266788
Diacylglycerol Kinase Inhibitor II
The Diacylglycerol Kinase Inhibitor II, also referenced under CAS 120166-69-0, controls the biological activity of Diacylglycerol KInase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
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Diacylglycerol Kinase Inhibitor II, R59949, 3-{2-[4-[ bis-(4-Fluorophenyl)methylene]-1-piperidinyl]ethyl}-2,3-dihydro-2-thioxo-4(1H)quinazolinone, DGK Inhibitor II, R59949, 3-{2-[4-[bis-(4-Fluorophenyl)methylene]-1-piperidinyl]ethyl}-2,3-dihydro-2-thioxo-4(1H)quinazolinone, DGK Inhibitor II
C28H25F2N3OS
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Quality Level
Assay
≥98% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
color
white
solubility
DMSO: 12.5 mg/mL
shipped in
ambient
storage temp.
10-30°C
InChI
1S/C28H25F2N3OS/c29-22-9-5-19(6-10-22)26(20-7-11-23(30)12-8-20)21-13-15-32(16-14-21)17-18-33-27(34)24-3-1-2-4-25(24)31-28(33)35/h1-12H,13-18H2,(H,31,35)
InChI key
ZCNBZFRECRPCKU-UHFFFAOYSA-N
General description
Inhibitor useful for elucidating roles of protein kinase C. Inhibits diacylglycerol (DAG) kinase in isolated platelet membranes (IC50 = 300 nM) and in intact platelets (IC50 = 120 nM). A more potent analog of DAG kinase inhibitor I.
Inhibits diacylglycerol kinase in isolated platelet membranes (IC50 = 300 nM) and in intact platelets (IC50 = 120 nM) by binding to the catalytic domain. A more potent analog of diacylglycerol kinase inhibitor I (Cat. No. 266785).
Biochem/physiol Actions
Cell permeable: no
Product does not compete with ATP.
Reversible: no
Target IC50: 300 nM and 120 nM against diacylglycerol kinase in isolated platelet membranes and in intact platelets, respectively
Warning
Toxicity: Irritant (B)
Reconstitution
Following reconstitution, aliquot, flush with an inert gas and freeze at -20°C. Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Jiang, Y., et al. 2000. Biochem. Pharmacol. 59, 763.
Jones, D.R., et al. 1999. J. Biol. Chem.274, 16846.
Rodriguez-Linares, B., et al. 1991. Biochem. Pharmacol. 41, 835.
de Chaffoy de Courcelles, D., et al. 1989. J. Biol. Chem.264, 3274.
Jones, D.R., et al. 1999. J. Biol. Chem.274, 16846.
Rodriguez-Linares, B., et al. 1991. Biochem. Pharmacol. 41, 835.
de Chaffoy de Courcelles, D., et al. 1989. J. Biol. Chem.264, 3274.
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)
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Immunology, 105(4), 391-398 (2002-05-03)
The diacylglycerol kinases (DGK) form a family of isoenzymes that catalyse the conversion of diacylglycerol (DAG) to phosphatidic acid (PA), both powerful second messengers in the cell. DGKalpha is expressed in brain, peripheral T cells and thymocytes and has been
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