XMD17-109

Research use only, not for human use.

XMD17-109 is a novel, specific ERK-5 inhibitor with an EC50 4.2 uM in HEK293 cells.

XMD17-109 is a novel, specific ERK-5 inhibitor with an EC50 4.2 uM in HEK293 cells.

XMD17-109 (Compound 26) inhibits ERK5 biochemically with an IC50 of 0.162 ± 0.006 μM, and blocks pidermal growth factor induced ERK5 autophosphorylation with an EC50 of 0.09 ± 0.03 μM in cells. XMD17-109 also inhibits LRRK2[G2019S] with an IC50 of 339 nM. XMD17-109 demonstrats low nanomolar cellular activity judged by the significant dose-dependent reduction of mobility shifted phosphorylated ERK5 bands from sorbitol stimulated cells. XMD17-109 completely inhibits the ERK5-mediated AP1 transcriptional activity at 30 μM and has an EC50 of 4.2 μM.

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ERK5-IN-1

MAPK/ERK Signaling

ERK

ERK5

Cancer

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1435488-37-1

638.81

C36H46N8O3

>98% (HPLC)

Ethanol: 100 mg/mL (156.54 mM); DMSO: 100 mg/mL (156.54 mM)

CN1CCN(C2CCN(C(C3=CC(OCC)=C(NC4=NC=C5C(N(C6CCCC6)C(C=CC=C7)=C7C(N5C)=O)=N4)C=C3)=O)CC2)CC1

11-cyclopentyl-2-((2-ethoxy-4-(4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl)phenyl)amino)-5-methyl-5,11-dihydro-6H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6-one

(-20℃)

With Ice Pack

≥ 2 years