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Formula | C15H17IN2O2S.HCl |
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Molecular Weight | 452.74 | CAS No. | 110448-33-4 | |
Solubility (25°C)* | In vitro | DMSO | 46 mg/mL (101.6 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | 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. | ||||||
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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]. |
Cell Assay:[2] |
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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]
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 |
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.