| Size | Price | Stock | Qty |
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| 5mg |
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| 25mg |
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Purity: ≥98%
SC79 is a novel, potent, selective, cell-permeable, and brain-penetrable activator of Akt phosphorylation with the potential to be used to enhance Akt activity in various physiological and pathological conditions, e.g. to prevent progressive neuronal death in neurological diseases. By interacting with the PH domain of Akt, SC79 inhibits the translocation of the Akt-PH (pleckstrin homology) domain and promotes Akt phosphorylation by upstream protein kinases. The cytosolic activation of Akt by SC79 is sufficient to recapitulate the primary cellular function of Akt signaling, resulting in increased neuronal survival, in a hippocampal neuronal culture system and a mouse model for ischemic stroke.
| Targets |
Akt
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|---|---|
| ln Vitro |
In HEK293, HeLa, HL60, NB4 and HsSulton (B cells) cells, SC79 reduces PHAKTM-GFP plasma membrane translocation and increases the phosphorylation of all three Akt isoforms. SC79 lessens neuronal excitotoxicity and stops the death of neurons brought on by stroke.[1] SC79 increases MitoSox-positive cells' ability to produce superoxide while decreasing the proliferation of BRAT1 knockdown cells.[2]
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| ln Vivo |
In the mouse model of permanent focal cerebral ischemia, SC79 (0.04 mg/g, i.p.) activates Akt in the cytosol and mimics the main cellular function of Akt signaling, increasing neuronal survival. [1]
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| Enzyme Assay |
Hela cells are serum starved for 1 hr and treated with IGF (100ng/mL) or SC79 (4 μg/mL) for 30 minutes. Protease inhibitors are added to the lysis buffer, which contains 250 mM sucrose, 20 mM HEPES, 10 mM KCl, 1.5 mM MgCl2, 1 mM EDTA, and 1 mM EGTA. Multiple passes of a 25G needle are made with the cells, which are then placed on ice for 20 minutes. At this point, the entire cell lysate is collected. Centrifuging cell lysates at 100,000 g for 30 minutes. The cytosolic fraction is obtained by collecting supernatant. The pellet, which represents the membrane fraction, is washed in lysis buffer. SDS-PAGE is used to separate the total cell lysate, cytosolic, and membrane fractions. Western blotting is then used to check for the presence of phospho-Akt (S473), total Akt, tubulin (a cytosolic marker), and Orai1 (a membrane marker).
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| Cell Assay |
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. Each compound (8 µg/mL) is added after 24 hours of incubation, and it is then cultured for an overnight period (16–20 h). Each well receives 50 microliters of MTT solution (5 mg/mL in PBS). After 2 hours of incubation, 500 L of isopropanol with 0.1 M HCl are added directly to each well to dissolve the purple formazan crystals. At a wavelength of 570 nm, the absorbance is measured after removing the cell debris by centrifugation.
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| Animal Protocol |
Permanent focal cerebral ischemia mouse model
0.04 mg/g i.p. |
| References |
Proc Natl Acad Sci U S A.2012 Jun 26;109(26):10581-6.
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| Molecular Formula |
C17H17CLN2O5
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|---|---|---|
| Molecular Weight |
364.78
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| Exact Mass |
364.0826
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| Elemental Analysis |
C, 55.98; H, 4.70; Cl, 9.72; N, 7.68; O, 21.93
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| CAS # |
305834-79-1
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
CCOC(=O)C1=C(OC2=C(C1C(C#N)C(=O)OCC)C=C(C=C2)Cl)N
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| InChi Key |
DXVKFBGVVRSOLI-UHFFFAOYSA-N
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| InChi Code |
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
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| Chemical Name |
ethyl 2-amino-6-chloro-4-(1-cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate
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| Synonyms |
SC79; SC-79; SC 79
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 72 mg/mL (~197.4 mM)
Water: <1 mg/mL Ethanol: 72 mg/mL (~197.4 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (13.71 mM) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.85 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.85 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.5 mg/mL (6.85 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL corn oil and mix evenly. Solubility in Formulation 5: 2% DMSO+corn oil: 5mg/mL |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Loss of BRAT1 leads to inhibition of Akt activity and Akt activation by SC79 partially restores BRAT1 knockdown cells. BMC Cancer. 2014 Jul 29;14:548. doi: 10.1186/1471-2407-14-548. |
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