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MilliporeSigma™ Calbiochem™ Ketohexokinase Inhibitor

Catalog No. 42064010MG Shop All MilliporeSigma Products
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42-064-010MG 10 mg
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Description

An orally bioavailable pyrimidinopyrimidine compound that acts as a potent, reversible and ATP-competitive inhibitor of human hepatic KHK activity (KHK-C isoform; IC50 = 12nM in a transcreener ADP assay) and efficiently blocks fructose-1-phosphate secretion (IC50 ≤ 400nM in HepG2

An orally bioavailable pyrimidinopyrimidine compound that acts as a potent, reversible and ATP-competitive inhibitor of human hepatic KHK activity (KHK-C isoform; IC50 = 12nM in a transcreener ADP assay) and efficiently blocks fructose-1-phosphate secretion (IC50 ≤ 400nM in HepG2 cells). Displays ∽50-fold lower potency towards metabolic kinases, namely, ribokinase, hexokinase and adenosine kinase, and minimal binding affinities to diverse receptors and ion-channels, and excellent selectivity among a panel of 31-kinases including Akt1, AMPK, CaMKI/II, InsR, IRAK4, PKA and PKCθ (IC50 >> 10μM). Shown to minimally affect the activities of human cytochrome p450 isozymes (1A2, 2C19, 2D6, 2C9 and 3A4), and exhibit high volume of distribution and high rate of clearance in rats.
TRUSTED_SUSTAINABILITY

Specifications

Color Yellow
Description 97% by HPLC
Molecular Formula C21H26N8S·2HCl
Formula Weight 495.5g/mol
Solubility DMSO
Content And Storage Protect from light
Form Solid
Quantity 10 mg
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