Home / Broad Spectrum Protein Kinase Inhibitors / K 252a

K 252a

Catalog #: 1683
7 Citations Datasheet
Catalog # Availability Size / Price Qty
1683/200U
K 252a | CAS No. 99533-80-9 | Broad Spectrum Protein Kinase Inhibitors
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Description: Protein kinase inhibitor
Alternative Names: SF 2370

Chemical Name: (9S,10R,12R)-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 methyl ester

Purity: ≥98%

Product Details
Citations (7)
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Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

K 252a is a non-selective protein kinase inhibitor; analog of staurosporine (Cat.No. 1285). Inhibits PKC (IC50 = 32.9 nM), Ca2+/calmodulin-stimulated phosphodiesterases (IC50 = 1.3 - 2.9 μM), MLCK (Ki = 20 nM) and receptor tyrosine kinases. Inhibits the oncogenic properties of MET; prevents autophosphorylation and activation of downstream effectors (MAPK, Akt).

Technical Data

M.Wt:
467.48
Formula:
C27H21N3O5
Solubility:
Soluble to 25 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
99533-80-9

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. Erythropoietin attenuates loss of potassium chloride co-transporters following prenatal brain injury.
    Jantzie L, Getsy P, Firl D, Wilson C, Miller R, Robinson S
    Mol Cell Neurosci, 2014;61(0):152-62.
  2. Potentiation of Synaptic GluN2B NMDAR Currents by Fyn Kinase Is Gated through BDNF-Mediated Disinhibition in Spinal Pain Processing

    Cell Rep, 2016;17(10):2753-2765.
  3. Oncogenic and drug-sensitive NTRK1 rearrangements in lung cancer.
    Vaishnavi A, Capelletti M, Le A, Kako S, Butaney M, Ercan D, Mahale S, Davies K, Aisner D, Pilling A, Berge E, Kim J, Sasaki H, Park S, Kryukov G, Garraway L, Hammerman P, Haas J, Andrews S, Lipson D, Stephens P, Miller V, Varella-Garcia M, Janne P, Doebele R
    Nat Med, 2013;19(11):1469-72.
  4. Epiregulin and EGFR interactions are involved in pain processing
    LJ Martin, SB Smith, A Khoutorsky, CA Magnussen, A Samoshkin, RE Sorge, C Cho, N Yosefpour, S Sivaselvac, S Tohyama, T Cole, TM Khuong, E Mir, DG Gibson, JS Wieskopf, SG Sotocinal, JS Austin, CB Meloto, JH Gitt, C Gkogkas, N Sonenberg, JD Greenspan, RB Fillingim, R Ohrbach, GD Slade, C Knott, R Dubner, AG Nackley, A Ribeiro-da, GG Neely, W Maixner, DV Zaykin, JS Mogil, L Diatchenko
    J. Clin. Invest., 2017;0(0):.
  5. K-252a, a potent inhibitor of protein kinase C from microbial origin.
    Kase et al.
    J.Antibiot., 1986;39:1059
  6. K-252 compounds: modulators of neurotrophin signal transduction.
    Knusel and Hefti
    J.Neurochem., 1992;59:1987
  7. K252a inhibits the oncogenic properties of Met, the HGF receptor.
    Morotti et al.
    Oncogene, 2002;21:4885
  8. Staurosporine, K-252 and UCN-01: potent but nonspecific inhibitors of protein kinases.
    Ruegg and Burgess
    TiPS, 1989;10:218

Product Datasheets

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Citations for K 252a

The citations listed below are publications that use Tocris products. Selected citations for K 252a include:

7 Citations: Showing 1 - 7

  1. Aging Increases Hippocampal DUSP2 by a Membrane Cholesterol Loss-Mediated RTK/p38MAPK Activation Mechanism.
    Authors: Martín-Segura Et al.
    Front Neurol  2019;10:675
  2. Exercise-induced neuroprotection in the spastic Han Wistar rat: the possible role of brain-derived neurotrophic factor.
    Authors: Kummer and Cohen
    Neuropsychopharmacology  2015;2015:834543
  3. BDNF released during neuropathic pain potentiates NMDA receptors in primary afferent terminals.
    Authors: Chen Et al.
    Eur J Neurosci  2014;39:1439
  4. TrkB interacts with ErbB4 and regulates NRG1-induced NR2B phosphorylation in cortical neurons before synaptogenesis.
    Authors: Pandya and Pillai
    Biomed Res Int  2014;12:47
  5. Paraneoplastic CDR2 and CDR2L antibodies affect Purkinje cell calcium homeostasis.
    Authors: Schubert Et al.
    Acta Neuropathol  2014;128:835
  6. Inactivation of JAK2/STAT3 signaling axis and downregulation of M1 mAChR cause cognitive impairment in klotho mutant mice, a genetic model of aging.
    Authors: Park Et al.
    Mol Cells  2013;38:1426
  7. β1-Adrenergic receptors activate two distinct signaling pathways in striatal neurons.
    Authors: Meitzen Et al.
    J Neurochem  2011;116:984

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