DAG Kinase Inhibitor II DAG Kinase Inhibitor is an inhibitor of DGK (Diacylglycerol kinase; DAG Kinase) and is useful for elucidating the roles of protein kinase C (PKC). This particular isoform, R59949, has been reported to potentially exhibit selective inhibition of DGK-α.

DAG Kinase Inhibitor II  (CAS 120166-69-0)

DAG Kinase Inhibitor II is rated 5.0 out of 5 by 1.
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| See 1 Citations
Synonym: Diacylglycerol Kinase Inhibitor II; R59949; 3-{2-[4-[bis-(4-Fluorophenyl)methylene]-1-piperidinyl]ethyl}-2,3-dihydro-2-thioxo-4(1H)quinazolinone
Application: An inhibitor of DGK
CAS Number: 120166-69-0
Purity: ≥98%
Molecular Weight: 489.6
Molecular Formula: C28H25F2N3OS
* Refer to Certificate of Analysis for lot specific data (including water content).
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Ordering Information

PRODUCT NAME CATALOG # UNIT PRICE QTY FAVORITES
DAG Kinase Inhibitor II sc-3551 5 mg $101.00

DAG Kinase Inhibitor is an inhibitor of DGK (Diacylglycerol kinase; DAG Kinase) and is useful for elucidating the roles of protein kinase C (PKC). DAG Kinase Inhibitor 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 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-α.


References

1. de Chaffoy de Courcelles, D., et al. 1989. J. Biol. Chem. 264: 3274-3285. PMID: 2536741
2. Rodríguez-Liñares, B., et al. 1991. Biochem. Pharmacol. 41: 835-838. PMID: 1847818
3. Jones, D.R., et al. 1999. J. Biol. Chem. 274: 16846-16852. PMID: 10358029
4. Jiang, Y., et al. 2000. Biochem. Pharmacol. 59: 763-772. PMID: 10718334
5. Palicz, A., et al. 2001. J. Biol. Chem. 276: 3090-3097. PMID: 11060300
6. Outram, S.V., et al. 2002. Immunology. 105: 391-398. PMID: 11985659

Physical State :
Solid
Solubility :
Soluble in N,N-DMF (89 g/l), DMSO (33 g/l), dichloromethane (35 g/l), ethanol, ethyl acetate, 0.1 M HCl (slightly soluble), 0.1 M NaOH (slightly soluble), and tetrahydro-furan. Insoluble in water.
Storage :
Store at 4° C
Melting Point :
228-230° C
Boiling Point :
637.07° C at 760 mmHg (Predicted)
Density :
1.37 g/cm3 (Predicted)
Refractive Index :
n20D 1.69 (Predicted)
IC50 :
diacylglycerol kinase in isolated platelet membranes: IC50 = 300 nM; diacylglycerol kinase in intact platelets: IC50 = 120 nM
pK Values :
pKa: 11.24 (Predicted), pKb: 8.33 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
657356
MDL Number :
MFCD00069258
SMILES :
C1CN(CCC1=C(C2=CC=C(C=C2)F)C3=CC=C(C=C3)F)CCN4C(=O)C5=CC=CC=C5NC4=S

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Certificate of Analysis

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PMID: # 26112921
Kelleher, RJ. et al. 2015. Extracellular Vesicles Present in Human Ovarian Tumor Microenvironments Induce a Phosphatidylserine-Dependent Arrest in the T-cell Signaling Cascade. Cancer Immunol Res. 3: 1269-78.

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Rated 5 out of 5 by from Yang Yang, L. et al. (PubMed 25451596) suggest that DAG Kinase Inhibitor II could suppress retinal neovascularization and protect retinal astrocytes in an oxygen-induced retinopathy model. -SCBT Publication Review
Date published: 2015-06-02
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