VH-298

VH-298 is a highly potent inhibitor of the VHL:HIF-α interaction with a Kd value of 80 to 90 nM. VH-298 leads to HIF-α accumulation inside HeLa cells. VH-298 is an E3 ligase Ligand, and can be used for synthesis of PROTACs[1].

Product Specifications

CAS Number

[2097381-85-4]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

HIF/HIF Prolyl-Hydroxylase; Ligands for E3 Ligase

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease; PROTAC

Field of Research

Cancer; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/VH-298.html

Purity

99.83

Solubility

DMSO : ≥ 83.3 mg/mL

Smiles

O=C([C@H]1N(C([C@H](C(C)(C)C)NC(C2(CC2)C#N)=O)=O)C[C@H](O)C1)NCC3=CC=C(C4=C(C)N=CS4)C=C3

Molecular Formula

C27H33N5O4S

Molecular Weight

523.65

Precautions

H302, H315, H319, H335

References & Citations

[1]Frost J, et al. Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition. Nat Commun. 2016 Nov 4;7:13312.