ML-7 hydrochloride |
| カタログ番号GC11411 |
ML-7 hydrochlorideは選択性のミオシン軽鎖キナーゼ(IC50 = 300nM)である。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 110448-33-4
Sample solution is provided at 25 µL, 10mM.
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ML-7 hydrochlorideは選択性のミオシン軽鎖キナーゼ(IC50 = 300nM)である[1]。ML-7 hydrochlorideはミオシン軽鎖キナーゼ（MLCK）のATP結合活性を競合的に阻害し、よってMLCのリン酸化を阻害し、細胞骨格、収縮と移動行動を調節する[2]。ML-7 hydrochlorideは細胞生物学、腫瘍学と血管生理学の研究に使われる[3-4]。
白血球で、ML-7 hydrochloride (20μM；24時間)の処理は、敗血症の患者の好中球で、リソソーム媒介の細胞死を誘発する[5]。クレブシエラ・ニューモニエで、ML-7 hydrochloride (64μg/mL；24時間)の処理は、チゲサイクリンの殺傷活性を増強できる[6]。oeFOXP2細胞で、ML-7 hydrochloride (40μM；48時間)の投与は、細胞の増殖を著しく増やした[7]。
Lewis肺癌細胞皮下腫瘍マウスモデルで、ML-7 hydrochloride (0.25mg/kg; ip; 7d)で事前処理した腫瘍は、溶媒対照物で事前処理された腫瘍よりも著しく小さかった[8]。トリメリット酸無水物で処理されたマウスモデルで、ML-7 hydrochloride (1mg/kg; ip; 5d)の注射は、固定化ストレスによる引っ掻き行動の悪化を著しく阻害した[9]。
References:
[1]. Simoes RL, Fierro IM. Involvement of the Rho-kinase/myosin light chain kinase pathway on human monocyte chemotaxis induced by ATL-1, an aspirin-triggered lipoxin A4 synthetic analog. The Journal of Immunology. 2005 Aug 1; 175(3): 1843-1850.
[2]. Ran Q, Li A, Tan Y, et al. Action and therapeutic targets of myosin light chain kinase, an important cardiovascular signaling mechanism. Pharmacological Research. 2024 Jun 27: 107276.
[3]. Xiong Y, Wang C, Shi L, et al. Myosin light chain kinase: a potential target for treatment of inflammatory diseases. Frontiers in pharmacology. 2017 May 23; 8: 292.
[4]. Gu LZ, Hu WY, Antic N, et al. Inhibiting myosin light chain kinase retards the growth of mammary and prostate cancer cells. European journal of cancer. 2006 May 1; 42(7): 948-957.
[5]. Wu J, Barkat MQ, Su J, et al. Inhibition of non-muscular myosin light chain kinase accelerates the clearance of inflammatory cells by promoting the lysosome-mediated cell death. Biomedicine & Pharmacotherapy. 2024 Jan 1; 170: 115986.
[6]. Sun L, Sun L, Li X, et al. A novel tigecycline adjuvant ML-7 reverses the susceptibility of tigecycline-resistant Klebsiella pneumoniae. Frontiers in Cellular and Infection Microbiology. 2022 Jan 5; 11: 809542.
[7]. Chang S. Effect of forkhead box protein P2-mediated activation of myosin light-chain kinase on the invasion and migration of endometrial cancer cells. CytoJournal. 2025 May 14; 22: 54.
[8]. Kim YE, Gwak SH, Hong BJ, et al. Effects of ultra-high doserate FLASH irradiation on the tumor microenvironment in Lewis lung carcinoma: role of myosin light chain. International Journal of Radiation Oncology* Biology* Physics. 2021 Apr 1;109(5):1440-1453.
[9]. Cho DE, Hong JP, Kim Y, et al. Role of gut-derived bacterial lipopolysaccharide and peripheral TLR4 in immobilization stress-induced itch aggravation in a mouse model of atopic dermatitis. Scientific reports. 2024 Mar 15; 14(1): 6263.
| 細胞実験[1]: | |
細胞株 | 白血球 |
準備方法 | 分離液境界の白血球層を採取し、PBSで三回洗浄した。細胞ペレットをRPM1640培地で再懸濁し、polyLでコーティングされたグラススライドに播種した。TUNELまたは免疫蛍光染色のために、ML-7 hydrochloride (20μM)または溶媒で培養した0時間または24時間後に細胞を採取した。 |
反応条件 | 20μM；24時間 |
アプリケーション | ML-7 hydrochlorideの処理は、敗血症の患者の好中球で、リソソーム媒介の細胞死を誘発する。 |
| 動物実験 [2]: | |
動物モデル | Lewis肺癌細胞皮下腫瘍マウスモデル |
準備方法 | 体内実験で、Lewis肺癌（LLC）細胞を6週齢の雄C57BL/6マウスに皮下移植し、腫瘍のサイズが約150mm2に達した時、放射線で照射した。ML-7処理について、15 Gy IRの前、LLC腫瘍を負うマウスにML-7 (0.25mg/kg)または溶媒を7日間、毎日腹腔内注射した。 |
投与形態 | 0.25mg/kg；腹腔内注射；7日間 |
アプリケーション | ML-7 hydrochlorideで事前処理した腫瘍は、溶媒対照物で事前処理された腫瘍よりも著しく小さかった。 |
References: | |
| Cas No. | 110448-33-4 | SDF | |
| Chemical Name | 1-((5-iodonaphthalen-1-yl)sulfonyl)-1,4-diazepane hydrochloride | ||
| Canonical SMILES | IC1=CC=CC2=C1C=CC=C2S(N3CCCNCC3)(=O)=O.Cl | ||
| Formula | C15H18ClIN2O2S | M.Wt | 452.74 |
| 溶解度 | ≥ 15.95 mg/mL in DMSO, ≥ 8.82 mg/mL in Water with ultrasonic and warming | Storage | Store at 2-8°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. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.2088 mL | 11.0439 mL | 22.0877 mL |
| 5 mM | 441.8 μL | 2.2088 mL | 4.4175 mL |
| 10 mM | 220.9 μL | 1.1044 mL | 2.2088 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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