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266785 Sigma-Aldrich

Diacylglycerol Kinase Inhibitor I - CAS 93076-89-2 - Calbiochem

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.

Synonym: 6-{2-{4-[(p-Fluorophenyl)phenylmethylene]-1-piperidinyl}ethyl}-7-methyl-5H-thiazolo(3,2-a)pyrimidine-5-one, R59022, Diacylglycerol Kinase Inhibitor I - CAS 93076-89-2 - Calbiochem, R59022, 6-{2-{4-[(p-Fluorophenyl)phenylmethylene]-1-piperidinyl}ethyl}-7-methyl-5H-thiazolo(3,2-a)pyrimidine-5-one

  • CAS Number 93076-89-2

  • Empirical Formula (Hill Notation) C27H26FN3OS

  • Molecular Weight 459.58

  •  MDL number MFCD00055114

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Properties

Related Categories Biochemicals and Reagents, D to K, Diacylglycerol kinase, Enzyme Inhibitors, Enzyme Inhibitors by Enzyme,
Quality Level   100
assay   ≥98% (HPLC)
form   solid
mfr. no.   Calbiochem®
storage condition   OK to freeze
storage conditions   +15C to +30C
color   white
solubility   ethanol: 12 mg/mL
  DMSO: 4 mg/mL
shipped in   ambient
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

Description

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.

Packaging

5 mg in Plastic ampoule

Biochem/physiol Actions

Cell permeable: no

Primary Target
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.

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