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Catalog:
SLK-S8388
Brand:
Selleck
CAS:
110448-33-4
Overview
MDL
MFCD00065524
Molecular Weight
452.74
Molecular Formula
C15H17IN2O2S.HCl
SMILES
Cl.IC1=CC=CC2=C1C=CC=C2S(=O)(=O)N1CCCNCC1
For research use only.
Storage
3 years,-20°C,powder 1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
1 mg
5 mg
10 mg
1 mM
2.2088 mL
11.0439 mL
22.0877 mL
5 mM
0.4418 mL
2.2088 mL
4.4175 mL
10 mM
0.2209 mL
1.1044 mL
2.2088 mL
50 mM
0.0442 mL
0.2209 mL
0.4418 mL
Description
ML-7 is an inhibitor of with a value of 0.3 µM and displays reversible, ATP-competitive inhibition of Ca2+-calmodulin-dependent and -independent smooth muscle MLCKs. ML-7 also inhibits and with Ki of 21 μM and 42 μM, respectively.
Inhibition of MLCK by ML-7 induces activation of caspase-3 in adherent MCF-10A and MCF-10A Ras-transformed cells. 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.
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.
