[CAS NO. 500363-63-3] NSC117079

Name: NSC117079
Brand: Arctom Scientific
SKU: AS903721

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PRODUCTS SPECIFICATIONS [500363-63-3]

Fulfillment

Catalog

AS903721

Brand

Arctom Scientific

CAS

500363-63-3

DESCRIPTION [500363-63-3]

Overview

MDL	-
Molecular Weight	473.48
Molecular Formula	C20H15N3O7S2
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

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

Summary

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] .

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

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] .

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

Appearance

Solid

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 : 50 mg/mL ( 105.60 mM ; Need ultrasonic)

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.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (5.28 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (5.28 mM); Clear solution

* All of the co-solvents are available by MCE.