VH032

• CAT Number: I038028
• CAS Number: 1448188-62-2
• Molecular Formula: C24H32N4O4S
• Molecular Weight: 472.60
• Purity: ≥95%
• Synonyms: (2S,4R)-1-[(2S)-2-acetamido-3,3-dimethylbutanoyl]-4-hydroxy-N-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl]pyrrolidine-2-carboxamide
• InChI: InChI=1S/C24H32N4O4S/c1-14-20(33-13-26-14)17-8-6-16(7-9-17)11-25-22(31)19-10-18(30)12-28(19)23(32)21(24(3,4)5)27-15(2)29/h6-9,13,18-19,21,30H,10-12H2,1-5H3,(H,25,31)(H,27,29)/t18-,19+,21-/m1/s1
• InChIKey: GFVIEZBZIUKYOG-SVFBPWRDSA-N
• SMILES: CC1=C(SC=N1)C2=CC=C(C=C2)CNC(=O)C3CC(CN3C(=O)C(C(C)(C)C)NC(=O)C)O

VH032 (Cat No.: I038028) is a small-molecule ligand widely used in targeted protein degradation research, particularly in the design of PROTACs (proteolysis-targeting chimeras). It functions as a high-affinity ligand for the Von Hippel–Lindau (VHL) E3 ubiquitin ligase complex, enabling recruitment of VHL to mediate ubiquitination and subsequent proteasomal degradation of target proteins. VH032 derivatives are commonly employed as chemical handles to link target-binding ligands, providing a versatile tool for studying protein function and advancing drug discovery applications in disease research.

Reference

[1]. Michael Zengerle, et al. Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4. ACS Chem Biol. 2015 Aug 21;10(8):1770-7.
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[2]. Carles Galdeano, et al. Structure-guided design and optimization of small molecules targeting the protein-protein interaction between the von Hippel-Lindau (VHL) E3 ubiquitin ligase and the hypoxia inducible factor (HIF) alpha subunit with in vitro nanomolar affinities. J Med Chem. 2014 Oct 23;57(20):8657-63.
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[3]. Kwok-Ho Chan, et al. Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds. J Med Chem. 2018 Jan 25;61(2):504-513.
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