(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.
VH032-PEG3-acetylene is a synthesized conjugate compound consisting of a VH032-based VHLligand and a linker, designed for use in PROTAC technology as an E3 ligase ligand-linker conjugate[1].
BRD7-IN-1 free base, a modified derivative of BI7273 (BRD7 9 inhibitor), interacts with a VHLligand through a linker, constituting the PROTAC VZ185 (targeting BRD7 9 with DC50 values of 4.5 and 1.8 nM, respectively)[1].
(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.
VHLLigand-Linker Conjugates 15 is a chemical compound that combines a VHLligand, which targets the E3 ubiquitin ligase, with a PROTAC linker. It is specifically designed for the creation of PROTACs[1].
(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-C6-PEG3-C4-Cl is a small molecule HaloPROTAC that incorporates the (S,R,S)-AHPC based VHLligand and 3-unit PEG linker. (S,R,S)-AHPC-C6-PEG3-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].
(S,R,S)-AHPC-PEG3-NH2 is a synthetic conjugate of an E3 ligase ligand-linker, incorporating the (S,R,S)-AHPC VHLligand and a 3-unit PEG linker, which are utilized in PROTAC technology.
(S,R,S)-AHPC-PEG6-C4-Cl is a small molecule HaloPROTAC that incorporates the (S,R,S)-AHPC based VHLligand and 6-unit PEG linker. (S,R,S)-AHPC-PEG6-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays[1].
EED226-COOH, derived from EED226, serves as a ligand targeting the EED protein for PROTAC applications. It attaches to a VHLligand through a linker, culminating in the formation of UNC6852, which specifically degrades PRC2[1].