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.
|Solubility (25°C)||DMSO 92 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
 Zheng-Da Pang, et al. Biochem Pharmacol. AMPK upregulates KCa2.3 channels and ameliorates endothelial dysfunction in diet-induced obese mice
 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
 Mengyan Zhang, et al. Pathol Res Pract. Cancer-associated fibroblasts promote cell growth by activating ERK5/PD-L1 signaling axis in colorectal cancer
 Pamela A Lochhead, et al. Nat Commun. Paradoxical activation of the protein kinase-transcription factor ERK5 by ERK5 kinase inhibitors
 Fang Wang, et al. J Exp Clin Cancer Res. Reversal of ABCB1-related multidrug resistance by ERK5-IN-1
|Related ERK Products|
RLX-33 is a potent and selective blood-brain barrier permeable relaxin family peptide 3 (RXFP3) antagonist that also blocks relaxin 3 (Relaxin 3) -induced ERK1/2 phosphorylation. The IC50 phosphorylated RXFP3, ERK1 and ERK2 were 2.36μM, 7.82μM and 13.86μM, respectively. RLX-33 can block the increase of food intake in rats induced by RXFP3 selective agonist R3/I5. RLX-33 can be used in the study of metabolic syndrome.
WAY-340245 is a ERK inhibitor.
Ulixertinib hydrochloride (BVD-523 hydrochloride) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of <0.3 nM against ERK2.
Magnolin, a major component of Magnolia flos (Shin-Yi), inhibits the Ras/ERKs/RSK2 signaling axis by targeting the active pocket of ERK1 and ERK2 with IC50s of 87 nM and 16.5 nM, respectively.
Ravoxertinib hydrochloride (GDC-0994 hydrochloride) is an orally bioavailable inhibitor selective for ERK kinase activity with IC50 of 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.