266785
Diacylglycerol Kinase Inhibitor I
The Diacylglycerol Kinase Inhibitor I, also referenced under CAS 93076-89-2, controls the biological activity of Diacylglycerol Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
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Synonym(s):
Diacylglycerol Kinase Inhibitor I, 6-{2-{4-[(p-Fluorophenyl)phenylmethylene]-1-piperidinyl}ethyl}-7-methyl-5H-thiazolo(3,2-a)pyrimidine-5-one, R59022, R59022, 6-{2-{4-[(p-Fluorophenyl)phenylmethylene]-1-piperidinyl}ethyl}-7-methyl-5H-thiazolo(3,2-a)pyrimidine-5-one
Empirical Formula (Hill Notation):
C27H26FN3OS
Recommended Products
Quality Level
Assay
≥98% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
color
white
solubility
ethanol: 12 mg/mL
DMSO: 4 mg/mL
shipped in
ambient
storage temp.
10-30°C
InChI
1S/C27H26FN3OS/c1-19-24(26(32)31-17-18-33-27(31)29-19)13-16-30-14-11-22(12-15-30)25(20-5-3-2-4-6-20)21-7-9-23(28)10-8-21/h2-10,17-18H,11-16H2,1H3
InChI key
MFVJXLPANKSLLD-UHFFFAOYSA-N
General description
Potentiates the activity of protein kinase C by inhibiting diacylglycerol metabolism. Inhibits diacylglycerol kinase (IC50 = 2.8 µM) without affecting phosphodiesterase or phosphatidylinositol kinase. Potentiates this effect in studies of signal-transducing inositol lipid metabolism. Inhibits human platelet DAG kinase in intact cells (IC50 = 3.6 µM) and in isolated membranes (IC50 = 6.7 µM). In porcine thymus cytosol it inhibits the 80 kDa DAG kinase (IC50 = 10 µM) but has no effect on the 150 kDa DAG kinase. Weak dopamine D2 and histamine H1 antagonist and strong serotonin-S2 antagonist.
Potentiates the activity of protein kinase C by inhibiting diacylglycerol metabolism. Inhibits diacylglycerol kinase (IC50 = 2.8 µM) without affecting phosphodiesterase or phosphatidylinositol kinase. Weak dopamine D2 and histamine H1 antagonist and strong serotonin S2 antagonist.
Biochem/physiol Actions
Cell permeable: no
Primary Target
Diacylglycerol Kinase
Diacylglycerol Kinase
Product does not compete with ATP.
Reversible: no
Warning
Toxicity: Irritant (B)
Reconstitution
Following reconstitution, store in the refrigerator (4°C). Stock solutions are stable for up to 3 months at 4°C.
Other Notes
Goin, M., et al. 1993. FEBS Lett. 316, 68.
Ohtsuka, T., et al. 1990. J. Biol. Chem.265, 15418.
de Chaffoy de Courcelles, D., et al. 1985. J. Biol. Chem.260, 15762.
Ohtsuka, T., et al. 1990. J. Biol. Chem.265, 15418.
de Chaffoy de Courcelles, D., et al. 1985. J. Biol. Chem.260, 15762.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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