VHL-IN-1

VHL-IN-1 (compound 30) is a ubiquitin E3 ligase von Hippel-Lindau (VHL) inhibitor (dissociation constant Kd=37 nM) that stabilizes and induces HIF-1α transcriptional activity. VHL-IN-1 has potential as a HIF-1α stabilizer and degrader of proteolytically targeted chimeras (PROTACs) [1].

Product Specifications

CAS Number

[3033117-53-9]

UNSPSC

12352005

Target

HIF/HIF Prolyl-Hydroxylase; Ligands for E3 Ligase

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease; PROTAC

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/vhl-in-1.html

Purity

99.84

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C([C@H]1N(C([C@@H](NC(C2(F)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)N[C@H](C3=CC=C(C4=C(C)N=CS4)C=C3C)C

Molecular Formula

C28H37FN4O4S

Molecular Weight

544.68

References & Citations

[1]Vu LP, et al. Expanding the Structural Diversity at the Phenylene Core of Ligands for the von Hippel-Lindau E3 Ubiquitin Ligase: Development of Highly Potent Hypoxia-Inducible Factor-1α Stabilizers. J Med Chem. 2023 Sep 14.. .