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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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Other Sizes |
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ML-9 HCl is a novel, potent and selective myosin light chain kinase (MLCK) inhibitor, also Akt kinase and and stromal interaction molecule 1 (STIM1). ML-9 enhances the anticancer activity of docetaxel, suggesting its potential application as an adjuvant to existing anticancer chemotherapy. By simultaneously inhibiting the Akt pathway and autophagy, ML-9 was found to have a complex effect on autophagy and to be a useful tool for targeting autophagy in cancer therapy.
ln Vitro |
While ML9 (0-100 μM; 0-24 hours) does not dramatically trigger cell death, it does significantly diminish the viability of cardiac cells [2]. ML9 (50 μM; 1-4 hours) dramatically raises the amounts of mitochondrial caspase-3, allowing
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Cell Assay |
cell viability assay [1]
Cell Types: Neonatal rat ventricular myocytes (NRVM) Cell Tested Concentrations: 0, 10, 50 and 100 μM Incubation Duration: 0, 1, 4, 8 and 24 STIM1 protein levels diminished by approximately 42% [2]. Hourly Experimental Results: diminished cell viability at concentrations of 50-100 μM. Apoptosis analysis[1] Cell Types: Neonatal rat ventricular myocytes (NRVM) Cell Tested Concentrations: 50 μM Incubation Duration: 1, 4 and 8 hrs (hours) Experimental Results: Induction of cardiomyocyte death via 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. |
Molecular Formula |
C15H18CL2N2O2S
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Molecular Weight |
361.28662
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Exact Mass |
360.0466
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Elemental Analysis |
C, 49.87; H, 5.02; Cl, 19.63; N, 7.75; O, 8.86; S, 8.88
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CAS # |
105637-50-1
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Related CAS # |
ML-9 Free Base;110448-31-2
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Appearance |
Solid powder
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SMILES |
C1CNCCN(C1)S(=O)(=O)C2=CC=CC3=C2C=CC=C3Cl.Cl
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InChi Key |
ZNRYCIVTNLZOGI-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C15H17ClN2O2S.ClH/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,3,8-11H21H
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Chemical Name |
1-(5-chloronaphthalen-1-yl)sulfonyl-1,4-diazepane;hydrochloride
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Synonyms |
ML9 HCl; ML-9 HCl; ML 9 HCl; ML-9 hydrochloride
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~83.33 mg/mL (~230.65 mM)
H2O : ≥ 5 mg/mL (~13.84 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.76 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.76 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.76 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.7679 mL | 13.8393 mL | 27.6786 mL | |
5 mM | 0.5536 mL | 2.7679 mL | 5.5357 mL | |
10 mM | 0.2768 mL | 1.3839 mL | 2.7679 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.