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K-252a

Cat. No.:YN310367

  • CAS No. :99533-80-9

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    • 产品名称: K-252a
      CAS No.: 99533-80-9
      Chemical Name: 2,3,9S,10R,11,12R-hexahydro-10-hydroxy-9-methyl-1-oxo-9,12-epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid, methyl ester
      Synonyms:SF2370; Antibiotic K 252a; Antibiotic SF 2370
      分子量:467.47
      分子式:C₂₇H₂₁N₃O₅
      SMILES:O=C(NC1)C2=C1C3=C4C5=C2C6=C(C=CC=C6)N5[C@](C[C@]7(O)C(OC)=O)([H])O[C@]7(C)N4C8=C3C=CC=C8
      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: K-252a 可从土壤真菌Nocardiopsis sp.中分离得到的一种十字孢碱的类似物,是蛋白激酶的抑制剂,对 PKC、PKA、II型钙调素依赖性激酶和磷酸化酶激酶的IC50值分别为470 nM、140 nM、270 nM和1.7 nM。K-252a 是一种有效抑制 NGF 受体 gp140trk 的酪氨酸蛋白激酶 (TRK) 活性,IC50为 3 nM。
      IC50和靶点:
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    • Yasuzawa, T., Iida, T., Yoshida, M., et al.The structures of the novel protein kinase C inhibitors K-252a, b, c and dJ. Antibiot. (Tokyo)39(8),1072-1078(1986)

      Davis, P.D., Hill, C.H., Lawton, G., et al.Inhibitors of protein kinase C. 1.1 2,3-bisarylmaleimidesJ. Med. Chem.35(1),177-184(1992)

      Kawamura, N., Kawamura, K., Manabe, M., et al.Inhibition of brain-derived neurotrophic factor/tyrosine kinase B signaling suppresses choriocarcinoma cell growthEndocrinology151(7),3006-3014(2010)

      Köhler, J., Erlenkamp, G., Eberlin, A., et al.Lestaurtinib inhibits histone phosphorylation and androgen-dependent gene expression in prostate cancer cellsPLoS One7(4),(2012)

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