DIACYLGLYCEROL KINASE INHIBITOR I
- Product Name
- DIACYLGLYCEROL KINASE INHIBITOR I
- CAS No.
- 93076-89-2
- Chemical Name
- DIACYLGLYCEROL KINASE INHIBITOR I
- Synonyms
- DKI;DAGK;DGKE;DGKI;DAGK4;DAGK7;DGK-θ;R59022;DKGI-I;DAG KINASE
- CBNumber
- CB3335279
- Molecular Formula
- C27H26FN3OS
- Formula Weight
- 459.58
- MOL File
- 93076-89-2.mol
DIACYLGLYCEROL KINASE INHIBITOR I Property
- 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
- Safety Statements
- 23-24/25
- WGK Germany
- 3
N-Bromosuccinimide Price
- Product number
- D5919
- Product name
- Diacylglycerol Kinase Inhibitor I
- Purity
- solid
- Packaging
- 1mg
- Price
- $127
- Updated
- 2024/03/01
- Product number
- 266785
- Product name
- Diacylglycerol Kinase Inhibitor I
- Packaging
- 5mg
- Price
- $172
- Updated
- 2024/03/01
- Product number
- 16772
- Product name
- R-59-022
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $37
- Updated
- 2024/03/01
- Product number
- 16772
- Product name
- R-59-022
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $90
- Updated
- 2024/03/01
- Product number
- D5919
- Product name
- Diacylglycerol Kinase Inhibitor I
- Purity
- solid
- Packaging
- 5mg
- Price
- $440
- Updated
- 2024/03/01
DIACYLGLYCEROL KINASE INHIBITOR I Chemical Properties,Usage,Production
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.
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