Biological Activity
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
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
XMD 8-92 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.
Technical Data
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 18.98 | 40 |
Preparing Stock Solutions
The following data is based on the product molecular weight 474.55. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.11 mL | 10.54 mL | 21.07 mL |
| 5 mM | 0.42 mL | 2.11 mL | 4.21 mL |
| 10 mM | 0.21 mL | 1.05 mL | 2.11 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.42 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
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
Keywords: XMD 8-92, supplier, erk5, bmk1, big, MAP, kinase, 1, inhibitors, inhibits, antitumor, antiproliferative, antiproliferation, XMD8-92, bromodomains, BRD4, ERK, Bromodomains, ERK, Tocris Bioscience
