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.

• Synonyme(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
• Formule empirique (notation de Hill): C₂₇H₂₆FN₃OS
• Numéro CAS: 93076-89-2
• Poids moléculaire : 459.58
• Numéro MDL: MFCD00055114
• Code UNSPSC : 51111800
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥98% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze
• Couleur: white
• Solubilité: ethanol: 12 mg/mL; DMSO: 4 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: 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
• Clé InChI: MFVJXLPANKSLLD-UHFFFAOYSA-N

Description

Description générale

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.

Actions biochimiques/physiologiques

Cell permeable: no

Primary Target
Diacylglycerol Kinase

Product does not compete with ATP.

Reversible: no

Avertissement

Toxicity: Irritant (B)

Reconstitution

Following reconstitution, store in the refrigerator (4°C). Stock solutions are stable for up to 3 months at 4°C.

Autres remarques

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.

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable