAC IRAK4 degrader-4 is a Cereblon-based IRAK4 degrader PROTAC.
V75071	PROTAC IRAK4 degrader-5	2360530-61-4	PROTAC IRAK4 Degrader-5 is an IRAK4 degrader based on Cereblon.