[CAS NO. 56396-35-1]  UK 5099

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PRODUCTS SPECIFICATIONS [56396-35-1]

Store
Catalog
SLK-S5317
Brand
Selleck
CAS
56396-35-1

DESCRIPTION [56396-35-1]

Overview

MDLMFCD19443867
Molecular Weight288.30
Molecular FormulaC18H12N2O2
SMILESC(=C(C(O)=O)C#N)C1=CN(C=2C1=CC=CC2)C3=CC=CC=C3

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM3.4686 mL17.3430 mL34.6861 mL
5 mM0.6937 mL3.4686 mL6.9372 mL
10 mM0.3469 mL1.7343 mL3.4686 mL
50 mM0.0694 mL0.3469 mL0.6937 mL

Description

UK5099 (PF-1005023) is a potent inhibitor of the , 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. 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.


Synonyms

2-Propenoic acid, 2-cyano-3-(1-phenyl-1H-indol-3-yl)-
2-Cyano-3-(1-phenyl-1H-indol-3-yl)-2-propenoic acid
UK 5099
2-Cyano-3-(1-phenyl-1H-indol-3-yl)-acrylic acid