| Company Name: |
Sigma-Aldrich |
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021-61415566 800-8193336 |
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orderCN@merckgroup.com |
DIACYLGLYCEROL KINASE INHIBITOR I manufacturers
- R 59-022
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- $32.00
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2026-07-14
- CAS:93076-89-2
- Purity: 99.18%
- Supply Ability: 10g
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| | DIACYLGLYCEROL KINASE INHIBITOR I Basic information |
| Product Name: | DIACYLGLYCEROL KINASE INHIBITOR I | | Synonyms: | 6-[2-[4-[(P-FLUOROPHENYL)PHENYLMETHYLENE]-1-PIPERIDINYL]ETHYL]-7-METHYL-5H-THIAZOLO(3,2-A)PYRIMIDINE-5-ONE;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;DIACYLGLYCEROL KINASE;DIACYLGLYCEROL KINASE INHIBITOR I;DIACYLGLYCEROL KINASE INHIBITOR I (R59 022);DAGK;DAG KINASE | | CAS: | 93076-89-2 | | MF: | C27H26FN3OS | | MW: | 459.58 | | EINECS: | | | Product Categories: | Lipid signaling | | Mol File: | 93076-89-2.mol |  |
| | DIACYLGLYCEROL KINASE INHIBITOR I Chemical Properties |
| 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. | | 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 | | InChIKey | MFVJXLPANKSLLD-UHFFFAOYSA-N | | SMILES | Fc1ccc(cc1)C(=C3CCN(CC3)CCc4[c]([n]5c([s]cc5)nc4C)=O)c2ccccc2 |
| Safety Statements | 23-24/25 | | WGK Germany | 3 | | Storage Class | 11 - Combustible Solids |
| | DIACYLGLYCEROL KINASE INHIBITOR I Usage And Synthesis |
| 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) | | References | [1] D C DE CHAFFOY DE COURCELLES H V B P Roevens. R 59 022, a diacylglycerol kinase inhibitor. Its effect on diacylglycerol and thrombin-induced C kinase activation in the intact platelet.[J]. The Journal of Biological Chemistry, 1985, 260 29: 15762-15770.
[2] TSUYOSHI TAKITA. Diacylglycerol kinase inhibitor R59022-induced autophagy and apoptosis in the neuronal cell line NG108-15[J]. Archives of biochemistry and biophysics, 2011, 509 2: Pages 197-201. DOI:10.1016/j.abb.2011.02.007
[3] KRISTINA MARTINEZ. Diacylglycerol kinase inhibitor R59022 attenuates conjugated linoleic acid-mediated inflammation in human adipocytes.[J]. Journal of Lipid Research, 2013, 54 3: 662-670. DOI:10.1194/jlr.m031211
[4] CORINA M STEWART. A Diacylglycerol Kinase Inhibitor, R-59-022, Blocks Filovirus Internalization in Host Cells.[J]. Viruses-Basel, 2019, 11 3. DOI:10.3390/v11030206 |
| | DIACYLGLYCEROL KINASE INHIBITOR I Preparation Products And Raw materials |
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