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.

• 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
• CAS Number: 93076-89-2
• Molecular Weight: 459.58
• MDL number: MFCD00055114
• UNSPSC Code: 51111800
• NACRES: NA.77

Properties

• Quality Level: 100
• 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

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.

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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable