420640
Ketohexokinase Inhibitor
别名:
Ketohexokinase Inhibitor, N⁸-(Cyclopropylmethyl)-N⁴-(2-(methylthio)phenyl)-2-(1-piperazinyl)-pyrimido[5,4-d]pyrimidine-4,8-diamine, KHK Inhibitor
assay
≥97% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
yellow
solubility
DMSO: 16.6 mg/mL
shipped in
ambient
storage temp.
−20°C
Quality Level
General 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 = 12 nM in a transcreener ADP assay) and efficiently blocks fructose-1-phosphate secretion (IC50 ≤ 400 nM 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 >>10 µM). 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.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Maryanoff, B.E., et al. 2011. ACS Med. Chem. Lett.2, 538.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
Yanfen Cui et al.
Cancer research, 83(24), 4063-4079 (2023-09-22)
Excessive fructose intake is associated with the occurrence, progression, and poor prognosis of various tumors. A better understanding of the mechanisms underlying the functions of fructose in cancer could facilitate the development of better treatment and prevention strategies. In this
Sangmoo Jeong et al.
Cell metabolism, 33(1), 145-159 (2020-12-29)
A significant increase in dietary fructose consumption has been implicated as a potential driver of cancer. Metabolic adaptation of cancer cells to utilize fructose confers advantages for their malignant growth, but compelling therapeutic targets have not been identified. Here, we
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