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XMD8-85 (ERK5-IN-1)

Cat. No. M20811
XMD8-85 (ERK5-IN-1) Structure
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Biological Activity

XMD8-85 (ERK5-IN-1) is a selective and potent inhibitor of ERK5 and LRRK2 with IC50s of 0.162 μM and 0.339 μM, respectively.

Chemical Information
Molecular Weight 459.54
Formula C25H29N7O2
CAS Number 1234479-76-5
Solubility (25°C) DMSO 92 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.


[1] Zheng-Da Pang, et al. Biochem Pharmacol. AMPK upregulates KCa2.3 channels and ameliorates endothelial dysfunction in diet-induced obese mice

[2] Kaoru Arakaki, et al. Biomed Res. Increased expression of EGR1 and KLF4 by polysulfide via activation of the ERK1/2 and ERK5 pathways in cultured intestinal epithelial cells

[3] Mengyan Zhang, et al. Pathol Res Pract. Cancer-associated fibroblasts promote cell growth by activating ERK5/PD-L1 signaling axis in colorectal cancer

[4] Pamela A Lochhead, et al. Nat Commun. Paradoxical activation of the protein kinase-transcription factor ERK5 by ERK5 kinase inhibitors

[5] Fang Wang, et al. J Exp Clin Cancer Res. Reversal of ABCB1-related multidrug resistance by ERK5-IN-1

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Keywords: XMD8-85 (ERK5-IN-1) supplier, ERK, inhibitors, activators

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