vhl ligand 2

(S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) is utilized in the synthesis of ARV-771, a potent BET protein degrader. It selectively degrades BET protein in castration-resistant cells with a DC50 <1 nM. Recognized as VHL ligand 2 hydrochloride, it serves as the VHL ligand from (S,R,S)-AHPC for recruiting von Hippel-Lindau (VHL) protein.

(S,R,S)-AHPC-Me dihydrochloride, also known as VHL ligand 2 dihydrochloride, is a chemical compound used in the synthesis of ARV-771. ARV-771 is a BET PROTAC degrader that relies on von Hippel-Landau (VHL) E3 ligase and exhibits potent degradation of BET proteins in castration-resistant prostate cancer (CRPC) cells, with a DC50 of less than 1 nM. This compound acts as the VHL ligand, specifically the (S,R,S)-AHPC-based VHL ligand, facilitating the recruitment of von Hippel-Lindau (VHL) protein.

(S,R,S)-AHPC-Me (E3 ligase Ligand 1A) (VHL ligand 2) is an (S,R,S)-AHPC-based VHL ligand used to recruit the von Hippel-Lindau (VHL) protein. It is utilized in the synthesis of ARV-771, a VHL E3 ligase-based BET PROTAC degrader that effectively degrades BET proteins in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM.

MAK683-CH2CH2COOH binds to EED (embryonic ectoderm development protein) and, together with a VHL ligand for the E3 ubiquitin ligase, has been used to design EED-Targeted PROTACs, specifically EED degrader-1 and PROTAC EED degrader-2 [1].

(S,R,S)-AHPC-PEG1-OTs is a chemically synthesized conjugate serving as a ligase ligand-linker for E3 ligase, incorporating the VHL ligand derived from (S,R,S)-AHPC and a 1-unit PEG linker. This compound is commonly utilized in PROTAC technology.

(S,R,S)-AHPC-PEG2-C4-Cl is a small molecule HaloPROTAC, comprising the (S,R,S)-AHPC based VHL ligand and a 2-unit PEG linker, that induces the degradation of GFP-HaloTag7 in cell-based assays[1].

(S,R,S)-AHPC-(C3-PEG)2-C6-Cl is a small molecule HaloPROTAC incorporating the (S,R,S)-AHPC-based VHL ligand and a 2-unit PEG linker, capable of inducing degradation of GFP-HaloTag7 in cell-based assays [1].

(S,R,S)-AHPC-PEG2-N3 (VHL Ligand-Linker Conjugates 6) is a synthesized E3 ligase ligand-linker conjugate comprising a (S,R,S)-AHPC-based VHL ligand and a 2-unit PEG linker.

(S,R,S)-AHPC-PEG2-NH2 hydrochloride (E3 ligase Ligand-Linker Conjugates 6) is a synthesized E3 ligase ligand-linker conjugate that includes the (S,R,S)-AHPC based VHL ligand and a 2-unit PEG linker used in the synthesis of PROTAC.

(S,R,S)-AHPC-PEG2-NH2 (VHL Ligand-Linker Conjugates 3) is a synthesized E3 ligase ligand-linker conjugate, incorporating the (S,R,S)-AHPC based VHL ligand and a 2-unit PEG linker used in PROTAC synthesis.

VH032-PEG5-C6-Cl (HaloPROTAC 2) is a small molecule that includes the VH032-based VHL ligand and a 5-unit PEG linker, capable of inducing the degradation of GFP-HaloTag7 in cell-based assays[1].

K-Ras ligand-Linker Conjugate 2 is a chemical compound that includes a ligand for K-Ras and a PROTAC linker, capable of recruiting E3 ligases like VHL, CRBN, MDM2, and IAP. It is utilized in synthesizing PROTAC K-Ras Degrader-1, a highly effective PROTAC K-Ras degrader with a degradation efficacy of ≥70% in SW1573 cells[1].

(S,R,S)-AHPC-Me-C10-Br is a chemically synthesized conjugate and ligand-linker for E3 ligase, consisting of MS432 for MEK1/2 inhibitors and a VHL E3 ligase linker.

(S,R,S)-AHPC-PEG2-NH2 dihydrochloride (VH032-linker 12) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC-based VHL ligand and a 2-unit PEG linker[1].

MEK ligand-2, a ligand for the target protein for PROTAC (Ligand for Target Protein for PROTAC), functions as an inhibitor for both MEK1 and MEK2. This compound plays a crucial role in MS934, which is a VHL-recruiting MEK1/2 PROTAC degrader.

(S,R,S)-AHPC-Me-12-((4-Bromobutyl)amino)dodecanamide comprises a VHL ligand for recruiting E3 ubiquitin ligases and a PROTAC linker. This compound is used in synthesizing PROTACs such as MS934. MS934 represents a novel and improved VHL-recruiting MEK1/2 PROTAC degrader.

RJS308 is a PROTAC degrader of cyclosporin A (cyclosporin A) with a DC50 of 284 nM. It exhibits antiviral activity by inhibiting the replication of HIV-1 and HCV. (Pink: ligand for target protein CypA ligand-2; Black: linker; Blue: ligand for E3 ligase VHL (S,R,S)-AHPC-Me)

AKTligand-2 (compound 5) is an AKT ligand. By using a linker, AKTligand-2 can be combined with the VHL ligand (S,R,S)-AHPC to synthesize PROTACMS21.

(S,R,S)-AHPC-Me-10-bromodecanoic acid is an E3 ligase ligand-linker conjugate composed of VHL ligand 2 and the linker 10-bromoheptanoic acid. This compound can be utilized in the synthesis of PROTACPI3Kδ degrader-1.

(S,S,S)-VH032 is a ligand for the E3 ligase (VHL) and is used in the synthesis of PROTACSGK3degrader-2.

Functionalized von-Hippel-Lindau protein ligand (VHL) for PROTAC research and development; incorporates an E3 ligase ligand plus a PEG linker ready for conjugation to a target protein ligand. Part of a range of functionalized tool molecules for PROTAC R&D. This product has been recently renamed. The previous name for this product was VH 032 - linker 2 PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license.

Functionalized von-Hippel-Lindau (VHL) protein ligand for PROTAC research and development; incorporates an E3 ligase ligand plus an alkyl linker ready for conjugation to a target protein ligand. Part of a range of functionalized tool molecules for PROTAC R&D. This product has been recently renamed. The previous name for this product was VH 032 phenol - linker 2 PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license.

MAK683-CH2CH2COOH, targeting embryonic ectoderm development protein (EED), alongside a VHL ligand for E3 ubiquitin ligase, contributes to the formulation of PROTAC EED degrader-1 and PROTAC EED degrader-2 [1].