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UK-5099

Catalog No. T4441 CAS 56396-35-1

Synonyms: UK5099, UK 5099, PF-1005023

UK 5099 is a specific and potent inhibitor of MPC carrier activity [1]. It potently inhibits pyruvate-dependent oxygen consumption by rat heart mitochondria (IC50: 50 nM) [1].

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UK-5099, CAS 56396-35-1

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Purity: 98%

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Description	UK 5099 is a specific and potent inhibitor of MPC carrier activity [1]. It potently inhibits pyruvate-dependent oxygen consumption by rat heart mitochondria (IC50: 50 nM) [1].
Targets&IC50	MPC:50 nM
In vitro	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 μM)[2]. UK-5099 also inhibits the monocarboxylate transporter (MCT) [3]. UK5099 dose-dependently significantly inhibits the glucose-stimulated rise in oxygen consumption and at 150 μM reduced oxygen consumption below basal levels. UK5099 reduces ATP levels and increases ADP and AMP levels in 832/13 cells[4]. The UK5099 treated cells show a significantly higher proportion of side population fraction and express higher levels of stemness markers Oct3/4 and Nanog. The UK5099 application may be an ideal model for Warburg effect studies[5].
In vivo	UK5099 increases the glucose excursion seen during an intraperitoneal glucose tolerance test in C57BLK mice[4].
Cell Research	The 832/13 cell line derived from INS-1 rat insulinoma cells is used for experiments. Cell viability is measured using CellTiter Blue. The assay is based on the cellular reduction of resazurin to resorufin. The appearance of resorufin is monitored by fluorescence emission at 585 nm using a Spectramax M5 microplate reader with excitation at 555 nm. For UK5099-treated cells, cells are allowed to recover for 1 h before measuring cell viability. Data are expressed as -fold relative to no treatment or siCtrl[4].
Animal Research	C57BLK mice are fasted for 16 h prior to glucose challenge. UK5099 (32 μmol/kg of body weight) or DMSO in PBS is injected into the intraperitoneal cavity 30 min before injecting glucose (1.5 mg of glucose/g of body weight). Blood glucose levels are measured at 0, 10, 20, 30, 60, and 120 min after glucose injection[4].

Synonyms	UK5099, UK 5099, PF-1005023
Molecular Weight	288.3
Formula	C18H12N2O2
CAS No.	56396-35-1

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 28.8 mg/mL(100 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Halestrap A P. The mitochondrial pyruvate carrier. Kinetics and specificity for substrates and inhibitors[J]. Biochemical Journal, 1975, 148(1): 85-96. 2. Wiemer E A C, Michels P A M, Opperdoes F R. The inhibition of pyruvate transport across the plasma membrane of the bloodstream form of Trypanosoma brucei and its metabolic implications[J]. Biochemical Journal, 1995, 312(2): 479-484. 3. Hinoi E, Takarada T, Tsuchihashi Y, et al. A molecular mechanism of pyruvate protection against cytotoxicity of reactive oxygen species in osteoblasts[J]. Molecular pharmacology, 2006, 70(3): 925-935. 4. Patterson J N, Cousteils K, Lou J W, et al. Mitochondrial metabolism of pyruvate is essential for regulating glucose-stimulated insulin secretion[J]. Journal of Biological Chemistry, 2014, 289(19): 13335-13346. 5. Zhong Y, Li X, Yu D, et al. Application of mitochondrial pyruvate carrier blocker UK5099 creates metabolic reprogram and greater stem-like properties in LnCap prostate cancer cells in vitro[J]. Oncotarget, 2015, 6(35): 37758.

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

UK-5099 56396-35-1 Metabolism Others Mitochondrial Metabolism UK5099 UK 5099 PF 1005023 inhibit PF1005023 PF-1005023 Inhibitor inhibitor

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