Catalog Number: 3528
Chemical Name: 6-Chloro-5-[[(2R,5S)-4-[(4-fluorophenyl)methyl]-2,5-dimethyl-1-piperazinyl]carbonyl]-N,N,1-trimethyl-α-oxo-1H-Indole-3-acetamide hydrochloride
Biological Activity
Selective, ATP-competitive p38 inhibitor (IC50 = 9 nM for p38α in vitro). Displays approximately 10-fold selectivity for p38α over p38β and 2000-fold selectivity for p38α over 20 other kinases. Reduces p38α phosphorylation in multiple myeloma cells in vitro and in vivo; activity results in decreased tumor burden and angiogenesis in murine models of multiple myeloma. Also enhances bortezomib-induced cytotoxicity against multiple myeloma cells.
Technical Data
  • M.Wt:
    549.46
  • Formula:
    C27H30ClFN4O3.HCl
  • Solubility:
    Soluble to 10 mM in water and to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Desiccate at +4°C
  • CAS No:
    309913-83-5
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. p38 MAPK inhibition enhances PS-341 (bortezomib)-induced cytotoxicity against multiple myeloma cells.
    Hideshima et al.
    Oncogene., 2004;23:8766
  2. Role of the p38 mitogen-activated protein kinase pathway in the generation of arsenic trioxide-dependent cellular responses.
    Giafis et al.
    Cancer Res., 2006;66:6763
  3. Inhibition of p38α mitogen-activated protein kinase prevents the development of osteolytic bone disease, reduces tumor burden, and increases survival in murine models of multiple myeloma.
    Vanderkerken et al.
    Cancer Res., 2007;67:4572

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