XMD 8-92
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
Purity: ≥98%
Biological Activity
XMD 8-92 is an ERK5 (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.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
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.
Additional Information
Background References
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Extracellular signal regulated kinase 5 and inflammasome in progression of mesothelioma
JK Thompson, A Shukla, AL Leggett, PB Munson, JM Miller, MB MacPherson, SL Beuschel, HI Pass, A Shukla
Oncotarget, 2018;9(1):293-305. -
ERK5 kinase activity is dispensable for cellular immune response and proliferation.
Lin et al.
Proc.Natl.Acad.Sci.U.S.A., 2016;113:11865 -
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
Product Datasheets
Citations for XMD 8-92
The citations listed below are publications that use Tocris products. Selected citations for XMD 8-92 include:
8 Citations: Showing 1 - 8
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ERK5 modulates IL-6 secretion and contributes to tumor-induced immune suppression.
Authors: Helmut Et al.
Cell Death Dis 2021;12:969
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MEKK3-MEK5-ERK5 signaling promotes mitochondrial degradation.
Authors: Jonathan A Et al.
Cell Death Discov 2020;6:107
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Slug regulates the Dll4-Notch-VEGFR2 axis to control endothelial cell activation and angiogenesis.
Authors: David S Et al.
Nat Commun 2020;11:5400
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Identification of Novel RAS Signaling Therapeutic Vulnerabilities in Diffuse Intrinsic Pontine Gliomas.
Authors: C David Et al.
Cancer Res 2019;79:4026-4041
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Extracellular signal regulated kinase 5 and inflammasome in progression of mesothelioma.
Authors: Thompson Et al.
Oncotarget 2018;9:293
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MEK5/ERK5 signaling inhibition increases colon cancer cell sensitivity to 5-fluorouracil through a p53-dependent mechanism.
Authors: Pereira Et al.
Oncotarget 2016;7:34322
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Aberrant MEK5/ERK5 signalling contributes to human colon cancer progression via NF-κB activation.
Authors: Simões Et al.
Cell Death Dis 2015;6:e1718
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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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