ML-7 hydrochloride

Names

[ Name ]:
ML-7 hydrochloride

[Synonym ]:
1-(5-Iodonaphthalene-1-sulfonyl)-1H-hexahydro-1,4-diazepine hydrochloride
ML-7 HYDROCHLORIDE
1H-1,4-Diazepine, hexahydro-1-[(5-iodo-1-naphthalenyl)sulfonyl]-, hydrochloride (1:1)
MFCD00065524
1-[(5-Iodo-1-naphthyl)sulfonyl]-1,4-diazepane hydrochloride (1:1)
ML-7 (hydrochloride)

Biological Activity

[Description]:

ML-7 hydrochloride is a naphthalene sulphonamide derivative, potently inhibits MLCK (IC50=300 nM) and TRPC6 channel (IC50>10 μM).

[Related Catalog]:

Signaling Pathways >> Cytoskeleton >> Myosin

Research Areas >> Cancer

[Target]

IC50: 300 nM (MLCK)[1]

[In Vitro]

ML-7 hydrochloride inhibits rabbit portal vein α1-adrenoceptor NSCC with IC50 of 0.8 μM[1]. The myosin light chain kinase (MLCK) inhibitor ML-7 hydrochloride (3 μ M and 10 μM) also attenuates the Dexmedetomidine (DMT)-induced contraction (p<0.05 versus control)[2].

[In Vivo]

In sham operated animals Evans Blue extravasation is not different between ML-7 hydrochloride and vehicle group (sham+vehicle: 0.26±0.02 OD/g; sham+ML-7: 0.26±0.02 OD/g). After CCI inhibition of MLCK with ML-7 results in a significant lower amount of intracerebral Evans Blue compared to vehicle treated animals (CCI+vehicle: 0.42±0.04 OD/g; CCI+ML-7: 0.35±0.05 OD/g, p=0.048)[3].

[Animal admin]

Mice[3] Mice are treated with intraperitoneal injection of the selective MLCK inhibitor ML-7 (1 mg/kg) or vehicle solution (0.9% NaCl,control group) 1 h prior to and 6 h after trauma. Hemispheric brain water content and neurological function are measured 24 h after controlled cortical impact (CCI) in animals randomized to: (i) vehicle+sham surgery, (ii) vehicle+CCI, (iii) ML-7+shamsurgery or (iv) ML-7+CCI (n=8 per group) and 15 min after CCI in animals randomized to: (i) vehicle+sham surgery, (ii) vehicle+CCI, (iii) ML-7+sham surgery or (iv) ML-7+CCI (n=6 per group). Mice are treated with intraperitoneal injection of the selective MLCK inhibitor ML-7 (1 mg/kg) or vehicle solution (0.9% NaCl, control group) 1 h prior to and 6 h after trauma. Evans Blue extravasation is determined 24 h after surgery in animals randomized to: (i) vehicle + CCI or (ii) ML-7+CCI (n=5 per group) and in animals randomized to (iii) vehicle + sham surgery or (iv) ML-7+sham surgery (n=6 per group). ICP is measured 24 h CCI and sham surgery.

[References]

[1]. Shi J, et al. Myosin light chain kinase-independent inhibition by ML-9 of murine TRPC6 channels expressed in HEK293cells. Br J Pharmacol. 2007 Sep;152(1):122-31.

[2]. Yu J, et al. Dexmedetomidine-Induced Contraction in the Isolated Endothelium-Denuded Rat Aorta Involves PKC-δ-mediated JNK Phosphorylation. Int J Med Sci. 2015 Sep 4;12(9):727-36.

[3]. Luh C, et al. Inhibition of myosin light chain kinase reduces brain edema formation after traumatic brain injury. J Neurochem. 2010 Feb;112(4):1015-25.

[Related Small Molecules]

(-)-Blebbistatin | Omecamtiv mecarbil (CK-1827452) | BTS | HA-100 | MLCK inhibitor peptide 18 | Mavacamten | ATM-3507 | MS-444

Chemical & Physical Properties

[ Boiling Point ]:
542.7ºC at 760 mmHg

[ Melting Point ]:
246-249ºC dec.

[ Molecular Formula ]:
C₁₅H₁₈ClIN₂O₂S

[ Molecular Weight ]:
452.738

[ Flash Point ]:
282ºC

[ Exact Mass ]:
451.982208

[ PSA ]:
57.79000

[ LogP ]:
4.57790

[ Storage condition ]:
-20℃

MSDS

Click to get detail MSDS

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

Articles

Myosin II controls cellular branching morphogenesis and migration in three dimensions by minimizing cell-surface curvature.

Nat. Cell Biol. 17(2) , 137-47, (2015)

In many cases, cell function is intimately linked to cell shape control. We used endothelial cell branching morphogenesis as a model to understand the role of myosin II in shape control of invasive ce...

Directional bleb formation in spherical cells under temperature gradient.

Biophys. J. 109 , 355-64, (2015)

Living cells sense absolute temperature and temporal changes in temperature using biological thermosensors such as ion channels. Here, we reveal, to our knowledge, a novel mechanism of sensing spatial...

MAPK3/1 (ERK1/2) and Myosin Light Chain Kinase in Mammalian Eggs Affect Myosin-II Function and Regulate the Metaphase II State in a Calcium- and Zinc-Dependent Manner.

Biol. Reprod. 92 , 146, (2015)

Vertebrate eggs are arrested at metaphase of meiosis II, a state classically known as cytostatic factor arrest. Maintenance of this arrest until the time of fertilization and then fertilization-induce...