Catalog Number: 4132
Chemical Name: 2-[[2-Ethoxy-4-(4-hydroxy-1-piperidinyl)phenyl]amino]-5,11-dihydro-5,11-dimethyl-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one
Biological Activity
ERK5/BMK1 inhibitor (KD values are 80, 190, 600 and 890 nM for BMK1, DCAMKL2, PLK4 and TNK1 respectively). Displays selectivity over 402 diverse kinases. Blocks growth factor-induced activation of cellular BMK1 and reduces BMK1 activity in in vitro kinase assays. Also reduces BMK1-dependent transactivating activity of MEF2C. Inhibits proliferation in a variety of cancer cell lines; blocks tumor cell proliferation and tumor-associated angiogenesis.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 40 mM in DMSO
  • Purity:
  • Storage:
    Store at RT
  • CAS No:
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.
Additional Information
Licensing Caveats:
Sold under license from the Dana-Farber Cancer Institute.
Background References
  1. Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein.
    Yang et al.
    Cancer Cell, 2010;18:258
  2. Targeting the BMK1 MAP kinase pathway in cancer therapy.
    Yang and Lee
    Clin.Cancer Res., 2011;17:3527
  3. Discovery of a benzo[e]pyrimido-[5,4-b][1,4]diazepin-6(11H)-one as a potent and selective inhibitor of big MAP kinase 1.
    Deng et al.
    ACS Med.Chem.Lett., 2011;2:195
  4. Canonical and kinase activity-independent mechanisms for extracellular signal-regulated kinase 5 (ERK5) nuclear translocation require dissociation of Hsp90 from the ERK5-Cdc37 complex.
    Erazo et al.
    Mol.Cell Biol., 2013;33:1671

The citations listed below are publications that use Tocris products. Selected citations for XMD 8-92 include:

Showing Results 1 - 2 of 2

  1. Aberrant MEK5/ERK5 signalling contributes to human colon cancer progression via NF-κB activation.
    Authors: Simões Et al.
    Cell Death Dis
  2. Kinome profiling reveals breast cancer heterogeneity and identifies targeted therapeutic opportunities for triple negative breast cancer.
    Authors: Al-Ejeh Et al.
    Mediators Inflamm
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