LY-411575 is a selective, cell permeable gamma-secretase inhibitor with IC50 of 0.082 nM for cell-based γ-secretase. LY-411575 decreased overall thymic cellularity and impaired intrathymic differentiation at the CD4(-)CD8(-)CD44(+)CD25(+) precursor stage. LY-411575 reduces Aβ/42 after acute or chronic treatment, and blocks Notch activation. Treatment with LY-411575 (LSN-411575) arrests KrasG12V-driven NSCLCs in association with inhibition of HES1 expression and ERK phosphorylation.
|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 60 mg/mL|
Critical role of soluble amyloid-β for early hippocampal hyperactivity in a mouse model of Alzheimer's disease.
Busche MA, et al. Proc Natl Acad Sci U S A. 2012 May 29;109(22):8740-5. PMID: 22592800.
Chronic treatment with the gamma-secretase inhibitor LY-411,575 inhibits beta-amyloid peptide production and alters lymphopoiesis and intestinal cell differentiation.
Wong GT, et al. J Biol Chem. 2004 Mar 26;279(13):12876-82. PMID: 14709552.
|Related Gamma-secretase Products|
PF-03084014 (Nirogacestat) is a potent and selective γ-secretase inhibitor with IC50 of 6.2 nM.
YO-01027 (Dibenzazepine, DBZ) is a dipeptidic γ-secretase inhibitor with IC50 of 2.6 nM and 2.9 nM for APPL and Notch cleavage, respectively.
LY900009 is a potent Notch inhibitor with IC50 of 0.27 nM.
LY3039478 is a novel and orally bioavailable inhibitor of Notch-1 intracellular domain (N1ICD) cleavage with IC50 of ~1 nM.
FLI-06 is a novel inhibitor of Notch signaling with EC50 of 2.3 μM.
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