| Size | Price | Stock | Qty |
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| 25mg |
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| 100mg |
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Purity: ≥98%
NSC117079 is a novel and potent PHLPP1 (Pleckstrin homology domain and leucine-rich repeat protein phosphatase 1) inhibitor. PHLPP1 inhibits protein kinase B (AKT) survival signaling in neurons. Small molecule pan-PHLPP inhibitors (selective for PHLPP1 and PHLPP2) may offer a translatable method to induce AKT neuroprotection. NSC-117079 at 30 μM induces neutrophil adhesion to plated fibrinogen from 9.0±2.4% to 27.0±8.0% and enhanced neutrophil adhesion caused by 50 ng/mL GM-CSF from 22.9±6.0% to 47.6±10.9%. Neutrophil adhesion is followed by neutrophil transendothelial migration. Results suggest that PHLPP inhibitor NSC-117079 is effective in preventing Akt from dephosphorylation in neutrophils, and Akt phosphatase PHLPP serves to attenuate neutrophil adhesion but not migration.
| ln Vitro |
Neutrophil adherence to plated fibrinogen was stimulated by NSC-117079 at 30 μM, increasing it from 9.0±2.4% to 27.0±8.0%. Similarly, 50 ng/mL GM-CSF induced neutrophil cell adhesion to 22.9± 6.0%, increasing it to 47.6±10.9%. Transendothelial migration of neutrophils occurs after neutrophil labeling. According to the findings, PHLPP NSC-117079 by itself can successfully stop Akt from becoming dephosphorylated in neutrophils, but PHLPP's Akt phosphatase can interfere with the migration of neutrophil markers [2].
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| ln Vivo |
In meniscally unstable joints, a single intra-articular injection of Phlpp twin NSC117079 reduces mechanical allodynia and interferes with joint damage. Seven weeks following injury, animals treated with Phlpp twins continued their regular activity levels, whereas three months following joint damage, animals with heart disease moved and walked less. More than 90% of human articular cartilage explants from osteoarthritis patients produce more cartilage extracellular matrix components (glucosamine antioxidants and aggregated proteins) when NSC117079 is added, and in human articular chondrocytes, Phlpp1 substrate increases the phosphorylation of substances (AKT2, ERK1/2, and PKC) [1].
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| References |
[1]. Jackson TC, et al. Pharmacological inhibition of pleckstrin homology domain leucine-rich repeat protein phosphatase is neuroprotective: differential effects on astrocytes. J Pharmacol Exp Ther. 2013 Nov;347(2):516-28.
[2]. Zhu X, et al. Regulation Of Neutrophil Adhesion And Migration By Ph Domain And Leucine Rich Repeat Protein Phosphatase. A35 RECENT ADVANCES IN PHAGOCYTE BIOLOGY / Thematic Poster Session / Sunday, May 20/8:15 AM-4:30 PM / Area G (Hall D, North Building, Lower Level), Moscone Center |
| Molecular Formula |
C20H15N3O7S2
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|---|---|
| Molecular Weight |
473.47900223732
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| CAS # |
500363-63-3
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| SMILES |
O=S(C(C(N)=C1C2=O)=CC(NC3=CC=CC(S(=O)(N)=O)=C3)=C1C(C4=C2C=CC=C4)=O)(O)=O
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| Synonyms |
NSC117079; NSC-117079; NSC 117079
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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 : ~50 mg/mL (~105.60 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.28 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.28 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. 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 of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1120 mL | 10.5601 mL | 21.1202 mL | |
| 5 mM | 0.4224 mL | 2.1120 mL | 4.2240 mL | |
| 10 mM | 0.2112 mL | 1.0560 mL | 2.1120 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.
 PHLPP inhibitor NSC117079 activates neuronal AKT.J Pharmacol Exp Ther. 2013 Nov;347(2):516-28. |
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 PHLPP inhibitors inactivate AKT/ERK and alter basal viability in astrocytes. PHLPP inhibitors protect cortical neurons from STS injury. |
 PHLPP inhibitor NSC45586 activates neuronal AKT.J Pharmacol Exp Ther. 2013 Nov;347(2):516-28. |
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