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XMD8-85 (ERK5-IN-1)

Cat. No. M20811
XMD8-85 (ERK5-IN-1) Structure
Size Price Availability Quantity
5mg USD 150  USD150 In stock
10mg USD 205  USD205 In stock
25mg USD 400  USD400 In stock
50mg USD 600  USD600 In stock
100mg USD 800  USD800 In stock
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Quality Control & Documentation
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.

References

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


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