XMD 8-92

Cat. No. 4132

XMD 8-92 C26H30N6O3 [1234480-50-2]

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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.

Licensing Information

Sold under license from the Dana-Farber Cancer Institute.

External Portal Information

Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of XMD 8-92 is reviewed on the chemical probes website.

Technical Data

Soluble to 40 mM in DMSO
>98 %
Store at RT

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.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
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Safety Data Sheet: View Safety Data Sheet

Erazo et al (2013) Canonical and kinase activity-independent mechanisms for extracellular signal-regulated kinase 5 (ERK5) nuclear translocation require dissociation of Hsp90 from the ERK5-Cdc37 complex. Mol.Cell Biol. 33 1671. PMID: 23428871.

Deng et al (2011) 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. ACS Med.Chem.Lett. 2 195. PMID: 21412406.

Yang and Lee (2011) Targeting the BMK1 MAP kinase pathway in cancer therapy. Clin.Cancer Res. 17 3527. PMID: 21385929.

Yang et al (2010) Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein. Cancer Cell 18 258. PMID: 20832753.

If you know of a relevant reference for this product please let us know.

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

Simões et al (2015) Aberrant MEK5/ERK5 signalling contributes to human colon cancer progression via NF-κB activation. Cell Death Dis 6 e1718. PMID: 25855966.

Al-Ejeh et al (2014) Kinome profiling reveals breast cancer heterogeneity and identifies targeted therapeutic opportunities for triple negative breast cancer. Mediators Inflamm 5 3145. PMID: 24762669.

Do you know of a great paper that uses XMD 8-92 from Tocris? If so please let us know.

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Keywords: XMD 8-92, supplier, erk5, bmk1, big, MAP, kinase, 1, selective, inhibitors, inhibits, antitumor, antiproliferative, antiproliferation, XMD8-92, Tocris Bioscience, ERK Inhibitor products

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