SC79, a unique specific and BBB permeable Akt activator, activates Akt in the cytosol and inhibits Akt membrane translocation. SC79 specifically binds to the PH domain of Akt.
IC50&Target
Akt
体外研究
SC79 augmentes Akt phosphorylation at both the Thr308 and S473 sites.
SC79 (10.96 μM) induces cytosolic phosphorylation of Akt. SC79 enhances IGF1-induced Akt phosphorylation in both serum-starved cells and cells grown in serum-rich medium.
SC79 reduces neuronal excitotoxicity and prevents stroke-induced neuronal death. SC79 suppresses PHAKTM-GFP plasma membrane translocation.
SC79 restores proliferation of BRAT1 knockdown cells, and reduces the production of superoxide in mitochondria of MitoSox positive cells.
SC79 upregulates FLIPL/S expression and consequently suppresses caspase-8 activation.
Western Blot Analysis
Cell Line:
HeLa cells.
Concentration:
4 μg/mL (10.96 μM).
Incubation Time:
30 min.
Result:
Induced cytosolic phosphorylation of Akt.
体内研究
SC79 treatment, even at much high dose (0.4 mg/g of body weight), does not induce any detectable changes in body weight, survival rate, appearance, and behavior in mice.
SC79 (10 mg/kg, i.p.) Protects C57BL/6 mice from fas-induced fulminant hepatic failure.
SC79 protects hepatocytes from TNFα-mediated apoptosis and mice from Gal/LPS-induced liver injury and damage.
Animal Model:
Male, age-matched (6- to 8-weekeold) C57BL/6 or BALB/c mice weighing 16 to 18 g.
Dosage:
10 mg/kg.
Administration:
Intraperitoneally at 0.5 hour before the i.p. administration of an agonistic anti-Fas Jo2 antibody at a lethal dose of 0.5 and 0.4 mg/kg for C57BL/6 and BALB/c mice, respectively.
Result:
Treatment of mice with 10 mg/kg of SC79 at 0.5 hour before Jo2 injection increased mouse survival at 12 hours after Jo2 injection from 0% to 35%, and no additional mortality was observed to the end of the 2-month observation period.
Animal Model:
Male, age-matched (6 to 8 weeks old) C57BL/6 mice weighing 16-18 g.
Dosage:
10 mg/kg.
Administration:
Intraperitoneally at 0.5 h before i.p. administration of 400 mg/kg of D-galactosamine (D-Gal) and 60 µg/kg of lipopolysaccharide (LPS) for C57BL/6 mice.
Result:
Gal/LPS challenge there was more bleeding on the liver of the vehicle control-treated mice as compared to that of SC79-treated mice.
A single dose of SC79 significantly reduced Gal/LPS-mediated liver damage but not an infiltration of inflammatory cells in liver sections.
分子式
C17H17ClN2O5
分子量
364.78
CAS号
305834-79-1
运输条件
Room temperature in continental US; may vary elsewhere.