Shelf life (days): 1460.0
Formulation: A crystalline solid
Formal Name: 11-cyclopentyl-2-[[2-ethoxy-4-[[4-(4-methyl-1-piperazinyl)-1-piperidinyl]carbonyl]phenyl]amino]-5,11-dihydro-5-methyl-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one
Purity: ≥98%
Formula Markup: C36H46N8O3
Formula Weight: 638.8
CAS Number: 1435488-37-1
Notes: 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}
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