SC 79 |
| Catalog No.GC11645 |
SC 79 is an activator of osmotic Akt phosphorylation in the brain and an inhibitor of AKT-PH domain translocation.
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Cas No.: 305834-79-1
Sample solution is provided at 25 µL, 10mM.
SC 79 is an activator of osmotic Akt phosphorylation in the brain and an inhibitor of AKT-PH domain translocation[1].
SC 79 enhances phosphorylation of all three Akt isotypes and enhances Akt activation in a variety of cell types[1]. Treatment of BRAT1 knockdown cells with Akt activator SC 79 can improve their proliferation and reduces mitochondrial ROS concentration[4]. In both SH-SY5Y cells and primary murine dopaminergic neurons, pre-treatment with SC 79 largely inhibited hydrogen peroxide (H2O2)-induced cell viability reduction, apoptosis and necrosis. SC 79 activated Akt in the neuronal cells, which was required for its neuroprotection against H2O2[5]. In primary murine osteoblasts and osteoblastic MC3T3-E1 cells, pretreatment with SC 79 significantly attenuated Dex-induced cell death. Further, Dex-induced mitochondrial permeability transition pore (mPTP) opening, cytochrome C release and apoptosis activation were dramatically alleviated with SC 79 pretreatment in above cells[6]. The protective role of SC 79 against H/R of hepatocytes or hepatic I/R injury is related to activation of phosphorylation of Akt, resulting in the decrease of pro-apoptotic protein of Bim, Bax, and Bad, and increase of the anti-apoptotic protein Bcl-2 and Bcl-xL induced by cell H/R and hepatic I/R injury[7].
SC 79 enhances Akt activity during neuronal cell death in an in vivo mouse model of ischemia, SC 79 attenuates stroke-induced neuron death[1]. SC 79 protects hepatocytes from apoptosis induced by agonistic anti-Fas antibody CH11 (for humans) or Jo2 (for mice) and significantly prolongs the survival of mice given a lethal dose of Jo2[2]. Akt activator SC 79 protects hepatocytes from TNF-α-induced apoptosis and protects mice from d-galactosamine (d-Gal)/lipopolysaccharide (LPS)-induced TNF-α-mediated liver injury and damage. SC 79 not only enhances the nuclear factor-κB (NF-κB) prosurvival signaling in response to TNF-α stimulation, but also increases the expression of cellular FLICE (FADD-like IL-1β-converting enzyme)-inhibitory protein L and S (FLIPL/S), which consequently inhibits the activation of procaspase-8[2].
References:
[1]: Jo H, Mondal S, et,al. Small molecule-induced cytosolic activation of protein kinase Akt rescues ischemia-elicited neuronal death. Proc Natl Acad Sci U S A. 2012 Jun 26;109(26):10581-6. doi: 10.1073/pnas.1202810109. Epub 2012 Jun 11. PMID: 22689977; PMCID: PMC3387065.
[2]: Liu W, Jing ZT, et,al. A Novel AKT Activator, SC79, Prevents Acute Hepatic Failure Induced by Fas-Mediated Apoptosis of Hepatocytes. Am J Pathol. 2018 May;188(5):1171-1182. doi: 10.1016/j.ajpath.2018.01.013. PMID: 29673487.
[3]: Jing ZT, Liu W, et,al. AKT activator SC79 protects hepatocytes from TNF-α-mediated apoptosis and alleviates d-Gal/LPS-induced liver injury. Am J Physiol Gastrointest Liver Physiol. 2019 Mar 1;316(3):G387-G396. doi: 10.1152/ajpgi.00350.2018. Epub 2019 Jan 10. PMID: 30629471.
[4]: So EY, Ouchi T. BRAT1 deficiency causes increased glucose metabolism and mitochondrial malfunction. BMC Cancer. 2014 Jul 29;14:548. doi: 10.1186/1471-2407-14-548. PMID: 25070371; PMCID: PMC4129107.
[5]: Xu Y, Gao YW, et,al. SC79 protects dopaminergic neurons from oxidative stress. Oncotarget. 2017 Dec 20;9(16):12639-12648. doi: 10.18632/oncotarget.23538. PMID: 29560097; PMCID: PMC5849161.
[6]: Li ST, Chen NN, et,al. SC79 rescues osteoblasts from dexamethasone though activating Akt-Nrf2 signaling. Biochem Biophys Res Commun. 2016 Oct 7;479(1):54-60. doi: 10.1016/j.bbrc.2016.09.027. Epub 2016 Sep 7. PMID: 27614310.
