UK-5099

UK-5099 (PF-1005023) is a potent inhibitor of the mitochondrial pyruvate carrier (MPC) . UK-5099 (PF-1005023) inhibits pyruvate-dependent O2 consumption with an IC50 of 50 nM.

Product Specifications

CAS Number

[56396-35-1]

Product Name Alternative

PF-1005023

UNSPSC

12352005

Hazard Statement

H302, H312, H332

Target

Mitochondrial Metabolism

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/uk-5099.html

Purity

99.95

Solubility

DMSO : ≥ 50 mg/mL

Smiles

O=C(O)/C(C#N)=C/C1=CN(C2=CC=CC=C2)C3=C1C=CC=C3

Molecular Formula

C18H12N2O2

Molecular Weight

288.30

Precautions

H302, H312, H332

References & Citations

[1]Halestrap AP. The mitochondrial pyruvate carrier. Kinetics and specificity for substrates and inhibitors. Biochem J. 1975 April; 148 (1) : 85-96.|[2]Wiemer EA, et al. The inhibition of pyruvate transport across the plasma membrane of the bloodstream form of Trypanosoma brucei and its metabolic implications. Biochem J. 1995 Dec 1;312 (Pt 2) :479-84.|[3]Hinoi E, et al. A molecular mechanism of pyruvate protection against cytotoxicity of reactive oxygen species in osteoblasts. Mol Pharmacol. 2006 Sep;70 (3) :925-35. Epub 2006 Jun 9.|[4]Patterson JN, et al. Mitochondrial metabolism of pyruvate is essential for regulating glucose-stimulated secretion. J Biol Chem. 2014 May 9;289 (19) :13335-46.|[5]Zhong Y, et al. Application of mitochondrial pyruvate carrier blocker UK5099 creates metabolic reprogram and greater stem-like properties in LnCap prostate cancer cells in vitro. Oncotarget. 2015 Nov 10;6 (35) :37758-69.