产品描述:
XMD17-109 is a selective ERK5 inhibitor (IC50 = 0.162 µM in an enzyme assay).{42420} It is selective for ERK5 over a panel of more than 200 kinases, inhibiting only ERK5 with greater than 90% target occupancy at a concentration of 10 µM. XMD17-109 inhibits ERK5 phosphorylation (IC50 = 0.09 µM in HeLa cells) and decreases AP-1 transcriptional activity (EC50 = 4.2 µM).{42421} It also inhibits human recombinant LRRK2[G2019S], which contains a mutation that has been linked to Parkinson’s disease, with an IC50 value of 0.339 µM in an enzyme assay.{42420}