Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C15H17IN2O2S |
| Molecular Weight | 416.277 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
IC1=CC=CC2=C(C=CC=C12)S(=O)(=O)N3CCCNCC3
InChI
InChIKey=GEHJIACZUFWBTK-UHFFFAOYSA-N
InChI=1S/C15H17IN2O2S/c16-14-6-1-5-13-12(14)4-2-7-15(13)21(19,20)18-10-3-8-17-9-11-18/h1-2,4-7,17H,3,8-11H2
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/3108259
Sources: https://www.ncbi.nlm.nih.gov/pubmed/3108259
1-(5-iodonaphthalene-1-sulfonyl)-1H-hexahydro-1,4-diazepine (ML-7) is an inhibitor of myosin light chain kinase (MLCK). It is widely used to study MLCK signaling both in vitro and in vivo.
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/16515842
Curator's Comment: ML-7 is CNS active in animals. No human data available.
Originator
Sources: https://www.ncbi.nlm.nih.gov/pubmed/3108259
Curator's Comment: 1987
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL3062 Sources: https://www.ncbi.nlm.nih.gov/pubmed/3108259 |
0.3 µM [Ki] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Unknown Approved UseUnknown |
|||
| Primary | Unknown Approved UseUnknown |
|||
| Primary | Unknown Approved UseUnknown |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Association of aorta intima permeability with myosin light chain kinase expression in hypercholesterolemic rabbits. | 2011-01 |
|
| Murine vasa recta pericyte chloride conductance is controlled by calcium, depolarization, and kinase activity. | 2010-11 |
|
| MDR1 function is sensitive to the phosphorylation state of myosin regulatory light chain. | 2010-07-16 |
|
| TRPC-mediated actin-myosin contraction is critical for BBB disruption following hypoxic stress. | 2010-06 |
|
| Cellular mechanisms of IL-17-induced blood-brain barrier disruption. | 2010-04 |
|
| Inhibition of myosin light chain kinase reduces brain edema formation after traumatic brain injury. | 2010-02 |
|
| Inhibition of myosin light chain phosphorylation decreases rat mesenteric lymphatic contractile activity. | 2009-08 |
|
| [Protective effect of myosin light-chain kinase inhibitor on acute lung injury]. | 2009-04 |
|
| Myosin light-chain kinase contributes to the proliferation and migration of breast cancer cells through cross-talk with activated ERK1/2. | 2008-11-08 |
|
| Myosin phosphorylation triggers actin polymerization in vascular smooth muscle. | 2008-11 |
|
| Dual role for myosin II in GLUT4-mediated glucose uptake in 3T3-L1 adipocytes. | 2008-10-15 |
|
| Extracellular matrix rigidity promotes invadopodia activity. | 2008-09-09 |
|
| In vivo phosphorylation of regulatory light chain of myosin II in sea urchin eggs and its role in controlling myosin localization and function during cytokinesis. | 2008-02 |
|
| Investigation into the signal transduction pathway via which heat stress impairs intestinal epithelial barrier function. | 2007-11 |
|
| The participation of the Na+-Ca2+ exchanger in primary cardiac myofibroblast migration, contraction, and proliferation. | 2007-11 |
|
| Myosin light chain kinase-independent inhibition by ML-9 of murine TRPC6 channels expressed in HEK293 cells. | 2007-09 |
|
| Inhibition of the myosin light chain kinase prevents hypoxia-induced blood-brain barrier disruption. | 2007-07 |
|
| Phospholipase C and myosin light chain kinase inhibition define a common step in actin regulation during cytokinesis. | 2007-05-17 |
|
| Calcium absorption by Cav1.3 induces terminal web myosin II phosphorylation and apical GLUT2 insertion in rat intestine. | 2007-04-15 |
|
| Organized migration of epithelial cells requires control of adhesion and protrusion through Rho kinase effectors. | 2007-03 |
|
| Myosin inhibitors block accumulation movement of chloroplasts in Arabidopsis thaliana leaf cells. | 2007 |
|
| Myosin light chain kinase is not a regulator of synaptic vesicle trafficking during repetitive exocytosis in cultured hippocampal neurons. | 2006-11-08 |
|
| Intracellular signal transduction for migration and actin remodeling in vascular smooth muscle cells after sphingosylphosphorylcholine stimulation. | 2006-09 |
