SC 79Akt activator CAS# 305834-79-1 |
Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 305834-79-1 | SDF | Download SDF |
| PubChem ID | 2810830 | Appearance | Powder |
| Formula | C17H17ClN2O5 | M.Wt | 364.78 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 100 mM in DMSO | ||
| Chemical Name | ethyl 2-amino-6-chloro-4-(1-cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate | ||
| SMILES | CCOC(=O)C1=C(OC2=C(C1C(C#N)C(=O)OCC)C=C(C=C2)Cl)N | ||
| Standard InChIKey | DXVKFBGVVRSOLI-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C17H17ClN2O5/c1-3-23-16(21)11(8-19)13-10-7-9(18)5-6-12(10)25-15(20)14(13)17(22)24-4-2/h5-7,11,13H,3-4,20H2,1-2H3 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Activator of Akt; binds to the pleckstrin homology domain of Akt. Enhances Akt phosphorylation by upstream protein kinases; also enables cytosolic activation of Akt. Shown to suppress excitotoxicity-induced neuronal death in vitro and in vivo. Exhibits brain penetrance. |
SC 79 Dilution Calculator
SC 79 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.7414 mL | 13.7069 mL | 27.4138 mL | 54.8276 mL | 68.5345 mL |
| 5 mM | 0.5483 mL | 2.7414 mL | 5.4828 mL | 10.9655 mL | 13.7069 mL |
| 10 mM | 0.2741 mL | 1.3707 mL | 2.7414 mL | 5.4828 mL | 6.8534 mL |
| 50 mM | 0.0548 mL | 0.2741 mL | 0.5483 mL | 1.0966 mL | 1.3707 mL |
| 100 mM | 0.0274 mL | 0.1371 mL | 0.2741 mL | 0.5483 mL | 0.6853 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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IC50: N/A
SC 79 is an activator of Akt. Akt/PKB with anti-apoptotic activity (a serine/threonine protein kinase) is one of the major downstream targets of PtdIns P3 signaling pathway.
In vitro: SC79 was identified by a cell-based high-throughput chemical genetic screening, and inhibits Akt membrane translocation. However, Akt was paradoxically activated by SC79in the cytosol, specifically binding to the PH domain of Akt. The conformation of SC79-bound Akt is favorable for phosphorylation by upstream protein kinases. In a mouse model and a hippocampal neuronal culture system for ischemic stroke, the result of augmented neuronal survival is attained, based on the cytosolic activation of Akt by SC79, which is sufficient to recapitulate the primary cellular function of Akt signaling. Thus, SC79, a unique specific Akt activator, may be applied to enhance Akt activity in various physiological and pathological conditions.
In vivo: In aqueous environment, SC79 is relatively unstable. Intriguingly, however, the sustained level of phosphorylated Akt was observed both in cell culture and in vivo after the removal of SC79, indicating that SC79 may act irreversibly. The chemical moieties of SC79 (i.e., nitrile group) could be modified and/or reacts with amino acids. Nevertheless, SC79, a relatively safe drug, was revealed by following fact. Assignment of SC79 treatment much high dose (0.4 mg/g of body weight) did not accelerate any detectable changes in body weight (survival rate, appearance, and behavior) in mice. Achievement of neuronal protective effect by i.p. injection suggests that SC79 also has a good penetration of blood–brain barrier. SC79 can be applied as a chemical platform to develop novel drugs for neurological and other complications
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Jo H, Mondal S, Tan D, Nagata E, Takizawa S, Sharma AK, Hou Q, Shanmugasundaram K, Prasad A, Tung JK, Tejeda AO, Man H, Rigby AC, Luo HR. 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.
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Small molecule-induced cytosolic activation of protein kinase Akt rescues ischemia-elicited neuronal death.[Pubmed:22689977]
Proc Natl Acad Sci U S A. 2012 Jun 26;109(26):10581-6.
Elevating Akt activation is an obvious clinical strategy to prevent progressive neuronal death in neurological diseases. However, this endeavor has been hindered because of the lack of specific Akt activators. Here, from a cell-based high-throughput chemical genetic screening, we identified a small molecule SC79 that inhibits Akt membrane translocation, but paradoxically activates Akt in the cytosol. SC79 specifically binds to the PH domain of Akt. SC79-bound Akt adopts a conformation favorable for phosphorylation by upstream protein kinases. In a hippocampal neuronal culture system and a mouse model for ischemic stroke, the cytosolic activation of Akt by SC79 is sufficient to recapitulate the primary cellular function of Akt signaling, resulting in augmented neuronal survival. Thus, SC79 is a unique specific Akt activator that may be used to enhance Akt activity in various physiological and pathological conditions.