[7]: Zhou H, Yu Y,et,al. Protective Effects the Akt Activator SC79 in Hepatic Ischemia-Reperfusion Injury. Med Sci Monit. 2018 Jun 24;24:4346-4354. doi: 10.12659/MSM.911178. PMID: 29936516; PMCID: PMC6049012.
| Kinase experiment [1]: | |
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Preparation Method |
Hela cells were serum-starved for 1 h, treated with IGF or SC 79 (4 μg/mL) for 30 min, lysed in lysis buffer, supplemented with protease inhibitors, and analyzed for phospho-Akt by Western blotting |
|
Reaction Conditions |
SC 79 (4 μg/mL) for 30 min |
|
Applications |
SC 79, which inhibits PH AkT-GFP plasma membrane translocation but enhances Akt phosphorylation and activation in the cytosols |
| Cell experiment [1]: | |
|
Cell lines |
HsSultan and NB4 cells |
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Preparation Method |
SC 79(8 ug/mL) was added to HsSultan or NB4 cell medium and incubated overnight (16-20 h). |
|
Reaction Conditions |
8 ug/mL SC 79 for 16-20 h |
|
Applications |
SC 79 enhances phosphorylation of all three Akt isotypes and enhances Akt activation in a variety of cell types. |
| Animal experiment [1]: | |
|
Animal models |
MCAO mice |
|
Preparation Method |
SC 79 was administered by intraperitoneal injection at a concentration of 0.04mg/g body weight. |
|
Dosage form |
0.04mg/g SC 79 |
|
Applications |
SC 79 enhances Akt activity during neuronal cell death in an in vivo mouse model of ischemia, SC 79 attenuates stroke-induced neuron death. |
|
References: [1]. Jo H, Mondal S, et,al. Small molecule-induced cytosolic activation of protein kinase Akt rescues ischemia-elicited neuronal death. Proc Natl Acad Sci U S A. 2012 Jun 26;109(26):10581-6. doi: 10.1073/pnas.1202810109. Epub 2012 Jun 11. PMID: 22689977; PMCID: PMC3387065. |
|
| Cas No. | 305834-79-1 | SDF | |
| Chemical Name | ethyl 2-amino-6-chloro-4-(1-cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate | ||
| Canonical SMILES | CCOC(C(C(C(C(OCC)=O)=C1N)C2=C(O1)C=CC(Cl)=C2)C#N)=O | ||
| Formula | C17H17ClN2O5 | M.Wt | 364.78 |
| Solubility | ≥ 36.5mg/mL in DMSO | Storage | Store at -20°C,unstable in solution, ready to use. |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7414 mL | 13.7069 mL | 27.4138 mL |
| 5 mM | 0.5483 mL | 2.7414 mL | 5.4828 mL |
| 10 mM | 0.2741 mL | 1.3707 mL | 2.7414 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Related Biological Data
Activation of PFK1 and PFKFB3 is due to phosphorylation of AKT and AMPK. (F) Representative images of ARS and ALP staining in MC3T3-E1 cells after treatment with SC79 and PFK15.
MK-2206 dihydrochloride (GC16304) and SC79 (GC11645) were obtained from GLPBIO.
Clin Transl Med 13.9 (2023): e1369. PMID: 37649137 IF: 10.6002 -
Related Biological Data
SC79 partially rescued the inhibitory effect of proliferation and migration caused by the knockdown of HRL-SC. a, b Western blot analysis showed that SC79 increased expression of p-AKT.
The medium was replaced with the medium containing 5 μg/mL of SC79 (10 μM, GlpBio) in AKT activation experiments.
Stem Cell Res Ther 13.1 (2022): 1-16. PMID: 35765088 IF: 7.4996 -
Related Biological Data
Melatonin inhibits the AKT/mTOR signaling to reduce autophagy and the expression of fibrotic proteins in HSFs. (E) Treatment with SC79 to activate the AKT/mTOR signaling rescued the melatonin-decreased AKT/mTOR signaling and fibrotic protein expression in HSFs.
HSFs were treated with vehicle (DMSO) or 200 μM melatonin and/or 10 μM SC79 (Glpbio) for 24 h.
Bba-Mol Basis Dis (2023): 166887. PMID: 37739092 IF: 6.2001 -
Related Biological Data
CST1 enhances SERPINB2 expression via AKT signaling pathway in bronchial epithelial cells. (C) SC-79 has a positive effect on SERPINB2 expression (n = 2).
BEAS-2B cells were stimulated with or without cytokines IL-4, IL-13, and IL-17A,17 stimulated with or without house dust mite, treated with or without E64d, induced with SC-79 (4 μg/mL, AKT activator; GlpBio) or MK2206USA).
Allergy Asthma Immun 15.3 (2023): 374. PMID: 37075800 IF: 4.4 -
Related Biological Data
Rescue experiments were conducted to verify the mechanism of TOP2A regulating OC cell behavior. (a-c) after SC79 treatment of cells in the SH-TOP2A group, WB results suggested that the levels of p-AKT/AKT and p-mTOR/mTOR were increased.
Lyophilized SC79 (GC11645, Glpbio), an activator of AKT, was resuspended in 500 μL of DMSO at 20 μg/μL, followed by storage at −20°C for later use.
Cancer Biol Ther 25.1 (2024): 2325126. PMID: 38445610 IF: 3.5999
Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)
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