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R 59-022

Cat. No.:YN310085

  • CAS No. :93076-89-2

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    • 产品名称: R 59-022
      CAS No.: 93076-89-2
      Chemical Name: 6-[2-[4-[(4-fluorophenyl)phenylmethylene]-1-piperidinyl]ethyl]-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one
      Synonyms:DKGI-I; Diacylglycerol kinase inhibitor I
      分子量:459.58
      分子式:C₂₇H₂₆FN₃OS
      SMILES:O=C1C(CCN(CC/2)CCC2=C(C3=CC=CC=C3)/C4=CC=C(F)C=C4)=C(C)N=C5N1C=CS5
      存储:Please store the product under the recommended conditions in theCertificate of Analysis.
      运输:Room temperature in continental US; may vary elsewhere.
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      Purity: 98%
    • 产品描述: R 59-022 (DKGI-I) 是一种二酰甘油激酶 (diacylglycerol kinase) 抑制剂 (IC50=2.8 μM)。R 59-022 是一种5-HTR拮抗剂,激活蛋白激酶 C(PKC)。R 59-022 增强凝血酶诱导血小板产生二酰甘油和抑制中性粒细胞产生磷脂酸。
      IC50和靶点:
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      In Vivo:
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    • Topham, M.K., and Prescott, S.M.Mammalian diacylglycerol kinases, a family of lipid kinases with signaling functionsJ. Biol. Chem.274(17),11447-11450(1999)

      de Chaffoy de Courcelles, D.C., Roevens, P., and Van Belle, H.R 59 022, a diacylglycerol kinase inhibitor. Its effect on diacylglycerol and thrombin-induced C kinase activation in the intact plateletJ. Biol. Chem.260(29),15762-15770(1985)

      Nunn, D.L., and Watson, S.P.A diacylglycerol kinase inhibitor, R59022, potentiates secretion by and aggregation of thrombin-stimulated human plateletsBiochem. J.243(3),809-813(1987)

      Nobe, K., Miyatake, M., Nobe, H., et al.Novel diacylglycerol kinase inhibitor selectively suppressed an U46619-induced enhancement of mouse portal vein contraction under high glucose conditionsBr. J. Pharmacol.143(1),166-179(2004)

      Dominguez, C.L., Floyd, D.H., Xiao, A., et al.Diacylglycerol kinase a is a critical signaling node and novel therapeutic target in glioblastoma and other cancersCancer Discov.3(7),782-797(2013)

      Tu-Sekine, B., Goldschmidt, H., Petro, E., et al.Diacylglycerol kinase θ: Regulation and stabilityAdv. Biol. Regul.53(1),118-126(2013)

      Gómez-Merino, F.C., Arana-Ceballos, F.A., Trejo-Téllez, L.I., et al.Arabidopsis AtDGK7, the smallest member of plant diacylglycerol kinases (DGKs), displays unique biochemical features and saturates at low substrate concentration: The DGK inhibitor R59022 differentially affects AtDGK2 and AtDGK7 activity in vitro and alters plant growth and developmentJ. Biol. Chem.280(41),34888-34899(2005)

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