UK 5099

Catalog No.S5317 Synonyms: PF-1005023

For research use only.

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.

UK 5099 Chemical Structure

CAS No. 56396-35-1

Selleck's UK 5099 has been cited by 7 Publications

Purity & Quality Control

Choose Selective Mitochondrial pyruvate carrier Inhibitors

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 [1]
()
49 μM(Ki)
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].

Assay
Methods Test Index PMID
Western blot GLUT1 / HK2 / LDHA / HIF-1α 27911865
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 Research:[2]
  • Cell lines: C2C12 cells
  • Concentrations: 10 μM
  • Incubation Time: 24 hr
  • Method: --
Animal Research:[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.

Solubility (25°C)

In vitro

DMSO 57 mg/mL
(197.71 mM)
Water Insoluble
Ethanol '1 mg/mL

Chemical Information

Molecular Weight 288.30
Formula

C18H12N2O2

CAS No. 56396-35-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC=C(C=C1)N2C=C(C3=CC=CC=C32)C=C(C#N)C(=O)O

In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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