1. Metabolic Enzyme/Protease
  2. Mitochondrial Metabolism
  3. UK-5099

UK-5099 (Synonyms: PF-1005023)

Cat. No.: HY-15475 Purity: 99.57%
Handling Instructions

UK-5099 is a potent inhibitor of the mitochondrial pyruvate carrier (MPC). UK-5099 ihibits pyruvate-dependent O2 consumption with an IC50 of 50 nM.

For research use only. We do not sell to patients.

UK-5099 Chemical Structure

UK-5099 Chemical Structure

CAS No. : 56396-35-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 92 In-stock
Estimated Time of Arrival: December 31
5 mg USD 84 In-stock
Estimated Time of Arrival: December 31
10 mg USD 120 In-stock
Estimated Time of Arrival: December 31
50 mg USD 410 In-stock
Estimated Time of Arrival: December 31
100 mg USD 640 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

UK-5099 is a potent inhibitor of the mitochondrial pyruvate carrier (MPC). UK-5099 ihibits pyruvate-dependent O2 consumption with an IC50 of 50 nM.

IC50 & Target

IC50: 50 nM (MPC)[1]

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 microM)[2]. UK-5099 also inhibits the monocarboxylate transporter (MCT) [3]. 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[4]. 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[5].

In Vivo

The MPC inhibitor UK5099 increases the glucose excursion seen during an intraperitoneal glucose tolerance test in C57BLK mice[4].

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (173.43 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4686 mL 17.3430 mL 34.6861 mL
5 mM 0.6937 mL 3.4686 mL 6.9372 mL
10 mM 0.3469 mL 1.7343 mL 3.4686 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (8.67 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (8.67 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[4]

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 cellular reduction of resazurin to resorufin. 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[4]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

288.30

Formula

C₁₈H₁₂N₂O₂

CAS No.

56396-35-1

SMILES

O=C(O)/C(C#N)=C/C1=CN(C2=CC=CC=C2)C3=C1C=CC=C3

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
UK-5099
Cat. No.:
HY-15475
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UK-5099

Cat. No.: HY-15475