DIACYLGLYCEROL KINASE INHIBITOR I Struktur

6-(2-(4-((4-Fluorphenyl)phenylme-thylen)-1-piperidinyl)ethyl)-7-methyl-5H-thiazol(3,2-a)pyrimidin-5-on

Bezeichnung:6-(2-(4-((4-Fluorphenyl)phenylme-thylen)-1-piperidinyl)ethyl)-7-methyl-5H-thiazol(3,2-a)pyrimidin-5-on

CAS-Nr93076-89-2

Englisch Name:DIACYLGLYCEROL KINASE INHIBITOR I

CBNumberCB3335279

SummenformelC27H26FN3OS

Molgewicht459.58

MOL-Datei93076-89-2.mol

Synonyma

6-(2-(4-((4-Fluorphenyl)phenylme-thylen)-1-piperidinyl)ethyl)-7-methyl-5H-thiazol(3,2-a)pyrimidin-5-on

6-(2-(4-((4-Fluorphenyl)phenylme-thylen)-1-piperidinyl)ethyl)-7-methyl-5H-thiazol(3,2-a)pyrimidin-5-on physikalisch-chemischer Eigenschaften

Siedepunkt	619.8±65.0 °C(Predicted)
Dichte	1.26±0.1 g/cm3(Predicted)
storage temp.	-20°C
Löslichkeit	0.1 M HCl: slightly soluble
Aggregatzustand	solid
pka	7.76±0.20(Predicted)
Farbe	pale yellow
Stabilität	Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

Sicherheit

S-Sätze:	23-24/25
WGK Germany	3

DIACYLGLYCEROL KINASE INHIBITOR I Chemische Eigenschaften,Einsatz,Produktion Methoden

S-Sätze Betriebsanweisung:
S23:Gas/Rauch/Dampf/Aerosol nicht einatmen(geeignete Bezeichnung(en) vom Hersteller anzugeben).
S24/25:Berührung mit den Augen und der Haut vermeiden.
Beschreibung
R-59022 (93076-89-2) is a diacylglycerol kinase (DAGK) inhibitor, nonselective for DAGK isotypes (IC50=2.8 μM in intact platelets).1 Induces autophagy and apoptosis in NG108-15 neuronal cells via an mTOR-independent mechanism.2 Prevents conjugated linoleic acid-mediated inflammatory signaling and insulin resistance in human adipocytes.3 Blocks filovirus internalization in host cells.4
Verwenden
R-59-022 acts as an inducer of apoptosis in glioblastoma cells and avoids apoptosis in non-cancerous cells. This selectivity makes this drug a highly effective anti-cancer agent. Diacylglycerol Kinase inhibitor.
Definition
ChEBI: 6-[2-[4-[(4-fluorophenyl)-phenylmethylidene]-1-piperidinyl]ethyl]-7-methyl-5-thiazolo[3,2-a]pyrimidinone is a diarylmethane.
Biologische Aktivität
Diacylglycerol (DAG) kinase inhibitor (IC 50 = 2.8 μ M); increases protein kinase C activity. Potentiates thrombin-induced platelet aggregation and induces neutrophil chemotaxis. Inhibits U46619-induced contractions in mouse aorta and porcine coronary artery.
Einzelnachweise
de Chaffoy de Courcelles et al. (1985), R 59 022, a diacylglycerol kinase inhibitor. Its effect on diacylglycerol and thrombin-induced C kinase activation in the intact platelet; J. Biol. Chem., 260 15762 Takita et al. (2011), Diacylglycerol kinase inhibitor R59022-induced autophagy and apoptosis in the neuronal cell line NG108-15; Arch. Biochem. Biophys., 509 197 Martinez et al. (2013), Diacylglycerol kinase inhibitor R59022 attenuates conjugated linoleic acid-mediated inflammation in human adipocytes; J. Lipid Res., 54 662 Stewart et al. (2019), A Diacylglycerol Kinase Inhibitor, R-59-022, Blocks Filovirus Internalization in Host Cells; Viruses, 11 206

6-(2-(4-((4-Fluorphenyl)phenylme-thylen)-1-piperidinyl)ethyl)-7-methyl-5H-thiazol(3,2-a)pyrimidin-5-on Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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