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
V96893	PROTAC CDK2 Degrader-1	3024971-78-3	PROTAC CDK2 Degrader-1 (compound 41) is a PROTAC degrader targeting cyclin-dependent kinase 2 (CDK2).
V94071	PROTAC CDK9 degrader-9		PROTAC CDK9 degrader-9 (compound 29) is a highly efficient and selective CDK9 degrader developed based on PROTAC technology and can be used in anti-cancer research.
V92059	PROTAC CYP1B1 degrader-2	2836297-26-6	PROTAC CYP1B1 degrader-2 (compound PV2) is a von Hippel-Landau (VHL) E3 ligase-based CYP1B1 degrader with a DC50 value of 1.0 nM in A549/Taxol cells at 24 h.
V101889	PROTAC DYRK2 degrader 1		PROTAC DYRK2 degrader 1 (compound CP134) is a PROTAC degrader of DYRK2 (red: DYRK2 ligand, black: linker, blue: E3 ligase ligand).
V82335	PROTAC EED degrader-1	2639882-72-5	PROTAC EED degrader-1 is a von Hippel-Lindau-based PROTAC molecule targeting EED with a pKD of 9.02.
V82336	PROTAC EED degrader-2	2639882-69-0	PROTAC EED degrader-2 is a von Hippel-Lindau-based PROTAC molecule targeting EED with a pKD of 9.27.
V88029	PROTAC EGFR degrader 11	3034244-71-5	PROTAC EGFR degrader 11 (Compound B71) is a PROTAC degrader of epidermal growth factor receptor (EGFR) with a DC50 of <100 nM.
V69375	PROTAC EGFR degrader 4	2882845-50-1	PROTAC EGFR degrader 4 is a potent PROTAC targeting mutant EGFR.
V76594	PROTAC EGFR degrader 7 diTFA		PROTAC EGFR degrader 7 diTFA (compound 13b) is a specific CRBN-recruiting degrader of PROTAC EGFRL858R/T790M with DC50 of 13.2 nM.
V67667	PROTAC ER Degrader-10	2504911-58-2	PROTAC ER Degrader-10 is a potent PROTAC ER degrader for use in cancer research.
V93039	PROTAC ER Degrader-11	2846112-04-5	PROTAC ER Degrader-11 (Example 26-1) is a potent PROTAC ER degrader with an IC50 of 0.66 nM.
V104988	PROTAC ER Degrader-14	2504911-73-1	PROTAC ER Degrader-14 (Compound 86) is a PTORAC-type estrogen receptor/ERR degrader composed of the E3 ubiquitin ligase ligand (blue part) (S)-deoxythalidomide, the PROTAC Linker (black part) N-Boc-piperazine and the target protein ligand (red part) ER ligand-6.
V37549	PROTAC ERα Degrader-1		PROTAC ERα Degrader-1 contains a ubiquitin E3 ligase binding group, linker and target protein binding group.
V99663	PROTAC erf3a Degrader-1	3033871-19-8	PROTAC erf3a Degrader-1 (compound C63) is an orally active PROTAC erf3a degrader.
V99669	PROTAC erf3a Degrader-2	3033871-15-4	PROTAC erf3a Degrader-2 (compound C59) is an orally active PROTAC erf3a degrader that inhibits the expression levels of SRD5A3 and GSPT1 (eRF3a).
V67722	PROTAC ERRα Degrader-3	2306388-65-6	PROTAC ERRα Degrader-3 is a potent and specific ERRα degrader based on von Hippel-Lindau ligand.
V67656	PROTAC ERα Degrader-1	2417369-94-7	PROTAC ERα Degrader-1 contains a ubiquitin E3 ligase binding group, linker and target protein binding group.
V104985	PROTAC ERα Degrader-10	2421260-43-5	PROTAC ERα degrader-10 (Compound 160a) is an orally available ERα degrader with DC50 of 0.37-1.1 nM in MCF7, T47D, and CAMA-1 cells.
V67713	PROTAC ERα Degrader-4	2521299-80-7	PROTAC ERα Degrader-4 is a highly efficient and selective estrogen receptor (Estrogen Receptor/ERR) ERα subtype PROTACs containing OBHSAs, linker and E3 ligase ligands.
V89488	PROTAC ERα Degrader-7	3025781-93-2	PROTAC ERα Degrader-7 (compound i-320) is a potent estrogen receptor alpha (ERα) PROTAC degrader with a DC50 value of 0.000006 µM.