SC79

Catalog No.S7863

SC79 Chemical Structure

Molecular Weight(MW): 364.78

SC79 is a brain-penetrable Akt phosphorylation activator and an inhibitor of Akt-PH domain translocation.

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Cited by 29 Publications

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Biological Activity

Description SC79 is a brain-penetrable Akt phosphorylation activator and an inhibitor of Akt-PH domain translocation.
Targets
Akt [1]
In vitro

SC79 suppresses PHAKTM-GFP plasma membrane translocation, and enhances phosphorylation of all three Akt isoforms in HEK293, HeLa, HL60, NB4, and HsSulton (B cells) cells. SC79 reduces neuronal excitotoxicity and prevents stroke-induced neuronal death. [1] SC79 restores proliferation of BRAT1 knockdown cells, and reduces the production of superoxide in mitochondria of MitoSox positive cells. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A549 M{\zXmFxd3C2b4Ppd{Bie3OjeR?= NYXrW5JvPSEQvH3vcE9N NEPORoNUSzhyIHLsc4NseyC4aYTlfIlvNWmwZIXj[YQh[XCxcITvd4l{ MlTpN|A4QTd{M{[=
HeLa M4\XN2Z2dmO2aX;uJIF{e2G7 M1e4XoRm[3KnYYPl[EB1cGViboXtZoVzKG:oIHH1eI9xcGGpb4PvcYV{KGmwZIXj[YQh[nliSG\KMWUhcW5iY3XscJM> NGTufFQ{ODV|NECwNS=>
SH-SY5Y M{TVSGZ2dmO2aX;uJIF{e2G7 NEXlepEyOCEQvF2= M2LCWlMxKG2rbh?= MoTDdJJmNXS{ZXH0cYVvfCC5aYToJHNEPzliKEGwJO69VSlibHHy[4VtgSCjdITlcpVifGWmIFiyU|IucW6mdXPl[EB{fXK4aY\hcEBz\WS3Y4Tpc44> NHixTHUzQTV4MEC5Oy=>
Sertoli M1f1c2Z2dmO2aX;uJIF{e2G7 NYDN[5dLPS534pEJxtVO NYLSTWFpOzBibXnu M2[2OZVxNXKnZ4XsZZRmKHSqZTDQSm9UNWmwZIXj[YQh\G:5bj3y[Yd2dGG2aX;uJI9nKHBvQXv0NUBVOzB6IHHu[EBxNUGtdEGgV|Q4Ow>? NHXKeFMzQDR|OUC2Oy=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-mTOR / mTOR / pAKT / AKT / P62 / Bcl-2 / Bax / LC3 / Cleaved PARP ; 

PubMed: 30301881     


C643 and KHM-5M cells were treated by apatinib (20 μM) implement with or without SC79 (4 μg/ml) for 24 h, respectively. Total AKT, phosphorylated AKT, total mTOR, phosphorylated AKT, P62, Bcl-2, Bax, LC3, cleaved-PARP, and GAPDH were detected by western blot. Densitometry represents the expression of the proteins relative to GAPDH. 

p-Akt / Akt / p-GSK3β / GSK3β / β-catenin / Cyclin D1; 

PubMed: 30556279     


The relative expression levels of phosphorylated Akt308, Akt, phosphorylated GSK-3b, GSK-3b, bcatenin, and cyclin D1 with respective control cells. GAPDH was used as a loading control.

p4EBP1 / 4EBP1 / pS6 / RPS6 / ESRP1 / ESRP2; 

PubMed: 28420690     


Western blot analyses of the phosphorylation pattern of proteins involved downstream of the AKT signaling pathway in epithelial-like MCF-7 cells transfected with control siRNAs or siRNAs targeting ESRP1 and ESRP2 and treated, or not, for 1 h with SC79 (AKT kinase activator). The p4EBP1(70) and p4EBP1(37&46) antibodies recognize phosphorylated residues on position 70, 37 and/or 46 of the E4BP1 protein. The pS6 antibody recognizes phosphorylated RPS6 protein. H3 (histone H3) is used as a loading control. 

30301881 30556279 28420690
In vivo In the permanent focal cerebral ischemia mouse model, SC79 (0.04 mg/g, i.p.) enables the cytosolic activation of Akt, and recapitulates the primary cellular function of Akt signaling, resulting in augmented neuronal survival. [1]

Protocol

Kinase Assay:

[1]

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Cytosolic phosphorylation of Akt:

Hela cells are serum starved for 1 hr and treated with IGF (100ng/mL) or SC79 (4 μg/mL) for 30 minutes. Cells are lysed in Lysis buffer containing 250 mM Sucrose, 20 mM HEPES, 10 mM KCl, 1.5 mM MgCl2, 1 mM EDTA, 1 mM EGTA supplemented with protease inhibitors. Cells are passed through 25G needle several times and kept on ice for 20 minutes. Total cell lysate is taken at this point. Cell lysates are centrifuged at 100,000g for 30 minutes. Supernatant is collected as the cytosolic fraction. Pellet is washed with lysis buffer and represents the membrane fraction. Total cell lysate, cytosolic and membrane fractions are resolved by SDS-PAGE and analyzed for phospho-Akt (S473), Total Akt, Tubulin (cytosolic marker) and Orai1 (membrane marker) by western blotting.
Cell Research:

[1]

+ Expand
  • Cell lines: HsSultan and NB4 cells
  • Concentrations: 8 μg/mL
  • Incubation Time: 24 h
  • Method:

    HsSultan or NB4 cells (2.5 × 105) are plated in a 24-well plate in 500 μL of phenol red-free RPMI medium supplemented with 10% FBS. After incubation for 24 hours, each compound (8 µg/mL) is added and cultured for overnight (16–20 h). Fifty microliters of MTT solution (5 mg/mL in PBS) are added to each well. Following 2 hrs incubation, the purple formazan crystals are dissolved by directly adding in 500 μL of isopropanol with 0.1 M HCl to each well. After clearing the cell debris by centrifugation, the absorbance is measured at a wavelength of 570 nm.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: Permanent focal cerebral ischemia mouse model
  • Formulation: DMSO
  • Dosages: 0.04 mg/g
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 72 mg/mL (197.37 mM)
Ethanol 72 mg/mL warmed (197.37 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+corn oil
For best results, use promptly after mixing.
5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 364.78
Formula

C17H17ClN2O5

CAS No. 305834-79-1
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID