NSC117079
目录号 : GC36774
NSC117079是新型的 PHLPP 抑制剂。
Cas No.:500363-63-3
Sample solution is provided at 25 µL, 10mM.
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NSC117079 is a novel PHLPP inhibitor. PHLPP[1]
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].
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].
[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
Animal experiment: | 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 ?M) 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]. |
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. | |
| Cas No. | 500363-63-3 | SDF | |
| Canonical 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 | ||
| 分子式 | C20H15N3O7S2 | 分子量 | 473.48 |
| 溶解度 | DMSO: 50 mg/mL (105.60 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.112 mL | 10.5601 mL | 21.1202 mL |
| 5 mM | 0.4224 mL | 2.112 mL | 4.224 mL |
| 10 mM | 0.2112 mL | 1.056 mL | 2.112 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet