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                同义名:
                    
                        
                            
                                ML-7 (hydrochloride); ML-7 hydrochloride
                            
                        
                    
                
                
                
                    
                     
                    
                     
                
            
ML-7 HCl是一种多靶向 MLCK 抑制剂,Ki 值分别为 300 nM(MLCK)、21 μM(PKA)、42 μM(PKC)。
 
                                 
                                
                            

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| 描述 | Myosin light chain kinase (MLCK) is a serine/threonine-specific protein kinase that plays a key role in regulating the actin-myosin interaction of smooth muscles. ML-7 is a naphthalene sulphonamide derivative that inhibits MLCK with an IC50 value of 300nM. It also shows inhibitory activities against rabbit portal vein α1-adrenoceptor non-selective cation channel with an IC50 value of 0.8μM[3]. In a mouse model of controlled cortical impact, specific inhibition of MLCK by ML-7 (1mg/kg; i.p. injection) significantly reduced post-traumatic brain edema formation and intracranial hypertension, decreased permeability of the brain-blood barrier, and suppressed phosphorylation of myosin light chains compared with vehicle-treated animals[4]. | 
| Concentration | Treated Time | Description | References | |
| Caco-2 cells | 25 µM | 6 hours | To mitigate down-regulation of mucosa-related protein expression. | Cells. 2024 May 25;13(11):913. | 
| Klebsiella pneumoniae | 32-128 mg/mL | 1 hour | ML-7 increases the efficacy of tigecycline against resistant strains by inhibiting efflux pumps and reducing ATP levels. | Front Cell Infect Microbiol. 2022 Jan 5;11:809542. | 
| PDGFRA D842V GIST cells, GIST T1 cells | 4 µM to 40 µM | 24 hours, 48 hours | ML-7 was used to induce apoptosis and disrupt actin filaments, showing an additive effect in combination with avapritinib in reducing cell viability. | Clin Cancer Res. 2023 Jun 1;29(11):2144-2157. | 
| Administration | Dosage | Frequency | Description | References | ||
| Mice | Patient-derived xenograft (PDX) model of PDGFRA D842V-mutant GIST | Gavage | 10 mg/kg | Daily for 2 weeks | The combined therapy with ML-7 improved the anti-tumor effects of low-dose avapritinib in vivo. | Clin Cancer Res. 2023 Jun 1;29(11):2144-2157. | 
| 计算器 | ||||
| 存储液制备 |  | 1mg | 5mg | 10mg | 
| 1 mM 5 mM 10 mM | 2.21mL 0.44mL 0.22mL | 11.04mL 2.21mL 1.10mL | 22.09mL 4.42mL 2.21mL | |
| CAS号 | 110448-33-4 | 
| 分子式 | C15H18ClIN2O2S | 
| 分子量 | 452.74 | 
| SMILES Code | Cl.IC1=CC=CC2=C1C=CC=C2S(=O)(=O)N1CCCNCC1 | 
| MDL No. | MFCD00065524 | 
| 别名 | ML-7 (hydrochloride); ML-7 hydrochloride; ML-7 | 
| 运输 | 蓝冰 | 
| InChI Key | KDDALCDYHZIZMH-UHFFFAOYSA-N | 
| Pubchem ID | 9803932 | 
| 存储条件 | In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry,2-8°C | 
| 溶解方案 | DMSO: 45 mg/mL(99.4 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO H2O: 1 mg/mL(2.21 mM),配合低频超声助溶 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 
 
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