Y-33075 (hydrochloride) (Synonyms: RKI-983, SNJ-1656, Y-39983) |
カタログ番号GC52274
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Y-33075 (hydrochloride)は有力なROCK（Rho関連のタンパク質キナーゼ）阻害剤であり、IC50値は3.6nMである。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 471843-75-1
Sample solution is provided at 25 µL, 10mM.
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Y-33075 (hydrochloride)は有力なROCK（Rho関連のタンパク質キナーゼ）阻害剤であり、IC50値は3.6nMである[1]。ROCKはAGC（PKA/PKG/PKC）ファミリーのキナーゼに属するセリン-トレオニンキナーゼであり、哺乳類、ゼブラフィッシュ、アフリカツメガエル、無脊椎動物とニワトリに存在している[2]。Y-33075 (hydrochloride)は、網膜神経節細胞（RGC）に神経保護作用を示す[3]。Y-33075 (hydrochloride)でアフリカツメガエルを処理し、繊毛上皮組織の恒常性を破壊し、尾部縁部で異常な上皮増殖を起こせる[4]。
体外で、FVB/NJマウスから分離された初代肝臓星状細胞（HSC）と不死化ヒト肝星細胞株（TWNT-4細胞）をY-33075 (hydrochloride)（10nM-10µM）で24時間処理した結果、活性化のHSCとTWNT-4細胞の収縮、線維症と増殖を著しく減らし、同時にマウスHSCの移動を著しく増やした[5]。Y-33075 (hydrochloride)（10nM）で活性化のLX-2細胞を処理した結果、ROCKとp-MLCの発見を下方制御し、cAMPとPKAの発見を上方制御した[6]。
References:
[1] Vercammen H, Ondra M, Kotulova J, et al. “Keep on ROCKIn”: Repurposed ROCK inhibitors to boost corneal endothelial regeneration[J]. Biomedicine & Pharmacotherapy, 2024, 174: 116435.
[2] Amin F, Ahmed A, Feroz A, et al. An update on the association of protein kinases with cardiovascular diseases[J]. Current Pharmaceutical Design, 2019, 25(2): 174-183.
[3] Reboussin É, Bastelica P, Benmessabih I, et al. Evaluation of Rho kinase inhibitor effects on neuroprotection and neuroinflammation in an ex-vivo retinal explant model[J]. Acta Neuropathologica Communications, 2024, 12(1): 150.
[4] Khan F, Pitstick L, Lara J, et al. Rho-Associated protein kinase activity is required for tissue homeostasis in the Xenopus laevis ciliated epithelium[J]. Journal of Developmental Biology, 2024, 12(2): 17.
[5] Bachtler N, Torres S, Ortiz C, et al. The non-selective Rho-kinase inhibitors Y-27632 and Y-33075 (hydrochloride) decrease contraction but increase migration in murine and human hepatic stellate cells[J]. PLoS One, 2023, 18(1): e0270288.
[6] Zeng R, Guo Y, Qi J, et al. Dantao formula alleviates hepatic fibrosis and portal hypertension via modulation of the cAMP/PKA/ROCK signaling pathway in hepatic stellate cells[J]. Journal of Ethnopharmacology, 2025: 120650.
| 細胞実験[1]: | |
細胞株 | FVB/NJマウスから単離された初代単離HSCと不死化ヒトHSC株TWNT-4 |
準備方法 | FVB/NJマウスから単離された初代単離HSCと不死化ヒトHSC株TWNT-4を培養活性化し、Y-27632とY-33075 (hydrochloride)（10nMから10μM）で24時間インキュベートした。タンパク質の発見レベルをウエスタンブロットで分析し、線維化促進マーカーと増殖マーカーの転写レベルをリアルタイムqPCRで評価した。移動を創傷治癒アッセイで調べた。増殖をBrdU法で評価した。 |
反応条件 | 10nM-10µM；24時間 |
アプリケーション | Rhoキナーゼ阻害剤であるY-27632とY-33075 (hydrochloride)は両方とも、活性化の初代マウスHSC（FVB/NJ）とヒトHSC株（TWNT-4）で収縮、線維形成と増殖を著しく減らした。Y-27632と比べ、Y-33075 (hydrochloride)は10倍増加した能力を示した。両方の阻害剤は、FVB/NJでHSCの遊離を、大幅で予想外に増やした。 |
References: | |
| Cas No. | 471843-75-1 | SDF | |
| 同義語 | RKI-983, SNJ-1656, Y-39983 | ||
| Canonical SMILES | O=C(C1=CC=C(C=C1)[C@H](N)C)NC2=C3C(NC=C3)=NC=C2.Cl | ||
| Formula | C16H16N4O • HCl | M.Wt | 316.8 |
| 溶解度 | DMSO: soluble | Storage | -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1566 mL | 15.7828 mL | 31.5657 mL |
| 5 mM | 631.3 μL | 3.1566 mL | 6.3131 mL |
| 10 mM | 315.7 μL | 1.5783 mL | 3.1566 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)