UK-5099 is a specific and potent mitochondrial pyruvate carrier blocker (MCK blocker). The UK5099 treated cells showed significantly higher proportion of side population (SP) fraction and expressed higher levels of stemness markers Oct3/4 and Nanog. Chemosensitivity examinations revealed that the UK5099 treated cells became more resistant to chemotherapy compared to the non-treated cells. MPC blocker (UK5099) application may be an ideal model for Warburg effect studies
Chemical Formula: C18H12N2O2
Exact Mass: 288.0899
Molecular Weight: 288.306
Elemental Analysis: C, 74.99; H, 4.20; N, 9.72; O, 11.10
InChi Code: InChI=1S/C18H12N2O2/c19-11-13(18(21)22)10-14-12-20(15-6-2-1-3-7-15)17-9-5-4-8-16(14)17/h1-10,12H,(H,21,22)/b13-10+
Appearance: Yellow to light brown solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life:>2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The trypanosomal pyruvate carrier is found to be rather insensitive to inhibition by alpha-cyano-4-hydroxycinnamate (Ki=17 mM) but can be completely blocked by UK-5099 (Ki=49 microM). UK-5099 also inhibits the monocarboxylate transporter (MCT) . UK5099 significantly inhibits the glucose-stimulated rise in oxygen consumption in a dose-dependent manner and at 150 μM reduced oxygen consumption below basal levels. UK5099 reduces ATP levels and increases ADP and AMP levels in 832/13 cells. The UK5099 treated cells show significantly higher proportion of side population fraction and express higher levels of stemness markers Oct3/4 and Nanog. UK5099 application may be an ideal model for Warburg effect studies.
The MPC inhibitor UK5099 increases the glucose excursion seen during an intraperitoneal glucose tolerance test in C57BLK mice.
Jourdain P, Allaman I, Rothenfusser K, Fiumelli H, Marquet P, Magistretti PJ. L-Lactate protects neurons against excitotoxicity: implication of an ATP-mediated signaling cascade. Sci Rep. 2016 Feb 19;6:21250. doi: 10.1038/srep21250. PubMed PMID: 26893204; PubMed Central PMCID: PMC4759786.
Zhong Y, Li X, Yu D, Li X, Li Y, Long Y, Yuan Y, Ji Z, Zhang M, Wen JG, Nesland JM, Suo Z. Application of mitochondrial pyruvate carrier blocker UK5099 creates metabolic reprogram and greater stem-like properties in LnCap prostate cancer cells in vitro. Oncotarget. 2015 Nov 10;6(35):37758-69. doi: 10.18632/oncotarget.5386. PubMed PMID: 26413751; PubMed Central PMCID: PMC4741963.
Patterson JN, Cousteils K, Lou JW, Manning Fox JE, MacDonald PE, Joseph JW. Mitochondrial metabolism of pyruvate is essential for regulating glucose-stimulated insulin secretion. J Biol Chem. 2014 May 9;289(19):13335-46. doi: 10.1074/jbc.M113.521666. Epub 2014 Mar 27. PubMed PMID: 24675076; PubMed Central PMCID: PMC4036342.
Colca JR, McDonald WG, Cavey GS, Cole SL, Holewa DD, Brightwell-Conrad AS, Wolfe CL, Wheeler JS, Coulter KR, Kilkuskie PM, Gracheva E, Korshunova Y, Trusgnich M, Karr R, Wiley SE, Divakaruni AS, Murphy AN, Vigueira PA, Finck BN, Kletzien RF. Identification of a mitochondrial target of thiazolidinedione insulin sensitizers (mTOT)--relationship to newly identified mitochondrial pyruvate carrier proteins. PLoS One. 2013 May 15;8(5):e61551. doi: 10.1371/journal.pone.0061551. Print 2013. PubMed PMID: 23690925; PubMed Central PMCID: PMC3655167.
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