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UK-5099 | Mitochondrial pyruvate transporter inhibitor

UK-5099 (56396-35-1) is a potent inhibitor of the mitochondrial pyruvate carrier (MPC).1 Rapidly increases glucose uptake in human monocytes.2 Attenuates mitochondrial oxidative phosphorylation and increases glycolysis creating greater stem-like properties in LnCap prostate cancer cells.3 Blocks the neuroprotective action of L-lactate or pyruvate during glutamate-induced excitotoxicity.4 Inhibits pyruvate transport across the plasma membrane of trypanosomes (Ki=49 μM).5

References/Citations

1) Shearman & Halestrap (1984), The concentration of the mitochondrial pyruvate carrier in rat liver and heart mitochondria determined with alpha-cyano-beta-(1-phenylindol-3-yl)acrylate; Biochem. J., 223 673
2) Divakaruni et al. (2013), Thiazolidinediones are acute, specific inhibitors of the mitochondrial pyruvate carrier.; Proc. Natl. Acad. Sci. USA, 110 5422
3) Zhong et al. (2015), Application of mitochondrial pyruvate carrier blocker UK5099 creates metabolic reprogram and greater stem-like properties in LnCap prostate cancer cells in vitro; Oncotarget, 6 37758
4) Jourdain et al. (2016), L-Lactate protects neurons against excitotoxicity: implication of an ATP-mediated signaling cascade; Sci. Rep., 6 21250
5) Wiemer et al. (1995), The inhibition of pyruvate transport across the plasma membrane of the bloodstream form of Trypanosoma brucei and its metabolic implications; Biochem. J., 312 479

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Focus Biomolecules supplier, chemical structure of UK-5099 | Mitochondrial pyruvate transporter inhibitor | CAS 56396-35-1

Catalog#  10-4748-0005

$70.00
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CAS:
56396-35-1
Catalog Number:
10-4748
Activity:
Mitochondrial pyruvate transporter inhibitor
Chemical Name:
2-Cyano-3-(1-phenyl-1H-indol-3-yl)-2-propenoic acid
Molecular Weight:
288.30
Molecular Formula:
C18H12N2O2
Solubility:
Soluble in DMSO (up to 30 mg/ml) or in Ethanol (up to 8 mg/ml)
Physical Properties:
Yellow solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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