Solanesol mainly accumulates in solanaceous crops, including tobacco, tomato, potato, eggplant, and pepper plants. Solanesol binds at ATP binding site and inhibit the phosphorylation of Focal Adhesion Kinase (FAK). Solanesol upregulates HO-1 and Hsp70 expression in L02 cells which activate Nrf2 and HSF1. It induces Nrf2 by enhancement of Keap1 interaction with Hsp90. Solanesol-activated HSF1 is involved in chaperones interaction.
|Cell lines||human hepatic cell L02|
|Preparation method||Cell viability is determined by MTT assays.
Cells are seeded into 96-well plates (5 × 104 cells/well) 24 h before treatment. The cells are then treated with various concentrations of solanesol followed by incubating with 5 mg/ml of MTT working solution for 4 h at 37 °C. After being treated with 100 μL of DMSO to dissolve the crystals, the cells are detected under an Microplate Reader to measure the absorbance at 570 nm.
|Concentrations||10, 50, 100, 250, 500, 1000 μM|
|Incubation time||12 h|
|Animal models||Male albino rats|
|Formulation||Gelling agent Carbopol-934|
|Dosages||0.2 g of gel containing solanesol (1 % w/v)|
|Administration||applied to the plantar surface of the right hind paw by gently rubbing with the index finger|
|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.
|Solubility||Soluble in Chloroform|
|Related FAK Products|
BI-4464 is a novel highly selective ATP competitive inhibitor of PTK2/FAK with IC50 of 17 nM, it is also a PTK2 ligand for PROTAC.
Defactinib hydrochloride is an orally bioavailable, small-molecule focal adhesion kinase (FAK) inhibitor with potential antiangiogenic and antineoplastic activities.
GSK2256098 is a potent, selective, reversible, and ATP competitive FAK kinase inhibitor with apparent Ki of 0.4 nM.
Y15 is a novel small molecule FAK phosphorylation inhibitor; specifically block phosphorylation of Y397-FAK and total phosphorylation of FAK.
PF-431396 is a dual PYK2/FAK inhibitor with IC50 of 11 nM and 2 nM, respectively.
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