R59949
Cat. No.:YN310401
CAS No. :120166-69-0
产品名称: | R59949 |
CAS No.: | 120166-69-0 |
Chemical Name: | 3-[2-[4-[bis(4-fluorophenyl)methylene]-1-piperidinyl]ethyl]-2,3-dihydro-2-thioxo-4(1H)-quinazolinone |
Synonyms: | R59949;R 59949 |
分子量: | 489.6 |
分子式: | C28H25F2N3OS |
SMILES: | S=C1N(CCN2CC/C(CC2)=C(C3=CC=C(F)C=C3)/C4=CC=C(F)C=C4)C(C5=CC=CC=C5N1)=O |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | R59949 是一种泛二酰甘油激酶(DGK)抑制剂,IC50为 300 nM。R59949 强烈抑制 Ⅰ 型 DGKα 和 γ 的活性,中度减弱 Ⅱ 型 DGKθ 和 κ 的活性。R59949 通过提高内源性配体二酰甘油水平来激活蛋白激酶C(PKC)。 |
IC50和靶点: | |
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Du, X., Jiang, Y., Qian, W., et al.Fatty acids inhibit growth-factor-induced diacylglycerol kinase alpha activation in vascular smooth-muscle cellsBiochem J.357(Pt. 1),275-282(2001)
Kurohane Kaneko, Y., Kobayashi, Y., Motoki, K., et al.Depression of type I diacylglycerol kinases in pancreatic β-cells from male mice results in impaired insulin secretionEndocrinology154(11),4089-4098(2013)
Yang, L., Xu, Y., Li, W., et al.Diacylglycerol kinase (DGK) inhibitor II (R59949) could suppress retinal neovascularization and protect retinal astrocytes in an oxygen-induced retinopathy modelJ. Mol. Neurosci.56(1),78-88(2015)