XMD17-109 ERK5-IN-1

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Chemical Information

Product name：XMD17-109 ERK5-IN-1	Purity：98% min
CAS NO：1435488-37-1	Solubility：DMSO : ≥ 100 mg/mL (156.54 mM)
Molecular Formula：C₃₆H₄₆N₈O₃	Package：Package according to customer requirements
Molecular Weight：638.802	Storage：Store at -20℃

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Remarks

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[1]. 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.

Chemical Name:

11-cyclopentyl-2-[2-ethoxy-4-[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]anilino]-5-methylpyrimido[4,5-b][1,4]benzodiazepin-6-one

ERK Inhibitors Related Products:

BIX02189; Resveratrol; SCH772984; Pluripotin; VX-11e; DEL-22379; Ulixertinib; Ravoxertinib; XMD8-92; Bosutinib; ONC-201 ; AZD-0364

References

[1]. Deng X, et al. Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones. Eur J Med Chem. 2013;70:758-67.

[2]. Elkins, Jonathan M., et al. X-ray Crystal Structure of ERK5 (MAPK7) in Complex with a Specific Inhibitor. Journal of Medicinal Chemistry (2013), 56(11), 4413-4421.