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AdipoGen Life Sciences
UK 5099
45
CHF
CHF 45.00
In stock
AG-CR1-3691-M0011 mgCHF 45.00
AG-CR1-3691-M0055 mgCHF 100.00
AG-CR1-3691-M01010 mgCHF 150.00
| Product Details | |
|---|---|
| Synonyms | PF-1005023; 2-Cyano-3-(1-phenyl-1H-indol-3-yl)-2-propenoic acid |
| Product Type | Chemical |
| Properties | |
| Formula |
C18H12N2O2 |
| MW | 288.3 |
| CAS | 56396-35-1 |
| Purity Chemicals | ≥98% (HPLC) |
| Appearance | Off-white to yellow solid. |
| Solubility | Soluble in DMSO (20mg/ml) or DMF (10mg/ml). Sparingly soluble in aqueous buffers. |
| Identity | Determined by 1H-NMR |
| InChi Key | BIZNHCWFGNKBBZ-JLHYYAGUSA-N |
| Smiles | N#C/C(C(O)=O)=C\C1=CN(C2=CC=CC=C2)C3=CC=CC=C31 |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Handling Advice |
Keep cool and dry. Protect from light. |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
Description
- 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.
Product 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)
- ERRα-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)
- Lactate dehydrogenase activity drives hair follicle stem cell activation: A. Flores, et al.; Nat. Cell Biol. 19, 1017 (2017)
- E3 Ligase VHL Promotes Group 2 Innate Lymphoid Cell Maturation and Function via Glycolysis Inhibition and Induction of Interleukin-33 Receptor: Q. Li, et al.; Immunity 48, 258 (2018)
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