ML-7 HCl

製品コードS8388 バッチS838801

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

C15H17IN2O2S.HCl
分子量 452.74 CAS No. 110448-33-4
Solubility (25°C)* 体外 DMSO 90 mg/mL (198.78 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
4.5mg/ml
5% DMSO 95% Corn oil
0.56mg/ml
* <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 ML-7 is an inhibitor of smooth muscle myosin light chain kinase (MLCK) with a Ki value of 0.3 µM and displays reversible, ATP-competitive inhibition of Ca2+-calmodulin-dependent and -independent smooth muscle MLCKs. ML-7 also inhibits PKA and PKC with Ki of 21 μM and 42 μM, respectively.
in vitro Inhibition of MLCK by ML-7 induces activation of caspase-3 in adherent MCF-10A and MCF-10A Ras-transformed cells[2]. Its treatment results in a dose-dependent decrease in MLC20 phosphorylation and a corresponding increase in cell death of SMC(smooth muscle cells). The inhibitory effect of ML-7 on MLCK is highly selective. The Ki of ML-7 for MLCK is 0.3 μM, while its Ki for protein kinase A is 21 μM and for protein kinase C is 42 μM. Overexpressing Bcl-2 can protect cells against apoptosis induced by ML-7[4].
in vivo ML7 is able to improve Vascular endothelial dysfunction(VED) and atherosclerosis(AS) by regulating the expression of the tight junction (TJ) proteins zona occludens (ZO)-1 and occludin via mechanisms involving MLCK and MLC phosphorylation in high-fat diet-fed rabbits. ML7 decreases the expression of MLCK and MLC phosphorylation in the arterial wall of rabbits fed a high-fat diet and reduces lipid deposition lesions in AS rabbits[1].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 MCF-10A cells, MDCK cells
濃度 40 μM
反応時間 16 h
実験の流れ Cells are treated with vehicle alone, Blebbistatin, ML-7, ML-9, latrunculin A or Y-27632 in media without serum at varying concentrations and time points before being fixed or prepared for FACS analysis. Untreated cells are also serum starved for the duration of the inhibitor treatment. Stock solutions of each agent are made in DMSO (50 μM Blebbistatin, 5 mM LA), 50% ethanol (10 mM ML-7), 70% ethanol (20 mM ML-9) or water (20 mM Y-27632) and are maintained at -20°C.
動物実験 動物モデル New Zealand white rabbits
投薬量 1 mg/kg/day
投与方法 oral administration

カスタマーフィードバック

Data from [Data independently produced by , , Blood, 2013, 122(4):580-9]

Data from [Data independently produced by , , FASEB J, 2018, doi:10.1096/fj.201800343R]

Data from [Data independently produced by , , Biomed Pharmacother, 2017, 92:810-818]

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：

Fluoride disrupts intestinal epithelial tight junction integrity through intracellular calcium-mediated RhoA/ROCK signaling and myosin light chain kinase [ Ecotoxicol Environ Saf, 2023, 257:114940] PubMed: 37099960
High extracellular glucose promotes cell motility by modulating cell deformability and contractility via the cAMP-RhoA-ROCK axis in human breast cancer cells [ Mol Biol Cell, 2023, 34(8):ar79] PubMed: 37195739
TREM-2 promotes Th1 responses by interacting with the CD3ζ-ZAP70 complex following Mycobacterium tuberculosis infection [ Nat Commun, 2022, 13(1):1768] PubMed: 35365657
Brain-Derived Neurotrophic Factor regulates LYN kinase mediated Myosin Light Chain Kinase activation to modulate non-muscle myosin II activity in hippocampal neurons [ J Biol Chem, 2022, S0021-9258(22)00494-X] PubMed: 35598826
HO-1/CO Maintains Intestinal Barrier Integrity through NF-κB/MLCK Pathway in Intestinal HO-1-/- Mice [ Oxid Med Cell Longev, 2021, 2021:6620873] PubMed: 34104309
Somatostatin receptor 5 is critical for protecting intestinal barrier function in vivo and in vitro [ Mol Cell Endocrinol, 2021, 535:111390] PubMed: 34224803
Kindlin-2 promotes rear focal adhesion disassembly and directional persistence during cell migration [ J Cell Sci, 2021, 134(1)jcs244616] PubMed: 33277381
Phosphorylated‑myosin light chain mediates the destruction of small intestinal epithelial tight junctions in mice with acute liver failure [ Mol Med Rep, 2021, 23(5)392] PubMed: 33760163
MICAL2 is a novel nucleocytoplasmic shuttling protein promoting cancer invasion and growth of lung adenocarcinoma. [ Cancer Lett, 2020, 28;483:75-86] PubMed: 32360180
Activation of the RhoA-YAP-β-catenin Signaling Axis Promotes the Expansion of Inner Ear Progenitor Cells in 3D Culture [ Stem Cells, 2020, 11] PubMed: 32159914

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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