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    UK-5099
    UK-5099

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0085
    CAS #: 56396-35-1Purity ≥98%

    Description: UK-5099 is a potent and specific inhibitor of the mitochondrial pyruvate carrier (MPC), it acts by inhibiting pyruvate transport across the plasma membrane of trypanosomes with Ki value of 49 μM. UK-5099 inhibits pyruvate-dependent O2 consumption with an IC50 of 50 nM. Cells treated with UK5099 showed significantly higher proportion of side population (SP) fraction and expressed higher levels of stemness markers Oct3/4 and Nanog. Meanwhile, chemosensitivity examinations revealed that the UK5099 treated cells became more resistant to chemotherapy compared to the non-treated cells.  

    References: . 1995 Dec 1; 312(Pt 2): 479–484;  2015 Nov 10;6(35):37758-69.

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    Molecular Weight (MW) 288.30
    Formula C18H12N2O2
    CAS No. 56396-35-1
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 57 mg/mL (197.7 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Chemical Name 2-cyano-3-(1-phenyl-1H-indol-3-yl)-2-propenoic acid
    Synonyms UK-5099, UK 5099, UK5099
    SMILES Code O=C(O)/C(C#N)=C/C1=CN(C2=CC=CC=C2)C3=C1C=CC=C3


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    In Vitro

    In vitro activity: UK-5099 is a potent and specific inhibitor of the mitochondrial pyruvate carrier (MPC), it acts by inhibiting pyruvate transport across the plasma membrane of trypanosomes with Ki value of 49 μM. UK-5099 inhibits pyruvate-dependent O2 consumption with an IC50 of 50 nM. Cells treated with UK5099 showed significantly higher proportion of side population (SP) fraction and expressed higher levels of stemness markers Oct3/4 and Nanog. Meanwhile, chemosensitivity examinations revealed that the UK5099 treated cells became more resistant to chemotherapy compared to the non-treated cells.  


    Kinase Assay:


    Cell Assay: 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. 

    In VivoUK-5099 suppresses the growth of patient-derived xenograft (PDX) tumors in mice without severe loss of animal body weight.
    Animal model Female C.B-17-Icr-scid-scidJcl mice implanted subcutaneously with patient-derived grafts
    Formulation & Dosage Dissolved in 0.5% methylcellulose; 10 or 100 mg/kg/day; oral
    References  2015 Nov 10;6(35):37758-69;  2017 May;19:31-38. doi


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    UK-5099


    UK5099 blocked pyruvate transportation into mitochondrial in LnCap cells in vitro. 


    UK-5099

    Cells treated with UK5099 tended to be highly resistant to cisplatin. 

     UK-5099


    UK5099 inhibited cell proliferation and changed cell cycle.  2015 Nov 10;6(35):37758-69. 

     UK-5099


    UK5099 attenuated mitochondrial function and increased glycolysis.  2015 Nov 10;6(35):37758-69. 

     UK-5099


    UK5099 increased side population cells and stemness markers in LnCap cell.  2015 Nov 10;6(35):37758-69. 

     UK-5099


    Metabolic Reprogramming Resulting from Pharmacological Mpc Inhibition Is Distinct from Hypoxia or Complex I Inhibition.


    UK-5099

    Mpc Controls Oxidative Substrate Utilization in Myotubes. Molecular cell. 2014, 56(3):425-4

     UK-5099


    An MPC inhibitor suppresses cancer cell growth. Molecular cell. 2014, 56(3):425-4


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