| Identification | Back Directory | [Name]
DIACYLGLYCEROL KINASE INHIBITOR I | [CAS]
93076-89-2 | [Synonyms]
DKI
DAGK
DGKI
DGKE
DAGK4
DAGK7
DGK-θ
DKGI-I
R59022
DAG KINASE
EC 2.7.1.107
EC: 2.7.1.107
Diglyceride kinase κ
DIACYLGLYCEROL KINASE
SN-1,2-DIACYLGLYCEROL KINASE
DIACYLGLYCEROL KINASE SOLUTION
DIACYLGLYCEROL KINASE INHIBITOR I
DIACYLGLYCEROL KINASE FROM E. COLI
sn-1,2-Diacylglycerol kinase, DAGK
DIACYLGLYCEROL KINASE INHIBITOR I (R59 022)
Diacylglycerol Kinase from Escherichia coli
SN-1,2-DIACYLGLYCEROL KINASE, RECOMBINANT, E COLI
Anti-DGKI, C-Terminal antibody produced in rabbit
Anti-DGKD, N-Terminal antibody produced in rabbit
Anti-DGKQ, C-Terminal antibody produced in rabbit
Diacylglycerol Kinase Inhibitor I - CAS 93076-89-2 - Calbiochem
6-[2-[(4-FLUOROPHENYL)PHENYLMETHYLENE]-1-PIPERIDINYL)ETHYL]-7-METHYL-5H-THIAZOLO-[3,2-A]-PYRIMIDIN-5-ONE
6-[2-[4-[(4-FLUOROPHENYL)PHENYLMETHYLENE]-1-PIPERIDINYL]ETHYL]-7-METHYL-5H-THIAZOLO[3,2-A]PYRIMIDIN-5-ONE
6-[2-[4-[(P-FLUOROPHENYL)PHENYLMETHYLENE]-1-PIPERIDINYL]ETHYL]-7-METHYL-5H-THIAZOLO(3,2-A)PYRIMIDINE-5-ONE
6-(2-(4-((4-Fluorophenyl)phenylmethylene)-1-piperidinyl)ethyl)-7-methyl-5H-thiazolo(3,2-A)pyrimidine-5-one
5H-Thiazolo(3,2-A)pyrimidin-5-one, 6-(2-(4-((4-fluorophenyl)phenylmethylene)-1-piperidinyl)ethyl)-7-methyl-
6-[2-[4-[(4-fluorophenyl)phenylmethylene]-1-piperidin-yl]ethyl]-7-methyl-5h-thiazolo-[3,2-a]-pyrimidin-5-one
6-[2-[4-[(4-fluorophenyl)-phenylmethylidene]piperidin-1-yl]ethyl]-7-methyl-[1,3]thiazolo[3,2-a]pyrimidin-5-one
6-[2-[4-[(4-Fluorophenyl)phenylMethylene]-1-piperidin-yl]ethyl]-7-Methyl-5H-thiazolo-[3,2-a]-pyriMidin-5-one, R59022
R59022, 6-[2-[4-[(4-Fluorophenyl)phenylmethylene]-1-piperidinyl]ethyl]-7-methyl-5H-thiazolo-[3,2-a]-pyrimidin-5-one | [Molecular Formula]
C27H26FN3OS | [MDL Number]
MFCD00055114 | [MOL File]
93076-89-2.mol | [Molecular Weight]
459.58 |
| Chemical Properties | Back Directory | [Boiling point ]
619.8±65.0 °C(Predicted) | [density ]
1.26±0.1 g/cm3(Predicted) | [storage temp. ]
-20°C | [solubility ]
0.1 M HCl: slightly soluble
| [form ]
solid
| [pka]
7.76±0.20(Predicted) | [color ]
pale yellow
| [biological source]
synthetic (organic) | [Stability:]
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| Hazard Information | Back Directory | [Description]
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 | [Uses]
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. | [Biological Activity]
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. | [in vivo]
R 59-022 (2 mg/kg, i.p., 12 days) significantly increases median survival in SCID mice implanted with U87 GBM cells[6].
| Animal Model: | SCID mice implanted with U87 GBM cells[6] | | Dosage: | 10 mg/kg | | Administration: | Intraperitoneal injection (i.p.) | | Result: | Increased median survival and decreased tumor volume. |
| [IC 50]
PKC; serotonin; diacylglycerol kinase: 2.8 μM (IC50) | [storage]
Store at -20°C | [References]
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 |
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