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PC1003 VH298 10mg

$195.00
  • Product Code: PC1003 VH298 10mg
  • Availability: In Stock
Tags: PROTAC

High-affinity inhibitor of E3 ubiquitin ligase VHL (Kd = 80-90 nM). Blocks interaction between VHL and HIF-α downstream of HIF-α hydroxylation, initiating hypoxic response. Results in time- and concentration-dependent accumulation of hydroxylated HIF-α, and upregulates mRNA and protein levels of HIF target genes. Cell permeable. 


Application


High-affinity inhibitor of VHL


Product Information



Purity:                         >98% 

MW:                          523.65

Formula:                          C27H33N5O4S

CAS No.                          2097381-85-4

Physical State:         Lyophilized white powder

Quantity:                   5mg; 10mg; 25 mg

Solubility:                         50 mg/mL in DMSO; 50 mg/mL in Ethanol

Storage:                         Store desiccated as supplied at -20°C for up to 3 years. Store solutions at -80°C for up to 6 months or -20°C for up to 1 month.


Documents



References


1.    Frost et al (2015) Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition. Nat.Commun. 7 13312 PMID: 27811928

2.    Soares et al (2018) Group-based optimization of potent and cell-active inhibitors of the von Hippel-Lindau (VHL) E3 ubiquitin ligase: structure-activity relationships leading to the chemical probe (2S,4R)-1-((S)-2-(1-Cyanocyclopropanecarboxamido)-3 J.Med.Chem. 61 599 PMID: 28853884


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