UK-5099 | Mitochondrial pyruvate transporter inhibitor

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
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.
Shipping Code:
RT

Available Options

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5 mg$70.00
25 mg$280.00
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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 and 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

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
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

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