me 1

(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.

Desmorpholinyl Navitoclax-NH-Me (Desmorpholinyl ABT-263-NH-Me) is a Bcl-xL inhibitor, which can be employed alongside a CRBN ligand to synthesize XZ739, a PROTAC BCL-XL degrader [1] [2].

(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.

N-Me-N-bis(PEG2-propargyl) is a PEG-based linker used in the synthesis of PROTACs [1].

N-Me-N-bis(PEG4-C2-Boc) is a PROTAC linker characterized by alkyl and ether functionalities, essential for PROTAC synthesis. [1]

NO2-SPP-sulfo-Me is a cleavable linker used in the synthesis of antibody-drug conjugates (ADC)[1].

GNF5-amido-Me, the moiety based on GNF5 (ABL inhibitor),binds through a linker to the IAP ligand forming SNIPER[1].

Bestatin-amido-Me, a derivative of Bestatin, acts as an IAP ligand and interacts with ABL inhibitor through a linker to produce SNIPER[1].

NH2-Ph-C4-acid-NH2-Me (PROTAC Linker 31) is an alkyl chain-based compound used in the synthesis of PROTACs [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-Me-C10-NH2 is a synthesized chemical compound incorporating a VHL ligand and a linker, serving as an E3 ligase ligand-linker conjugate. It is utilized in PROTAC MS432[1].

(S,R,S)-AHPC-Me-C5-COOH is a synthetic E3 ligase ligand-linker conjugate composed of a VHL ligand and a linker, used in PROTAC DT2216[1].

(S,R,S)-AHPC-Me-C7 ester is an E3 ligase ligand-linker conjugate used to synthesize BCL-XL PROTAC degraders[1].

THP-PEG4-Pyrrolidine(N-Me)-CH2OH, a PEG-based PROTAC linker, aids in the synthesis of PROTAC K-Ras Degrader-1[1].

Me-SJ46411 is an E3 ubiquitin ligase ligand used in the synthesis of PROTAC molecules. For instance, when combined with the PROTAC linker Boc-Piperazine-OH and the target protein ligand (+)-JQ-1, Me-SJ46411 can be employed to create the selective BRD3 PROTAC degrader SJ46420.

Me-(S,R,S)-AHPC-PEG2-OTs is a conjugate of E3 ligase ligand and linker (E3 Ligase Ligand-Linker Conjugates) utilized in the synthesis of PROTAC HIF-1α degrader-1.

SMD-1087 is a selective PROTAC targeting SMARCA2 with a DC50 of 8 nM and a maximum degradation (Dmax) of 89%, while its DC50 for SMARCA4 exceeds 1 μM. The compound is composed of an E3 ligase ligand, (S,R,S)-AHPC-Me [blue part], a target protein ligand SMI-1074 [red part], and a PROTAC linker, (1r,4r)-tert-Butyl 4-(bromomethyl)cyclohexanecarboxylate [black part]. Notably, its target protein ligand plus linker section corresponds to the SMARCA2 Ligand-Linker Conjugate-1.

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)

(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.