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Submit ReviewXMD 8-92
Description: ERK5/BMK1 inhibitor; also BRD4 inhibitor
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% (HPLC)
Biological Activity for XMD 8-92
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.
Licensing Information
Sold under license from the Dana-Farber Cancer Institute.
External Portal Information for XMD 8-92
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.
Compound Libraries for XMD 8-92
XMD 8-92 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.
Technical Data for XMD 8-92
| M. Wt | 474.55 |
| Formula | C26H30N6O3 |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 1234480-50-2 |
| PubChem ID | 46843772 |
| InChI Key | QAPAJIZPZGWAND-UHFFFAOYSA-N |
| Smiles | O=C2C3=C(C=CC=C3)N(C)C1=NC(NC4=C(OCC)C=C(N5CCC(O)CC5)C=C4)=NC=C1N2C |
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.
Solubility Data for XMD 8-92
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 18.98 | 40 |
Preparing Stock Solutions for XMD 8-92
The following data is based on the product molecular weight 474.55. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.4 mM | 5.27 mL | 26.34 mL | 52.68 mL |
| 2 mM | 1.05 mL | 5.27 mL | 10.54 mL |
| 4 mM | 0.53 mL | 2.63 mL | 5.27 mL |
| 20 mM | 0.11 mL | 0.53 mL | 1.05 mL |
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Product Datasheets for XMD 8-92
References for XMD 8-92
References are publications that support the biological activity of the product.
Yang et al (2010) Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein. Cancer Cell 18 258 PMID: 20832753
Yang and Lee (2011) Targeting the BMK1 MAP kinase pathway in cancer therapy. Clin.Cancer Res. 17 3527 PMID: 21385929
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
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
Lin et al (2016) ERK5 kinase activity is dispensable for cellular immune response and proliferation. Proc.Natl.Acad.Sci.U.S.A. 113 11865 PMID: 27679845
If you know of a relevant reference for XMD 8-92, please let us know.
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Keywords: XMD 8-92, XMD 8-92 supplier, erk5, bmk1, big, MAP, kinase, 1, inhibitors, inhibits, antitumor, antiproliferative, antiproliferation, XMD8-92, bromodomains, BRD4, ERK, Bromodomains, 4132, Tocris Bioscience
8 Citations for XMD 8-92
Citations are publications that use Tocris products. Selected citations for XMD 8-92 include:
Helmut et al (2021) ERK5 modulates IL-6 secretion and contributes to tumor-induced immune suppression. Cell Death Dis 12 969 PMID: 34671021
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
C David et al (2019) Identification of Novel RAS Signaling Therapeutic Vulnerabilities in Diffuse Intrinsic Pontine Gliomas. Cancer Res 79 4026-4041 PMID: 31201162
Thompson et al (2018) Extracellular signal regulated kinase 5 and inflammasome in progression of mesothelioma. Oncotarget 9 293 PMID: 29416614
Pereira et al (2016) MEK5/ERK5 signaling inhibition increases colon cancer cell sensitivity to 5-fluorouracil through a p53-dependent mechanism. Oncotarget 7 34322 PMID: 27144434
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
David S et al (2020) Slug regulates the Dll4-Notch-VEGFR2 axis to control endothelial cell activation and angiogenesis. Nat Commun 11 5400 PMID: 33106502
Jonathan A et al (2020) MEKK3-MEK5-ERK5 signaling promotes mitochondrial degradation. Cell Death Discov 6 107 PMID: 33101709
Do you know of a great paper that uses XMD 8-92 from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
MAPK Signaling Scientific Review
MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.
Pathways for XMD 8-92
