DIACYLGLYCEROL KINASE INHIBITOR I
Synonym(s):6-[2-[4-[(4-Fluorophenyl)phenylmethylene]-1-piperidin-yl]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, R59022;Diacylglycerol Kinase Inhibitor I - CAS 93076-89-2 - Calbiochem;R59022;R59022, 6-{2-{4-[(p-Fluorophenyl)phenylmethylene]-1-piperidinyl}ethyl}-7-methyl-5H-thiazolo(3,2-a)pyrimidine-5-one
- CAS NO.:93076-89-2
- Empirical Formula: C27H26FN3OS
- Molecular Weight: 459.58
- MDL number: MFCD00055114
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-07-14 17:34:50
What is DIACYLGLYCEROL KINASE INHIBITOR I?
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
The Uses of DIACYLGLYCEROL KINASE INHIBITOR I
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.
What are the applications of Application
R 59-022 is an inhibitor of DGK and serotonin
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.
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
Properties of DIACYLGLYCEROL KINASE INHIBITOR I
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 |
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. |
Safety information for DIACYLGLYCEROL KINASE INHIBITOR I
Computed Descriptors for DIACYLGLYCEROL KINASE INHIBITOR I
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