Molecular structure of DAG Kinase Inhibitor II, CAS Number: 120166-69-0
DAG Kinase Inhibitor II (CAS 120166-69-0)
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Alternate Names:
Diacylglycerol Kinase Inhibitor II; R59949; 3-{2-[4-[bis-(4-Fluorophenyl)methylene]-1-piperidinyl]ethyl}-2,3-dihydro-2-thioxo-4(1H)quinazolinone
Application:
DAG Kinase Inhibitor II is an inhibitor of DGK
CAS Number:
120166-69-0
Purity:
≥98%
Molecular Weight:
489.60
Molecular Formula:
C28H25F2N3OS
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
DAG Kinase Inhibitor II is an inhibitor of DGK (Diacylglycerol kinase DAG Kinase) and is useful for elucidating the roles of protein kinase C (PKC). DAG Kinase Inhibitor II has also been reported to inhibit DGK in several systems such as isolated platelet membranes, whole platelets and ghost erythrocytes. Additional reports have shown to inhibit in a concentration dependent manner. DAG Kinase Inhibitor II may also inhibit other pathways such as NADPH and potentially interfere with the lipid-mediated assembly process of oxidase components as reported using a cell-free system. This particular isoform, R59949, has been reported to potentially exhibit selective inhibition of DGK-alpha.
DAG Kinase Inhibitor II (CAS 120166-69-0) References
- Interleukin-2 causes an increase in saturated/monounsaturated phosphatidic acid derived from 1,2-diacylglycerol and 1-O-alkyl-2-acylglycerol. | Jones, DR., et al. 1999. J Biol Chem. 274: 16846-52. PMID: 10358029
- Selectivity of the diacylglycerol kinase inhibitor 3-[2-(4-[bis-(4-fluorophenyl)methylene]-1-piperidinyl)ethyl]-2, 3-dihydro-2-thioxo-4(1H)quinazolinone (R59949) among diacylglycerol kinase subtypes. | Jiang, Y., et al. 2000. Biochem Pharmacol. 59: 763-72. PMID: 10718334
- Phosphatidic acid and diacylglycerol directly activate NADPH oxidase by interacting with enzyme components. | Palicz, A., et al. 2001. J Biol Chem. 276: 3090-7. PMID: 11060300
- Diacylglycerol kinase alpha activity promotes survival of CD4+ 8+ double positive cells during thymocyte development. | Outram, SV., et al. 2002. Immunology. 105: 391-8. PMID: 11985659
- Phosphatidylcholine-derived phosphatidic acid and diacylglycerol are involved in the signaling pathways activated by docetaxel. | Maestre, N., et al. 2003. J Exp Ther Oncol. 3: 36-46. PMID: 12724857
- Angiotensin II-induced Akt activation through the epidermal growth factor receptor in vascular smooth muscle cells is mediated by phospholipid metabolites derived by activation of phospholipase D. | Li, F. and Malik, KU. 2005. J Pharmacol Exp Ther. 312: 1043-54. PMID: 15525798
- Classical transient receptor potential channel 6 (TRPC6) is essential for hypoxic pulmonary vasoconstriction and alveolar gas exchange. | Weissmann, N., et al. 2006. Proc Natl Acad Sci U S A. 103: 19093-8. PMID: 17142322
- The diacylglycerol kinase inhibitor, R59949, potentiates secretion but not increased phosphorylation of a 47 kDalton protein in human platelets. | Rodríguez-Liñares, B., et al. 1991. Biochem Pharmacol. 41: 835-8. PMID: 1847818
- The role of endogenously formed diacylglycerol in the propagation and termination of platelet activation. A biochemical and functional analysis using the novel diacylglycerol kinase inhibitor, R 59 949. | de Chaffoy de Courcelles, D., et al. 1989. J Biol Chem. 264: 3274-85. PMID: 2536741
- Diacylglycerol kinase (DGK) inhibitor II (R59949) could suppress retinal neovascularization and protect retinal astrocytes in an oxygen-induced retinopathy model. | Yang, L., et al. 2015. J Mol Neurosci. 56: 78-88. PMID: 25451596
- PHD2 attenuates high-glucose-induced blood retinal barrier breakdown in human retinal microvascular endothelial cells by regulating the Hif-1α/VEGF pathway. | Li, J., et al. 2022. Inflamm Res. 71: 69-79. PMID: 34773469
- Alpha 1-adrenoceptor activation of a non-selective cation current in rabbit portal vein by 1,2-diacyl-sn-glycerol. | Helliwell, RM. and Large, WA. 1997. J Physiol. 499 (Pt 2): 417-28. PMID: 9080371
- Secretory vesicle budding from the trans-Golgi network is mediated by phosphatidic acid levels. | Siddhanta, A. and Shields, D. 1998. J Biol Chem. 273: 17995-8. PMID: 9660750
Inhibitor of:
DGK, Enzyme, and PLC γ1.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
DAG Kinase Inhibitor II, 5 mg | sc-3551 | 5 mg | $138.00 | |||
DAG Kinase Inhibitor II, 25 mg | sc-3551A | 25 mg | $388.00 |