ML-7 HCl

Catalog No.S8388 Batch:S838801

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Technical Data

Formula

C15H17IN2O2S.HCl
Molecular Weight 452.74 CAS No. 110448-33-4
Solubility (25°C)* In vitro DMSO 90 mg/mL (198.78 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
5% DMSO 95% Corn oil
0.56mg/ml
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
4.5mg/ml
* <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.)

Preparing Stock Solutions

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].
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 Assay:[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.

Customer Product Validation

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]

Selleck's ML-7 HCl has been cited by 16 publications

Regulatory effects of the p38 mitogen-activated protein kinase-myosin light chain kinase pathway on the intestinal epithelial mechanical barrier and the mechanism of modified Pulsatilla decoction in the treatment of ulcerative colitis [ J Tradit Chin Med, 2024, 44(5):885-895] PubMed: 39380219
Suppression of non-muscle myosin II boosts T cell cytotoxicity against tumors [ Sci Adv, 2024, 10(44):eadp0631] PubMed: 39485850
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

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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.