Y-39983 Dihydrochloride

製品コードS7935 バッチS793502

印刷

化学情報

Chemical Structure Synonyms Y-33075 Dihydrochloride Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C16H16N4O.2HCl
分子量 353.25 CAS No. 173897-44-4
Solubility (25°C)* 体外 DMSO 70 mg/mL (198.15 mM)
Water 70 mg/mL (198.15 mM)
Ethanol 3 mg/mL (8.49 mM)
* <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.

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生物活性

製品説明 Y-39983 (Y-33075) Dihydrochloride is a selective rho-associated protein kinase(ROCK) inhibitor with an IC50 of 3.6 nM.
in vitro

Y-39983 opposes ROCK-dependent phosphorylation of MYPT1 predominantly at Thr853 with a corresponding decrease in MLC phosphorylation. It reduces the phosphorylation at Thr696 and Thr853 and leads to reduced actomyosin contraction. Y-39983 shows an IC50 of ~200 nM for dephosphorylation at Thr696 and only 15 nM for dephosphorylation at Thr853. The IC50 for dephosphorylation of MLC is 14 nM[3].
in vivo

Y-39983 significantly suppresses clinical symptoms of EAE and prevents its relapse while increasing the amount of myelin proteins. Its treatment results in reduced demyelination with no significant change in axonal damage, which may be due to the inactivation of ROCK substrates, including phosphorylated (p)-MLC, LIMK2 and CRMP-2, which are important for neurite outgrowth, growth cone collapse and remyelination of oligodendrocytes[2].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Human glaucomatous trabecular meshwork (GTM3) cell line
濃度 5 μM
反応時間 1 h
実験の流れ

Cell cultures of an immortalized human glaucomatous trabecular meshwork (GTM3) cell line are grown at 37℃ in 5% CO2 in Dulbecco's Minimum Essential Medium (DMEM + Glutamax) supplemented with 10% fetal bovine serum and 10 μg/ml of gentamicin. Upon reaching confluence, cells are divided using 0.05% trypsin. Cells of passages 13 to 20 are used in experiments. Cells are treated with 5 μM of the specific ROCK inhibitors, Y-27632 and Y-39983, for 1 h in a serum-rich medium. Cell lysate is used for western blotting to test effect of ROCK inhibitors on the phosphorylation of MYPT1 and MLC.
動物実験 動物モデル SJL/J mice
投薬量 100 μl of 10 μM
投与方法 i.p.

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：

Effects of Rho-Associated Kinase (Rock) Inhibitors (Alternative to Y-27632) on Primary Human Corneal Endothelial Cells [ Cells, 2023, 12(9)1307] PubMed: 37174707
The Global Phosphorylation Landscape of SARS-CoV-2 Infection [ Cell, 2020, 182(3):685-712.e19] PubMed: 32645325
The Global Phosphorylation Landscape of SARS-CoV-2 Infection [ Cell, 2020, 182(3):685-712.e19] PubMed: 32645325
Simulated microgravity inhibits the viability and migration of glioma via FAK/RhoA/Rock and FAK/Nek2 signaling. [ In Vitro Cell Dev Biol Anim, 2019, 55(4):260-271] PubMed: 30820814
Phosphorylation of ARHGAP19 by CDK1 and ROCK regulates its subcellular localization and function during mitosis. [ J Cell Sci, 2018, 131(5)] PubMed: 29420299

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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