UK-5099 (PF-1005023)

Catalog No.S5317 Batch:S531703

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Technical Data

Formula

C18H12N2O2
Molecular Weight 288.30 CAS No. 56396-35-1
Solubility (25°C)* In vitro DMSO 57 mg/mL (197.71 mM)
Water Insoluble
Ethanol Insoluble
In Vivo (Add solvents to the product individually and in order.)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description UK5099 (PF-1005023) is a potent inhibitor of the mitochondrial pyruvate carrier, inhibiting pyruvate transport across the plasma membrane of trypanosomes with Ki value of 49 μM.
Targets
mitochondrial pyruvate carrier
49 μM(Ki)
In vitro UK5099 covalently binds to Mpc and blocks pyruvate transport. UK5099 enhances aerobic glycolysis and decreases mitochondrial oxidative phosphorylation in LnCap cell in vitro, which is accompanied by increasing proportion of side population (SP) fraction, higher level of stemness markers expression and exhibiting high resistance to chemotherapy. UK5099 enhances stem-like phenotype of prostatic cancer cell through metabolic shift from oxidative phosphorylation to aerobic glycolysis. UK5099 suppresses proliferation and arrested LnCap cell cycle at G1/G0.
In Vivo UK-5099 slows the growth of patient-derived xenograft (PDX) tumours in mice without severe loss of animal body weight.

Protocol (from reference)

Cell Assay:[2]
  • Cell Lines

    C2C12 cells

  • Concentrations

    10 μM

  • Incubation Time

    24 hr

  • Method

    --
Animal Study:[4]
  • Animal Models

    Female C.B-17-Icr-scid-scidJcl mice implanted subcutaneously with patient-derived grafts

  • Dosages

    10 or 100 mg/kg/day

  • Administration

    p.o.

References

  • https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1136287/
  • https://www.sciencedirect.com/science/article/pii/S1097276514007813
  • https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4741963/
  • https://pubmed.ncbi.nlm.nih.gov/28408240/

Sellecks UK-5099 (PF-1005023) Has Been Cited by 20 Publications

Integrated molecular-phenotypic profiling reveals metabolic control of morphological variation in a stem-cell-based embryo model [ Cell Stem Cell, 2025, 32(5):759-777.e13] PubMed: 40245869
Hexokinase detachment from mitochondria drives the Warburg effect to support compartmentalized ATP production [ bioRxiv, 2025, 2025.02.07.637120] PubMed: 39975027
Hypoxia promotes metastasis by relieving miR-598-3p-restricted glycolysis in gastric cancer [ J Transl Med, 2024, 22(1):283] PubMed: 38491378
Inhibition of the mitochondrial pyruvate carrier simultaneously mitigates hyperinflammation and hyperglycemia in COVID-19 [ Sci Immunol, 2023, eadf0348] PubMed: 36821695
PASK links cellular energy metabolism with a mitotic self-renewal network to establish differentiation competence [ Elife, 2023, 12e81717] PubMed: 37052079
The mitochondrial pyruvate carrier complex potentiates the efficacy of proteasome inhibitors in multiple myeloma [ Blood Adv, 2023, 7(14):3485-3500] PubMed: 36920785
Perturbation of Copper Homeostasis Sensitizes Cancer Cells to Elevated Temperature [ Int J Mol Sci, 2023, 25(1)423] PubMed: 38203594
Generación de una plataforma para la producción de células CAR-T alogénicas: estudios de eficacia y seguridad [ University of Granada, 2023, ] PubMed: None
Copper induces cell death by targeting lipoylated TCA cycle proteins [ Science, 2022, 375(6586):1254-1261] PubMed: 35298263
A Heme-Binding Transcription Factor BACH1 Regulates Lactate Catabolism Suggesting a Combined Therapy for Triple-Negative Breast Cancer [ Cells, 2022, 11(7)1177] PubMed: 35406740

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.