Home Metabolism Mitochondrial pyruvate carrier inhibitor UK 5099 For research use only.

UK 5099

Synonyms: PF-1005023

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

UK 5099 Chemical Structure

CAS No. 56396-35-1

Purity & Quality Control

UK 5099 Related Products

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
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].
Cell Research Cell lines C2C12 cells
Concentrations 10 μM
Incubation Time 24 hr
Method --
Experimental Result Images Methods Biomarkers Images PMID
Western blot GLUT1 / HK2 / LDHA / HIF-1α 27911865
In Vivo
In vivo UK-5099 slows the growth of patient-derived xenograft (PDX) tumors in mice without severe loss of animal body weight[4].
Animal Research 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.

Chemical Information & Solubility

Molecular Weight 288.30 Formula

C18H12N2O2
CAS No. 56396-35-1 SDF --
Smiles C1=CC=C(C=C1)N2C=C(C3=CC=CC=C32)C=C(C#N)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 57 mg/mL ( (197.71 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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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