L-Prolinamide, 3-methyl-L-valyl-4-hydroxy-N-[(1S)-1-[4-(4-methyl-5-thiazolyl)phenyl]ethyl]-, hydrochloride (1:2), (4R)-

Uses

(S,R,S)-AHPC-Me dihydrochloride (VHL ligand 2 dihydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein[1]. (S,R,S)-AHPC-Me dihydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM[2].

Biological Activity

Me VH 032, amine is a derivative of the von Hippel-Lindau (VHL) ligand, VH 032 for use as a precursor to a PROTAC that hijacks VHL as the E3 ubiquitin ligase component. Me VH 032, amine is supplied with a primary amine functional handle, for ready conjugation to a linker/target protein ligand. Introduction of the methyl group at the benzylic position of VH 032 is associated with improved binding affinity.

IC 50

VHL

storage

Desiccate at RT

References

[1] Raina K, et al. PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer. Proc Natl Acad Sci U S A. 2016 Jun 28;113(26):7124-9. DOI:10.1073/pnas.1521738113