ML-9盐酸盐

ML-9盐酸盐用途

ML-9 是 Akt 激酶的选择性强效抑制剂,可抑制肌球蛋白轻链激酶 (MLCK) 和基质相互作用分子1 (STIM1) 的活性。 ML-9 抑制 MLCK,PKA 和 PKC 活性,Ki 值分别为 4、32 和 54 μM。 ML-9 通过刺激自噬小体的形成并抑制其降解来诱导自噬 (autophagy)。

ML-9盐酸盐名称

[ CAS 号 ]:
105637-50-1

[ 中文名 ]:
1-(5-氯萘-1-磺酰基)-1H-六氢-1,4-二吖庚因盐酸盐

[ 英文名 ]:
ML-9

[中文别名 ]:

ML-9盐酸盐

[英文别名 ]:

MFCD00065525

ML-9盐酸盐生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 细胞骨架 >> 肌球蛋白

[体外研究]

ML9(0-100 μM；0-24 h)不降低心肌细胞活力,50-100 μM显著诱导细胞死亡[2]。ML9(50μM；1-4小时)显著提高caspase-3的裂解水平,使STIM1蛋白水平降低约42%[2]。细胞活力测定[1]细胞系：新生大鼠心室肌细胞(NRVM)细胞浓度：0、10、50和100μM培养时间：0、1、4、8和24小时结果：50-100μM浓度下细胞活力降低。凋亡分析[1]细胞系：新生大鼠心室肌细胞(NRVM)细胞浓度：50μM孵育时间：1、4、8小时结果：通过坏死和凋亡诱导心肌细胞死亡。

[参考文献]

[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.

ML-9盐酸盐物理化学性质

[ 沸点 ]:
508.8ºC at 760mmHg

[ 熔点 ]:
196-200ºC

[ 分子式 ]:
C₁₅H₁₈Cl₂N₂O₂S

[ 分子量 ]:
361.287

[ 闪点 ]:
261.5ºC

[ 精确质量 ]:
360.046600

[ PSA ]:
57.79000

[ LogP ]:
4.62670

[ 外观性状 ]:
结晶固体

[ 蒸汽压 ]:
1.79E-10mmHg at 25°C

[ 储存条件 ]:
2-8°C，避光，惰性气体

ML-9盐酸盐MSDS

详细MSDS(安全技术说明书)

ML-9盐酸盐安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xi

[ 危险品运输编码 ]:
NONH for all modes of transport

[ 海关编码 ]:
2933990090

ML-9盐酸盐海关

[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ 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%

ML-9盐酸盐文献

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...

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