ML-9

Names

[ Name ]:
ML-9

[Synonym ]:
1H-1,4-Diazepine, 1-[(5-chloro-1-naphthalenyl)sulfonyl]hexahydro-, hydrochloride (1:1)
1-[(5-Chloro-1-naphthyl)sulfonyl]-1,4-diazepane hydrochloride (1:1)
1-(5-chloronaphthalen-1-yl)sulfonyl-1,4-diazepane,hydrochloride
MFCD00065525

Biological Activity

[Description]:

ML-9 is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity[3]. ML-9 inhibits inhibits MLCK, PKA and PKC activity with Ki values of 4, 32 and 54 μM, respectively[1]. ML-9 induces autophagy by stimulating autophagosome formation and inhibiting their degradation[3].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Cytoskeleton >> Myosin

[In Vitro]

ML9 (0-100 μM; 0-24 hours) has no reduction in cardiomyocyte viability, 50-100 μM significantly induces cell death[2]. ML9 (50 μM; 1-4 hours) significantly increases cleaved caspase-3 levels, decreased STIM1 protein levels by about 42%[2]. Cell Viability Assay[1] Cell Line: Neonatal rat ventricular myocytes (NRVM) cells Concentration: 0, 10, 50 and 100 μM Incubation Time: 0, 1, 4, 8 and 24 hours Result: Decreased cell viability at 50-100 μM concentration. Apoptosis Analysis[1] Cell Line: Neonatal rat ventricular myocytes (NRVM) cells Concentration: 50 μM Incubation Time: 1, 4 and 8 hours Result: Induced cardiomyocyte death through necrosis and apoptosis.

[References]

[1]. Ito S, et al. ML-9, a myosin light chain kinase inhibitor, reduces intracellular Ca2+ concentration in guinea pig trachealis.Eur J Pharmacol. 2004 Feb 23;486(3):325-33.

[2]. Shaikh S, et al. The STIM1 inhibitor ML9 disrupts basal autophagy in cardiomyocytes by decreasing lysosome content.Toxicol In Vitro. 2018 Apr;48:121-127.

[3]. Kondratskyi A1, et al.Identification of ML-9 as a lysosomotropic agent targeting autophagy and cell death.Cell Death Dis. 2014 Apr 24;5:e1193.

Chemical & Physical Properties

[ Boiling Point ]:
508.8ºC at 760mmHg

[ Melting Point ]:
196-200ºC

[ Molecular Formula ]:
C₁₅H₁₈Cl₂N₂O₂S

[ Molecular Weight ]:
361.287

[ Flash Point ]:
261.5ºC

[ Exact Mass ]:
360.046600

[ PSA ]:
57.79000

[ LogP ]:
4.62670

[ Vapour Pressure ]:
1.79E-10mmHg at 25°C

MSDS

Click to get detail MSDS

Safety Information

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

[ Hazard Codes ]:
Xi

[ RIDADR ]:
NONH for all modes of transport

[ HS Code ]:
2933990090

Customs

[ HS Code ]: 2933990090

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Articles

Modulation of macrophage phenotype by cell shape.

Proc. Natl. Acad. Sci. U. S. A. 110(43) , 17253-8, (2013)

Phenotypic polarization of macrophages is regulated by a milieu of cues in the local tissue microenvironment. Although much is known about how soluble factors influence macrophage polarization, relati...

Calcium-Dependent Isoforms of Protein Kinase C Mediate Posttetanic Potentiation at the Calyx of Held

Neuron 70(5) , 1005-19, (2011)

High-frequency stimulation leads to a transient increase in the amplitude of evoked synaptic transmission that is known as posttetanic potentiation (PTP). Here we examine the roles of the calcium-depe...

Linalyl acetate as a major ingredient of lavender essential oil relaxes the rabbit vascular smooth muscle through dephosphorylation of myosin light chain.

J. Cardiovasc. Pharmacol. 48(1) , 850-6, (2006)

In a preliminary experiment, we found that lavender essential oil relaxes vascular smooth muscle. Thus, the present experiments were designed to investigate the relaxation mechanism of linalyl acetate...