Application
XMD8-92 has been used as a specific extracellular signal regulated kinase 5 (ERK5) inhibitor in human umbilical vein endothelial cells (HUVECs) culture.
Biochem/physiol Actions
XMD8-92 is a potent and selective inhibitor of BMK1/ERK5/MAPK7 and DCAMKL1 (DCLK1), kinases implicated in tumorigenesis. XMD8-92 has a Kd of 80 nM for ERK5 and a Kd of 97 nM for DCAMKL1. The next closest targets are DCAMKL2 (190 nM), TNK1 (890 nM), and PLK4 (600 nM). Through inhibition of BMK1 activity, XMD8-92 blocked tumor cell proliferation in vitro in a wide variety of cancer cell lines and significantly inhibited tumor growth in vivo by 95% in mouse studies. XMD8-92 inhibited AsPC-1 human pancreatic cancer cell proliferation and pancreatic tumor xenograft growth via a DCLK1-dependent mechanism.
Other Notes
XMD8-92 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the XMD8-92 probe summary on the Chemical Probes Portal website.
Packaging
5, 25 mg in glass bottle
| Colour | white to beige |
|---|---|
| Quality Level | 100 |
| InChI key | QAPAJIZPZGWAND-UHFFFAOYSA-N |
| InChI | 1S/C26H30N6O3/c1-4-35-23-15-17(32-13-11-18(33)12-14-32)9-10-20(23)28-26-27-16-22-24(29-26)30(2)21-8-6-5-7-19(21)25(34)31(22)3/h5-10,15-16,18,33H,4,11-14H2,1-3H |
| Manufacturer | SIGMA-ALDRICH |
| Solubility | DMSO: 25 mg/mL, clear |
| Form | powder |
| Assay | ≥98% (HPLC) |
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