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ML-7 HCl MLCK inhibitor

Name: ML-7 HCl
Brand: Selleck Chemicals
SKU: S8388
Availability: InStock
Rating: 5 (22 reviews)

Cat.No.S8388

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.

Chemical Structure

Molecular Weight: 452.74

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Quality Control

Batch: Purity: 99.89%

99.89

Related Targets	Akt Wnt/beta-catenin HSP PKC ROCK Microtubule Associated Integrin Bcr-Abl Actin FAK
Other MLCK Inhibitors	2,3-Butanedione-2-monoxime Sevasemten

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
Vero cells	Antiviral assay	3 days	Antiviral activity against Dengue virus infected in african green monkey Vero cells administered after viral challenge after 3 days by viral plaque assay	17360676
neural precursor cells	Function assay		Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay	17417631
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 90 mg/mL (198.78 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.500mg/ml (9.94mM)
	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.560mg/ml (1.24mM)
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	452.74	Formula	C₁₅H₁₇IN₂O₂S.HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	110448-33-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1CNCCN(C1)S(=O)(=O)C2=CC=CC3=C2C=CC=C3I.Cl

Mechanism of Action

Targets/IC₅₀/Ki	MLCK (Cell-free assay) 0.3 μM(Ki) PKA (in Ehrlich cells) 21 μM PKC (in Ehrlich cells) 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] https://pubmed.ncbi.nlm.nih.gov/26096176/ [2] https://pubmed.ncbi.nlm.nih.gov/16723733/ [3] https://pubmed.ncbi.nlm.nih.gov/3108259/ [4] https://pubmed.ncbi.nlm.nih.gov/15988034/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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