Product overview

  • Name
    K-252a
  • Short description
    Non-selective protein kinase inhibitor
  • Biological description
    Non-selective protein kinase inhibitor (IC50 values are 10-30 nM for serine/threonine protein kinases). PKC and Ca2+ / calmodulin-stimulated phosphodiesterase inhibitor (IC50 values are 32.9 nM and 1.8 - 2.8 µM respectively). Competitively inhibits myosin light chain kinase (MLCK) - may interact with the ATP-binding domain (Ki = 20 nM). Blocks neuronal differentiation by potently inhibiting NGF receptor gp140trk tyrosine protein kinase (IC50 = 3nM). Cell permeable and shows potential anti-tumor actions.
  • Biological action
    Inhibitor
  • Purity
    >97%
  • Our products in action

Properties

  • Chemical name
    SF 2370
  • Molecular Weight
    467.5
  • Chemical structure
    K-252a  [99533-80-9]
  • Molecular Formula
    C27H21N3O5
  • CAS Number
    99533-80-9
  • PubChem identifier
    11612445
  • SMILES
    C[C@]12[C@@](CC(O1)N3C4=CC=CC=C4C5=C6C(=C7C8=CC=CC=C8N2C7=C53)CNC6=O)(C(=O)OC)O

Storing and Using Your Product

  • Solubility overview
    soluble in DMSO (1mg/ml) or DMF (1mg/ml)

References for K-252a

  • K-252a, a potent inhibitor of protein kinase C from microbial origin.

    Kase H et al (1986) J Antibiot (Tokyo) 39(8) : 1059-65.
    PubMedID: 3759657
  • K-252a, a novel microbial product, inhibits smooth muscle myosin light chain kinase.

    Nakanishi S et al (1988) J Biol Chem 263(13) : 6215-9.
    PubMedID: 2966151
  • K252a is a selective inhibitor of the tyrosine protein kinase activity of the trk family of oncogenes and neurotrophin receptors.

    Tapley P et al (1992) Oncogene 7(2) : 371-81.
    PubMedID: 1312698
  • The effect of K-252a, a potent microbial inhibitor of protein kinase, on activated cyclic nucleotide phosphodiesterase.

    Matsuda Y et al (1988) Biochem J 256(1) : 75-80.
    PubMedID: 2851986

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