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
V81221	PROTAC Bcl-xL degrader-1		PROTAC Bcl-xL degrader-1 is a PROTAC containing a Bcl-xL (Bcl-2 family member) ligand-binding group, a linker, and an IAP E3 ligase-binding group.
V76603	PROTAC Bcl-xL degrader-2		PROTAC Bcl-xL degrader-2 is a von Hippel-Lindau ligand-based degrader of Bcl-xL (a member of the Bcl-2 family) with IC50 of 0.6 nM.
V74130	PROTAC BRAF-V600E degrader-2	2417296-82-1	PROTAC BRAF-V600E degrader-2 (compound 12) is a potent BRAF-V600E degrader with Kd of 14.4 nM and 9.5 nM for BRAF and BRAF-V600E respectively.
V75497	PROTAC BRD2/BRD4 degrader-1	2570470-42-5	PROTAC BRD2/BRD4 degrader-1 (compound 15) is a highly efficient and selective degrader of BET proteins BRD4 and BRD2, linked by Cereblon ligand and BET ligand.
V81222	PROTAC BRD3/BRD4-L degrader-2		PROTAC BRD3/BRD4-L degrader-2 is a PROTAC molecule that can selectively degrade cellular BRD3 and BRD4-L with Kis of 16.91 and 2.8 nM respectively.
V81224	PROTAC BRD4 Degrader-22		PROTAC BRD4 Degrader-22 (Compd 44h) is a potent BRD4 PROTAC protein degrader with pDC50 (MOLT4, 24 h) of 9.2.
V81225	PROTAC BRD9 Degrader-7		PROTAC BRD9 Degrader-7 is an orally bioactive BRD9 selective degrader with DC50 of 1.02 nM.
V87977	PROTAC BRD9 Degrader-8		PROTAC BRD9 Degrader-8 (compound E5) is a PROTAC-based BRD9 degrader with a DC50 value of 16 pM.
V37560	PROTAC BRD9-binding moiety 1 hydrochloride		PROTAC BRD9-binding moiety 1 HCl is a structure that can bind to BRD9 and inhibits the activity of BRD9 based on PROTAC technology.
V69681	PROTAC BTK Degrader-1	2801715-13-7	PROTAC BTK Degrader-1 is a specific and orally bioactive PROTAC BTK degrader with IC50s of 34.51 nM and 64.56 nM for wild-type BTK and mutant BTK-481S, respectively.
V103773	PROTAC BTK Degrader-10	2988804-46-0	PROTAC BTK Degrader-10 (Example 1P) is a PROTAC degrader targeting BTK.
V103700	PROTAC BTK Degrader-11	2736508-94-2	PROTAC BTK Degrader-11 is a PROTAC degrader that can degrade BTK with a DC50 of 1.7 nM.
V105040	PROTAC BTK Degrader-12	2736508-65-7	PROTAC BTK Degrader-12 (Example 19) is a PROTAC-based BTK degrader (pink and black: BTK ligand and linker; black: linker; blue: VHL ligand).
V69700	PROTAC BTK Degrader-2	2250382-66-0	PROTAC BTK Degrader-2 is an effective BTK PROTAC protein degrader.
V69684	PROTAC BTK Degrader-3	2563861-90-3	PROTAC BTK Degrader-3 is a potent BTK PROTAC degrader with DC50 of 10.9 nM for BTK degradation in Mino cells.
V69694	PROTAC BTK Degrader-6	2767204-39-5	PROTAC BTK Degrader-6 (Compound 15) is a PROTAC BTK degrader (DC50= 3.18 nM).
V86936	PROTAC BTK Degrader-9		PROTAC BTK Degrader-9 (compound 23) is a PROTACs degrader that effectively targets BTK.
V94398	PROTAC c-Met degrader-1	3056647-52-7	PROTAC c-Met degrader-1 (compound Met-DD4) is an oral PROTAC degrader with a DC50 of 6.21 nM for c-Met.
V104984	PROTAC c-Met degrader-2	2254608-80-3	PROTAC c-Met Degrader-2 (PROTAC2) is a c-Met degrader based on PROTAC technology with a DC50 value of 50 nM (pink: Foretinib; black: linker; blue: CRBN ligand thalidomide-4-O-C2-NH2).
V97446	PROTAC Cbl-b-IN-1	3035210-39-7	PROTAC Cbl-b-IN-1 (compound 64) is a PROTAC targeting Cbl-b.