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UK-5099 (PF-1005023) Mitochondrial pyruvate carrier inhibitor

Name: UK-5099 (PF-1005023)
Brand: Selleck Chemicals
SKU: S5317
Availability: InStock
Rating: 5 (19 reviews)

Cat.No.S5317

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.

Chemical Structure

Molecular Weight: 288.30

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Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism
Other Mitochondrial pyruvate carrier Products	Azemiglitazone (MSDC-0602)

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (346.86 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.250mg/ml (4.34mM)	Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
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.
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.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.000mg/ml (13.87mM)	Taking the 1 mL working solution as an example, add 50 μL of 80 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
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.
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.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

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.

Chemical Information, Storage & Stability

Molecular Weight	288.30	Formula	C₁₈H₁₂N₂O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	56396-35-1	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	PF-1005023			Smiles	C1=CC=C(C=C1)N2C=C(C3=CC=CC=C32)C=C(C#N)C(=O)O

Mechanism of Action

Targets/IC₅₀/Ki	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) tumors in mice without severe loss of animal body weight.
References	[1] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1136287/ [2] https://www.sciencedirect.com/science/article/pii/S1097276514007813 [3] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4741963/ [4] https://pubmed.ncbi.nlm.nih.gov/28408240/

Applications

Methods	Biomarkers	Images	PMID
Western blot	GLUT1 / HK2 / LDHA / HIF-1α		27911865

Tech Support

Handling Instructions

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