Spautin-1 is a potent and specific autophagy inhibitor, and inhibits the deubiquitinating activity of USP10 and USP13 with IC50 of ∼0.6-0.7 μM. In Bcap-37 cells, Spautin-1 dramatically enhanced cell death in glucose-free media and induces apoptotic morphology. In PDGF-treated cells, spautin-1 stabilizes α-smooth muscle cell actin and calponin, prevents actin filament disorganization, diminishes production of extracellular matrix, and abrogates VSMC hyperproliferation and migration. Spautin-1 also specifically reduces infectious dengue virus titers in BHK-21 cells. In contrast, co-treatment with Spautin-1 increased IM-induced inhibition of cell viability with IC50 of 0.45 μM.
|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|
Spautin-1, a novel autophagy inhibitor, enhances imatinib-induced apoptosis in chronic myeloid leukemia.
Shao S, et al. Int J Oncol. 2014 May;44(5):1661-8. PMID: 24585095.
PDGF-mediated autophagy regulates vascular smooth muscle cell phenotype and resistance to oxidative stress.
Salabei JK, et al. Biochem J. 2013 May 1;451(3):375-88. PMID: 23421427.
Inhibition of cellular autophagy deranges dengue virion maturation.
Mateo R, et al. J Virol. 2013 Feb;87(3):1312-21. PMID: 23175363.
Beclin1 controls the levels of p53 by regulating the deubiquitination activity of USP10 and USP13.
Liu J, et al. Cell. 2011 Sep 30;147(1):223-34. PMID: 21962518.
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