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    UK-5099 (PF-1005023)
    UK-5099 (PF-1005023)

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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  (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). 

    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, PF1005023, PF-1005023, PF 1005023
    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.  

    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.


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


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


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


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


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


    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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