[CAS NO. 110448-33-4] ML-7 HCl

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PRODUCTS SPECIFICATIONS [110448-33-4]

Catalog

SLK-S8388

Brand

Selleck

CAS

110448-33-4

DESCRIPTION [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

Concentration Volume Mass	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.

Targets

MLCK ^[3] (Cell-free assay)	PKA ^[4] (in Ehrlich cells)	PKC ^[4] (in Ehrlich cells)
0.3 μM(Ki)	21 μM	42 μM

In vitro

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.

References

[1] Cheng X, et al. Mol Med Rep. 2015, 12(3):4109-16.
[2] Connell LE, et al. J Cell Sci. 2006, 119(Pt 11):2269-81.
[3] Saitoh M, et al. J Biol Chem. 1987, 262(16):7796-801.
[4] Fazal F, et al. Mol Cell Biol. 2005, 25(14):6259-66.