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 ActivityERK5 (BMK1) and BRD4 inhibitor (Kd values are 80 and 190 nM, respectively). Also inhibits DCAMKL2, PLK4 and TNK1 (Kd values are 190, 600 and 890 nM). 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.
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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.
ERK5 kinase activity is dispensable for cellular immune response and proliferation.
Lin et al.
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
Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein.
Yang et al.
Cancer Cell, 2010;18:258
Targeting the BMK1 MAP kinase pathway in cancer therapy.
Yang and Lee
Clin.Cancer Res., 2011;17:3527
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
Citations for XMD 8-92
The citations listed below are publications that use Tocris products. Selected citations for XMD 8-92 include:
4 Citations: Showing 1 - 4
Extracellular signal regulated kinase 5 and inflammasome in progression of mesothelioma.
Authors: Thompson Et al.
MEK5/ERK5 signaling inhibition increases colon cancer cell sensitivity to 5-fluorouracil through a p53-dependent mechanism.
Authors: Pereira Et al.
Aberrant MEK5/ERK5 signalling contributes to human colon cancer progression via NF-κB activation.
Authors: Simões Et al.
Cell Death Dis 2015;6:e1718
Kinome profiling reveals breast cancer heterogeneity and identifies targeted therapeutic opportunities for triple negative breast cancer.
Authors: Al-Ejeh Et al.
Mediators Inflamm 2014;5:3145
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