FRAX486

製品コードS7807 バッチS780701

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C25H23Cl2FN6O
分子量 513.39 CAS No. 1232030-35-1
Solubility (25°C)* 体外 DMSO 22 mg/mL (42.85 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 FRAX486 is a potent p21-activated kinase (PAK) inhibitor with IC50 values of 14, 33, 39 and 575 nM for PAK1, PAK2, PAK3 and PAK4 respectively.
in vitro In WPMY-1 cells, FRAX486 induces concentration-dependent (1-10 μM) degeneration of actin filaments. This was paralleled by attenuation of proliferation rate, being observed from 1 to 10 μM FRAX486. Cytotoxicity of FRAX486 in WPMY-1 cells is time- and concentration-dependent. In WPMY-1 cells, effects of FRAX486 on actin organization, survival, and proliferation occurred already at concentrations of 1-5 μM. In these concentrations, full inhibition of PAK1-3 may be expected, while PAK4 may be inhibited only partially[2].
in vivo FRAX486 crosses the blood-brain barrier and that therapeutically useful concentrations of FRAX486 are in the brain as early as 1 h and remain as long as 24 h after administration, with the maximum concentration in the target tissue at 8 h. Daily dosing results in steady-state levels of FRAX486 in the brain. FRAX486 specifically rescues the Fmr1 KO abnormality in which the spine phenotype is present in apical neurons and not simply decreasing spine density irrespective of genotype or existence of a phenotype. Also, FRAX486 reduces hyperactivity and stereotypical movements, both of which are phenotypes that characterize the mouse model of Fragile X syndrome[3].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 WPMY-1 cells(an immortalized cell line obtained from nonmalignant human prostate stroma)
濃度 1, 5, 10 μM
反応時間 24, 48, 72 h
実験の流れ Cells are grown in 96-well plates (20,000 cells/well) for 24 h, before FRAX486, IPA3, or DMSO are added in indicated concentrations (1, 5, 10 μM). Subsequently, cells are grown for different periods (24, 48, 72 h). Separate controls are performed for each period. At the end of this period, 10 μl of [2-(2-methoxy-4-nitrophenyl)-3-(4-nitrophenyl)-5-(2,4-disulfophenyl)-2H-tetrazolium monosodium salt (WST-8) from CCK-8 is added, and absorbance in each well is measured at 450 nm after incubation for 2 h at 37°C.
動物実験 動物モデル Male C57BL/6 mice
投薬量 3 mg/kg(i.v.) or 30 mg/kg(p.o.)
投与方法 i.v. or p.o.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

PAK1 contributes to cerebral ischemia/reperfusion injury by regulating the blood-brain barrier integrity [ iScience, 2023, 26(8):107333] PubMed: 37529106
ERK phosphorylation is dependent on cell adhesion in a subset of pediatric sarcoma cell lines [ Biochim Biophys Acta Mol Cell Res, 2022, 1869(8):119264] PubMed: 35381293
Actionable Cytopathogenic Host Responses of Human Alveolar Type 2 Cells to SARS-CoV-2 [ Mol Cell, 2020, 80(6):1104-1122.e9] PubMed: 33259812
Src-Dependent DBL Family Members Drive Resistance to Vemurafenib in Human Melanoma. [ Cancer Res, 2019, 79(19):5074-5087] PubMed: 31416844
Elucidating essential kinases of endothelin signalling by logic modelling of phosphoproteomics data [ Mol Syst Biol, 2019, 15(8):e8828] PubMed: 31464372
Salmonella stimulates pro-inflammatory signalling through p21-activated kinases bypassing innate immune receptors. [ Nat Microbiol, 2018, 3(10):1122-1130] PubMed: 30224799
PAK4 crystal structures suggest unusual kinase conformational movements. [ Biochim Biophys Acta Proteins Proteom, 2018, 1866(2):356-365] PubMed: 28993291
Protein kinase D1 (PKD1) phosphorylation on Ser203 by type I p21-activated kinase (PAK) regulates PKD1 localization. [ J Biol Chem, 2017, 292(23):9523-9539] PubMed: 28408623
P21-activated kinase 1 regulates resistance to BRAF inhibition in human cancer cells [Babagana M Mol Carcinog, 2017, 56(5):1515-1525] PubMed: 28052407

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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