|
| Thrombin-induced contraction in alveolar epithelial cells probed by traction microscopy. | 2006-08 |
|
| An MLCK-dependent window in late G1 controls S phase entry of proliferating rodent hepatocytes via ERK-p70S6K pathway. | 2006-07 |
|
| Myosin light chain kinase plays a role in the regulation of epithelial cell survival. | 2006-06-01 |
|
| Inhibiting myosin light chain kinase retards the growth of mammary and prostate cancer cells. | 2006-05 |
|
| Actin and non-muscle myosin II facilitate apical exocytosis of tear proteins in rabbit lacrimal acinar epithelial cells. | 2005-10-15 |
|
| Aluminium causes variable responses in actin filament cytoskeleton of the root tip cells of Triticum turgidum. | 2005-10 |
|
| Myosin 2 is a key Rho kinase target necessary for the local concentration of E-cadherin at cell-cell contacts. | 2005-10 |
|
| Effects of ML-7 and Y-27632 on carbachol- and endothelin-1-induced contraction of bovine trabecular meshwork. | 2005-06 |
|
| The inositol trisphosphate pathway mediates platelet-activating-factor-induced pulmonary oedema. | 2005-05 |
|
| LPS-induced lung inflammation is linked to increased epithelial permeability: role of MLCK. | 2005-05 |
|
| Calcium transients regulate titin organization during myofibrillogenesis. | 2005-03 |
|
| Endothelial cell myosin light chain kinase (MLCK) regulates TNFalpha-induced NFkappaB activity. | 2005-02-01 |
|
| Key role of myosin light chain (MLC) kinase-mediated MLC2a phosphorylation in the alpha 1-adrenergic positive inotropic effect in human atrium. | 2005-01-01 |
|
| Non-muscle myosin II and myosin light chain kinase are downstream targets for vasopressin signaling in the renal collecting duct. | 2004-11-19 |
|
| Differential regulation of human lung epithelial and endothelial barrier function by thrombin. | 2004-11 |
|
| Modulation of acto-myosin contractility in skeletal muscle myoblasts uncouples growth arrest from differentiation. | 2004-08-01 |
|
| Myosin-mediated cytoskeleton contraction and Rho GTPases regulate laminin-5 matrix assembly. | 2004-02 |
|
| The catalytic domain of xPAK1 is sufficient to induce myosin II dependent in vivo cell fragmentation independently of other apoptotic events. | 2003-11-15 |
|
| Regulation of renin secretion through reversible phosphorylation of myosin by myosin light chain kinase and protein phosphatase type 1. | 1998-06 |
|
| Adherent neutrophils activate endothelial myosin light chain kinase: role in transendothelial migration. | 1998-05 |
|
| An essential role of myosin light-chain kinase in the regulation of agonist- and fluid flow-stimulated Ca2+ influx in endothelial cells. | 1998-03 |
|
| Inhibition of sandfly fever Sicilian virus (Phlebovirus) replication in vitro by antiviral compounds. | 1997-12-24 |
|
| ML-7 and W-7 facilitate thromboxane A2-mediated Ca2+ mobilization in rabbit platelets. | 1996-03-07 |
|
| Role of myosin phosphorylation and [Ca2+]i in myogenic reactivity and arteriolar tone. | 1995-11 |
|
| Naphthalenesulphonamides block neutrophil superoxide production by intact cells and in a cell-free system: is myosin light chain kinase responsible for these effects? | 1995-10-01 |
|
| Differentiation of human monoblastic leukemia U937 cells induced by inhibitors of myosin light chain kinase and prevention of differentiation by granulocyte-macrophage colony-stimulating factor. | 1993-04-16 |
|
| Diphosphorylation of platelet myosin ex vivo in the initial phase of activation by thrombin. | 1992-07-22 |
Sample Use Guides
The rabbits were fed a high‑fat diet supplemented with 1 mg/kg/day ML7.
Rats: 1 mg/kg ML-7 i.p.
Route of Administration:
Other
1-(5-iodonaphthalene-1-sulfonyl)-1H-hexahydro-1,4-diazepine hydrochloride (ML-7), induced Nitroblue tetrazolium reducing activity, lysozyme activity and morphological maturation of human monoblastic U937, THP-1 and promyelocytic HL-60 cells, but not of erythroblastic K562 cells.
40 uM ML-7 induces activation of caspase-3 in adherent MCF-10A and MCF-10A Ras-transformed cells.
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