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NSC117079 

Cat. No.: HY-19819 Purity: 98.90%
Handling Instructions

NSC117079 is a novel PHLPP inhibitor.

For research use only. We do not sell to patients.

NSC117079 Chemical Structure

NSC117079 Chemical Structure

CAS No. : 500363-63-3

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 176 In-stock
Estimated Time of Arrival: December 31
5 mg USD 160 In-stock
Estimated Time of Arrival: December 31
10 mg USD 260 In-stock
Estimated Time of Arrival: December 31
25 mg USD 550 In-stock
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50 mg USD 950 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1600 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

NSC117079 is a novel PHLPP inhibitor.

IC50 & Target

PHLPP[1]

In Vitro

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[2].

In Vivo

A single intraarticular injection of the Phlpp inhibitor NSC117079 attenuates mechanical allodynia and slows articular cartilage degradation in joints with a destabilized meniscus. Animals treated with the Phlpp inhibitor seven weeks after injury maintain normal activity levels, while those in the control group travel shorter distances and are less active three months after the joint injury. NSC117079 also increases production of cartilage extracellular matrix components (glycosaminoglycans and aggrecan) in over 90% of human articular cartilage explants from osteoarthritis patients and increased phosphorylation of Phlpp1 substrates (AKT2, ERK1/2 and PKC) in human articular chondrocytes[1].

Molecular Weight

473.48

Formula

C₂₀H₁₅N₃O₇S₂

CAS No.

500363-63-3

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 150 mg/mL (316.80 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Mice[1]

Posttraumatic osteoarthritis is induced in male C57Bl/6 mice by surgically destabilizing the meniscus. Seven weeks after surgery, mice receive a single intra-articular injection of the PHLPP inhibitor NSC117079 (8 µM) or saline. Mechanical allodynia is measured with von Frey assays, mobility is tracked in an open field system, and cartilage damage is assessed histologically[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Product name:
NSC117079
Cat. No.:
HY-19819
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