Quercetin significantly down regulates myofibroblast differentiation and fibrotic markers, such as α-smooth muscle actin (α-SMA) and Collagen III (Col III), in both HCFs and HKCs. Collagen III secretion was reduced 80% in both HCFs and HKCs following Quercetin treatment.Furthermore, Quercetin reduced lactate production by HKCs to normal HCF levels. Quercetin down regulated TGF-βR2 and TGF-β2 expression in HKCs suggesting a significant link to the TGF-β pathway. Quercetin is a key regulator of fibrotic markers and ECM assembly by modulating cellular metabolism and TGF-β signaling. Quercetin strongly abrogated PI3K and Src kinases, mildly inhibited Akt1/2, and slightly affected PKC, p38 and ERK1/2. Quercetin or the combined use of adenosine diphosphate and thromboxane A(2) inhibitors abrogated platelet spreading on these surfaces to a similar extent. The inhibitory effect of quercetin on platelet kinases blocks early signaling events preventing a complete platelet spreading. PKC inhibitors H-7 and quercetin protect BPAEC from TNF induced injuries and PKC play an important role in EC activation by TNF.
|Animal models||Mice bearing LNCaP xenografts or PC-3 xenografts|
|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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 50 mg/mL|
Quercetin attenuates lactate production and extracellular matrix secretion in keratoconus.
McKay TB, et al. Sci Rep. 2015 Mar 11;5:9003. PMID: 25758533.
Effect of quercetin on platelet spreading on collagen and fibrinogen and on multiple platelet kinases.
Navarro-Núñez L, et al. Fitoterapia. 2010 Mar;81(2):75-80. PMID: 19686810.
[Inhibitory effects of protein kinase C inhibitors on tumor necrosis factor induced bovine pulmonary artery endothelial cell injuries].
Yu XB, et al. Yao Xue Xue Bao. 1996;31(3):176-81. PMID: 9206266.
|Related PI3K Products|
Parsaclisib (INCB050465) is a potent and selective PI3Kδ inhibitor, with an IC50 of 1 nM at 1 mM ATP.
740 Y-P is a potent and cell permeable PI3K activator.
GSK2292767 is a potent and selective PI3Kδ inhibitor.
Bimiralisib (PQR309) is an orally bioavailable inhibitor of PI3K and mTOR, with potential antineoplastic activity.
PIK-III (also known as VPS34-IN2) is a potent and selective inhibitor of VPS34 enzymatic activity, with IC50s of 18 nM and 1.2 μM for VPS34 and PI(3)Kδ, 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.