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UK-5099 (PF1005023) is a novel potent and specific/selective inhibitor of the mitochondrial pyruvate carrier (MPC), it acts by inhibiting pyruvate transport across the plasma membrane of trypanosomes (Ki = 49 μM). UK-5099 also inhibits pyruvate-dependent O2 consumption (IC50 = 50 nM).
| ln Vitro |
The inhibitory impact of alpha-cyano-4-hydroxycinnamate (Ki=17 mM) was found to be somewhat insensitive to the trypanopyruvate carrier; nevertheless, UK-5099 (Ki=49 microM) was able to inhibit it [2]. The monocarboxylate transporter (MCT) is likewise inhibited by UK-5099 [3]. At 150 μM, UK5099 decreased oxygen consumption below basal levels and in a dose-dependent manner prevented the glucose-stimulated increase in oxygen consumption. In 832/13 cells, UK5099 lowers ATP levels while raising ADP and AMP levels [4]. The cells treated with UK5099 exhibited a notably increased fraction of side population and expressed larger amounts of the stemness markers Oct3/4 and Nanog. Warburg effect studies should benefit greatly from using the UK5099 application as a paradigm [5].
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| ln Vivo |
In the intraperitoneal glucose tolerance test conducted on C57BLK mice, the MPC inhibitor UK5099 causes an increase in the glucose excursion [4].
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| References |
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| Molecular Formula |
C18H12N2O2
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| Molecular Weight |
288.30
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| Exact Mass |
288.089
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| CAS # |
56396-35-1
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| Related CAS # |
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| PubChem CID |
6438504
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
448.6±45.0 °C at 760 mmHg
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| Flash Point |
225.1±28.7 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.634
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| LogP |
4.6
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
22
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| Complexity |
499
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C=C1)N2C=C(C3=CC=CC=C32)/C=C(\C#N)/C(=O)O
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| InChi Key |
BIZNHCWFGNKBBZ-JLHYYAGUSA-N
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| 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+
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| Chemical Name |
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.67 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.67 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
 UK5099 blocked pyruvate transportation into mitochondrial in LnCap cellsin vitro.
Cells treated with UK5099 tended to be highly resistant to cisplatin. |
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 UK5099 inhibited cell proliferation and changed cell cycle.Oncotarget.2015 Nov 10;6(35):37758-69. |
 UK5099 attenuated mitochondrial function and increased glycolysis.Oncotarget.2015 Nov 10;6(35):37758-69. |
 UK5099 increased side population cells and stemness markers in LnCap cell.Oncotarget.2015 Nov 10;6(35):37758-69. |
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 Metabolic Reprogramming Resulting from Pharmacological Mpc Inhibition Is Distinct from Hypoxia or Complex I Inhibition.
Mpc Controls Oxidative Substrate Utilization in Myotubes.Molecular cell. 2014, 56(3):425-4 |
 An MPC inhibitor suppresses cancer cell growth.Molecular cell. 2014, 56(3):425-4 |
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