QS11 binds and inhibits the GTPase activating protein of ADP-ribosylation factor 1 (ARFGAP1), suggesting that QS11 modulates Wnt/β-catenin signaling through an effect on protein trafficking. QS11 (2.5 μM) activates the Super(8X)TOPFlash reporter 200-fold in the presence of Wnt-3a CM, whereas Wnt-3a treatment alone increases reporter activity 40-fold. QS11 increases reporter activity only 2-fold in the absence of Wnt-3a. QS11 shows potent activity (EC50=0.5 μM) with little cytotoxicity toward HEK293 and human primary fibroblast cells. QS11 effectively reduces in vitro migration of metastatic human breast cancer cells.
|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||10 mM in DMSO|
The perilipin-2 (adipophilin) coat of cytosolic lipid droplets is regulated by an Arf1-dependent mechanism in HC11 mouse mammary epithelial cells.
Pauloin A, et al. Cell Biol Int. 2016 Feb;40(2):143-55. PMID: 26399370.
Ascorbic Acid-Induced Cardiac Differentiation of Murine Pluripotent Stem Cells: Transcriptional Profiling and Effect of a Small Molecule Synergist of Wnt/β-Catenin Signaling Pathway.
Ivanyuk D, et al. Cell Physiol Biochem. 2015;36(2):810-30. PMID: 26021268.
Brevianamide F belongs to a class of naturally occurring 2,5-diketopiperazines.
Telotristat ethyl, also known as LX1606, is an oral serotonin synthesis inhibitor or peripheral tryptophan hydroxylase (TPH) inhibitor.
ML18 is Bombesin receptor subtype 3 (BRS-3) antagonist (IC50 = 4.8 μM).
Acecainide HCl, also known as N-acetylprocainamide and ASL 601, is the N-acetylated metabolite of procainamide.
Sematilide (CK-1752) hydrochloride is a novel class III antiarrhythmic agent.
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