(S,R,S)-AHPC-Me dihydrochloride, also known as VHLligand 2 dihydrochloride, is a chemical compound utilized in the synthesis of ARV-771. ARV-771, a BET PROTAC degrader relying on von Hippel-Landau (VHL) E3 ligase, demonstrates potent degradation of BET protein in castration-resistant prostate cancer (CRPC) cells, with a DC50 of less than 1 nM. This compound serves as the VHLligand, specifically the (S,R,S)-AHPC-based VHLligand, that facilitates the recruitment of von Hippel-Lindau (VHL) protein.
(S,R,S)-AHPC-PEG1-OTs is a chemically synthesized conjugate, functioning as an ligase ligand-linker for E3 ligase. It incorporates the VHLligand derived from (S,R,S)-AHPC and a 1-unit PEG linker. This synthesized compound is commonly employed in PROTAC technology.
(S,R,S)-AHPC-PEG2-C4-Cl is a small molecule HaloPROTAC that incorporates the (S,R,S)-AHPC based VHLligand and 2-unit PEG linker. (S,R,S)-AHPC-PEG2-C4-Cl is capable of inducing 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 VHLligand and a 2-unit PEG linker, capable of inducing degradation of GFP-HaloTag7 in cell-based assays [1].
VH032-PEG5-C6-Cl (HaloPROTAC 2) is a small molecule HaloPROTAC that incorporates the VH032 based VHLligand and 5-unit PEG linker. VH032-PEG5-C6-Cl is 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. This compound is capable of recruiting E3 ligases like VHL, CRBN, MDM2, and IAP. It is utilized in the synthesis of PROTAC K-Ras Degrader-1, which is a highly effective PROTAC K-Ras degrader with a degradation efficacy of ≥70% in SW1573 cells[1].
RJS308 是一种环孢菌素 A (cyclosporin A) 的PROTAC降解剂,具有284 nM的DC50。RJS308 抑制HIV-1和HCV的复制,从而展现出抗病毒活性。(Pink: ligand for target proteinCypA ligand-2; Black: linker; Blue: ligand for E3ligaseVHL(S,R,S)-AHPC-Me)
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.