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ProductsBack/UK 5099 [56396-35-1]
Chemical Structure
Chemical Structure
Chemical Structure

UK 5099 [56396-35-1]

Research Use Only
AG-CR1-3691
AdipoGen Life Sciences
CAS Number56396-35-1
DownloadDatasheet
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Product group Chemicals
Estimated Purity>95%
Molecular Weight288.3
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Overview

  • Supplier
    AdipoGen Life Sciences
  • Product Name
    UK 5099 [56396-35-1]
  • Delivery Days Customer
    10
  • CAS Number
    56396-35-1
  • Certification
    Research Use Only
  • Estimated Purity
    >95%
  • Hazard Information
    Non-hazardous,Warning
  • Molecular Formula
    C18H12N2O2
  • Molecular Weight
    288.3
  • Scientific Description
    Chemical. CAS: 56396-35-1. Formula: C18H12N2O2. MW: 288.3. . Potent and specific inhibitor of the mitochondrial pyruvate carrier (MPC), blocking pyruvate from entering the mitochondria, consequently promoting lactate production. Inhibitor of tricarboxylic acid (TCA) cycle. Plasma membrane monocarboxylate transporters (MCTs) inhibitor, but with Ki values some two or three orders of magnitude higher than those for the inhibition of the MPC. Inhibits mitochondrial lactate and pyruvate transport. Decreases glycolysis. Useful agent for immunometabolism research. - Potent and specific inhibitor of the mitochondrial pyruvate carrier (MPC), blocking pyruvate from entering the mitochondria, consequently promoting lactate production. Inhibitor of tricarboxylic acid (TCA) cycle. Plasma membrane monocarboxylate transporters (MCTs) inhibitor, but with Ki values some two or three orders of magnitude higher than those for the inhibition of the MPC. Inhibits mitochondrial lactate and pyruvate transport. Decreases glycolysis. Useful agent for immunometabolism research.
  • SMILES
    N#C/C(C(O)=O)=C\C1=CN(C2=CC=CC=C2)C3=CC=CC=C31
  • Storage Instruction
    2°C to 8°C,-20°C
  • UNSPSC
    12352200

References

  • The concentration of the mitochondrial pyruvate carrier in rat liver and heart mitochondria determined with alpha-cyano-beta-(1-phenylindol-3-yl)acrylate: M.S. Shearman & A.P. Halestrap; Biochem. J. 223, 673 (1984)
  • The inhibition of pyruvate transport across the plasma membrane of the bloodstream form of Trypanosoma brucei and its metabolic implications: E.A. Wiemer, et al.; Biochem. J. 312, 479 (1995)
  • Identification of the mitochondrial pyruvate carrier in Saccharomyces cerevisiae: J.C.W. Hildyard, et al.; Biochem, J. 374, 607 (2003)
  • A molecular mechanism of pyruvate protection against cytotoxicity of reactive oxygen species in osteoblasts: E. Hinoi, et al.; Mol. Pharmacol. 70, 925 (2006)
  • Thiazolidinediones are acute, specific inhibitors of the mitochondrial pyruvate carrier: A.S. Divakaruni, et al.; PNAS 110, 5422 (2013)
  • Mitochondrial metabolism of pyruvate is essential for regulating glucose-stimulated insulin secretion: J.N. Patterson, et al.; J. Biol. Chem. 289, 13335 (2014)
  • Application of mitochondrial pyruvate carrier blocker UK5099 creates metabolic reprogram and greater stem-like properties in LnCap prostate cancer cells in vitro: Y. Zhong, et al.; Oncotarget 6, 37758 (2015)
  • A guide to immunometabolism for immunologists: L.A. O'Neill, et al.; Nat. Rev. Immunol. 16, 553 (2016) (Review)
  • ERRalpha-Regulated Lactate Metabolism Contributes to Resistance to Targeted Therapies in Breast Cancer: S. Park, et al.; Cell Rep. 15, 323 (2016)
  • Inhibition of the mitochondrial pyruvate carrier protects from excitotoxic neuronal death: A.S. Divakaruni, et al.; J. Cell Biol. 216, 1091 (2017)