ML-7 HCl

Catalog No.S8388

For research use only.

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.

ML-7 HCl Chemical Structure

CAS No. 110448-33-4

Selleck's ML-7 HCl has been cited by 11 Publications

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Choose Selective MLCK Inhibitors

Biological Activity

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.
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[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].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Vero cells NXnsdmIzSW62aY\pdoFtKGG|c3H5 M{e3OFMh\GG7cx?= M{G4fmFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGRmdme3ZTD2bZJ2eyCrbn\lZ5Rm\CCrbjDh[pJq[2GwIHfy[YVvKG2xbnvlfUBX\XKxIHPlcIx{KGGmbXnubZN1\XKnZDDh[pRmeiC4aYLhcEBkcGGubHXu[4Uh[W[2ZYKgN{Bl[Xm|IHL5JJZqemGuIIDsZZF2\SCjc4PhfS=> M2T0WVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5M{[wOlc3Lz5zN{O2NFY4PjxxYU6=
neural precursor cells NU[yPVRITnWwY4Tpc44h[XO|YYm= M3nYdGlvcGmkaYTpc44hd2ZibnX1do9{eGincnWgdJJwdGmoZYLheIlwdiCxZjDtc5V{\SCwZYXyZYwheHKnY4Xyd49zKGOnbHzzJIJ6KE2WVDDhd5NigQ>? M2TEcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NEG3OlMyLz5zN{SxO|Y{OTxxYU6=
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].

Protocol (from reference)

Cell Research:[2]
  • Cell lines: MCF-10A cells, MDCK cells
  • Concentrations: 40 μM
  • Incubation Time: 16 h
  • Method: 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.

Solubility (25°C)

In vitro

DMSO 90 mg/mL
(198.78 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 452.74
Formula

C15H17IN2O2S.HCl

CAS No. 110448-33-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CNCCN(C1)S(=O)(=O)C2=CC=CC3=C2C=CC=C3I.Cl

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00190242 Completed Drug: group1|Drug: group2 HIV Infection Assistance Publique - Hôpitaux de Paris|Ensemble contre le SIDA|GlaxoSmithKline June 2003 Phase 3

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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