Custom Premix Selecting "Custom Premix" option means that all of the beads you have chosen will be premixed in manufacturing before the kit is sent to you.
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.
Maryanoff, B.E., et al. 2011. ACS Med. Chem. Lett.2, 538.
数据表
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
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.
Form
Yellow solid
Intert gas (Yes/No)
Packaged under inert gas
Chemical formula
C₂₁H₂₆N₈S•2HCl
Structure formula
Purity
≥97% by HPLC
Solubility
DMSO (16.6 mg/ml)
Storage
Protect from light
-20°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity
Standard Handling
References
Maryanoff, B.E., et al. 2011. ACS Med. Chem. Lett.2, 538.
