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
V76637	PF15 TFA		PF15 TFA is a PROTAC linked by FLT3 kinase ligand and CRBN ligand.
V81119	phoBET1		phoBET1 is a photo-sealed PROTAC.
V81123	PhosTAC7		Similar to the ability of PROTACs to induce ternary complexes, PhosTAC7 focuses on recruiting Ser/Thr phosphatases to phosphorylated substrates to mediate their dephosphorylation.
V81140	PIK5-12d		PIK5-12d is a PROTAC PIKfyve degrader (DC50= 1.48 nM).
V83032	Pomalidomide-5'-PEG8-C2-COOH	2138440-78-3	Pomalidomide-5'-PEG8-C2-COOH is a ligand (for E3 ligase)-linker conjugate consisting of Pomalidomide and Linker.
V80369	Pomalidomide-5-C2-NH2 hydrochloride		Pomalidomide-5-C2-NH2 (HCl) is a linker conjugate used in the preparation /synthesis of E3 ligase ligand and PROTAC.
V83029	Pomalidomide-C3-NH2 hydrochloride	2154342-45-5	Pomalidomide-C3-NH2 HCl is a synthetic E3 ligase (e.g. CRBN) ligand-linker conjugate, containing Pomalidomide-based cereblon ligand and 1 linker, which may be utilized to prepare PROTAC molecules.
V81185	PPM-3		PPM-3 is an effective and selective PROTAC ERK5 degrader.
V81206	PRO-HD1		PRO-HD1 is a PROTAC HDAC6 degrader (IC50= 5.8 μM).
V81207	PRO-HD2		PRO-HD2 is a cell-specific PROTAC protein degrader of HDAC6.
V81208	PRO-HD3		PRO-HD3 is a cell-specific PROTAC protein degrader of HDAC6.
V37564	PROTAC ABL binding moiety 3		PROTAC ABL binding moiety 3 is a warhead targeting the BCR-ABL kinase for degradation via PROTAC technology.
V67595	PROTAC AR-V7 degrader-1	2767440-24-2	PROTAC AR-V7 degrader-1 (Compound 6) is an orally bioavailable and selective AR-V7 degrader with DC50 of 0.32 µM.
V74132	PROTAC B-Raf degrader 1	2364367-27-9	PROTAC B-Raf degrader 1 (compound 2) is a B-Raf PROTAC based on Cereblon ligand.
V37545	PROTAC B-Raf degrader 1		PROTAC B-Raf degrader 1 (compound 2) is a B-Raf PROTAC based on Cereblon ligand.
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.