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Technical Data
| Formula | C18H12N2O2 |
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| 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 | |||
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* <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.) |
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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. | ||
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| In vitro | UK5099 covalently binds to Mpc and blocks pyruvate transport[2]. 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[3]. | ||
| In vivo | UK-5099 slows the growth of patient-derived xenograft (PDX) tumors in mice without severe loss of animal body weight[4]. |
Protocol (from reference)
| Cell Assay:[2] |
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| Animal Study:[4] |
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References
Selleck's UK 5099 has been cited by 18 publications
| 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 |
| 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 |
| 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 |
| Energy metabolic shift contributes to the phenotype modulation of maturation stage ameloblasts [ Front Physiol, 2022, 13:1062042] | PubMed: 36523561 |
| Determination and pharmacokinetics study of UK-5099 in mouse plasma by LC-MS/MS [ BMC Vet Res, 2022, 18(1):145] | PubMed: 35443692 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
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.