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K252b

A Potent Inhibitor of Protein Kinase A, Protein Kinase C, and Protein Kinase G

Cat #: K-170
Lyophilized Powder yes
  • Bioassay Tested
    • Origin Nocardiopsis sp. (soil fungi).
    Source Natural
    MW: 453
    Purity: >98%
    Effective concentration 50-500 nM.
    Structure
    Chemical name (9R,10S,12S)-2,3,9,10,11,12-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.
    Molecular formula C26H19N3O5.
    CAS No.: 99570-78-2
    Activity K252b is a less potent derivative of K252a and inhibits a variety of kinases including PKC (IC50 = 20 nM), PKA (IC50 = 90 nM) and PKG (IC50 = 100 nM)1. It also inhibits MLCK (IC50 = 147 nM) and CaMK (IC50 = 12 nM).
    References-Activity
    1. Kase, H. et al. (1987) Biochem. Biopphys. Res. Commun. 142, 436.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility DMSO or DMF. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to one week at 4°C or three months at -20°C.
    Protect from light.
    Our bioassay
    • Alomone Labs K252b inhibits MARCKS phosphorylation via PKC in C6 glioma cells.
      Alomone Labs K252b inhibits MARCKS phosphorylation via PKC in C6 glioma cells.
      Cells were grown to 70% confluence, and then serum starved for 18 h. The cells were preincubated for 30 min with different concentrations of K252b (#K-170) and stimulated with 2 µM PMA (#P-800) for 30 min. Cell proteins were resolved by SDS-PAGE and probed with anti-phospho (ser)- MARCKS (myristoylated alanine-rich protein kinase C substrate).
    • Alomone Labs K252b inhibits tyrosine phosphorylation of TrKA in PC12 cells.
      Alomone Labs K252b inhibits tyrosine phosphorylation of TrKA in PC12 cells.
      Cells were incubated in the presence or absence of 10 ng/ml NGF with or without various concentrations of K252b (#K-170). The inhibitory effect of K252b on neurite outgrowth stimulated by NGF is presented.
    References - Scientific background
    1. Yasuzawa T. et al. (1986) J. Antibiotics 39, 1072.
    2. Ross, A.H. et al. (1995) J. Neurochem. 65, 2748.
    3. Kojima, M. et al. (1995) J. Neurosci Res. 42, 775.
    4. Galter, D. and Unsicker, K. (2000) J. Neurosci Res. 61, 295.
    5. Taoka, M. et al. (1990) Biochem Biophys Res Commun. 170, 1151.
    Scientific background

    K252b is an alkaloid isolated from Nocardiopsis sp. soil fungi. It is a less potent derivative of K252a,3-5 cell-permeable protein kinase inhibitor.

    This compound potentiates neurotrophin-3 activity in certain neurons by an unknown mechanism. In other neurons it serves as a control to K252a since it accumulates in the plasma membrane of the neuron.1

    Lyophilized Powder
    Last update: 13/10/2022

    K252b (#K-170) is a highly pure, natural, and biologically active compound.

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    For research purposes only, not for human use

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