XMD 8-92

Key Product Details

Product Description

XMD 8-92 is an ERK5 (BMK1) and BRD4 inhibitor (K_d values are 80 and 190 nM, respectively). Also inhibits DCAMKL2, PLK4 and TNK1 (K_d 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.

Product Specifications for XMD 8-92

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

3 2 1 Recalculate

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

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 13 publications citing the usage of this product.

• Lin ERK5 kinase activity is dispensable for cellular immune response and proliferation. Proc.Natl.Acad.Sci.U.S.A. 2016 PMID: 27679845
• Erazo 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. 2013 PMID: 23428871
• Yang and Lee Targeting the BMK1 MAP kinase pathway in cancer therapy. Clin.Cancer Res. 2011 PMID: 21385929
• Deng 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. 2011 PMID: 21412406
• Yang Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein. Cancer Cell 2010 PMID: 20832753

Product Documents for XMD 8-92