CAS |
No.105637-50-1 |
中文名称 |
mL-9盐酸盐 |
英文名称 |
mL-9 Hydrochloride |
分子式 |
C15H18Cl2N2O2S |
分子量 |
361.29 |
溶解性 |
Soluble in DMSO ≥5mg/mL |
纯度 |
≥98% |
外观(性状) |
Off-white to yellow Solid |
储存条件 |
Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year |
运输条件 |
冷藏运输 |
EC |
EINECS 200-258-5 |
MDL |
MFCD00065525 |
SMILES |
C1CNCCN(C1)S(=O)(=O)C2=CC=CC3=C2C=CC=C3Cl.Cl |
InChIKey |
ZNRYCIVTNLZOGI-UHFFFAOYSA-N |
InChI |
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,3,8-11H2;1H |
PubChem CID |
108047 |
靶点 |
Akt;MLCK;STIM1 |
通路 |
Cytoskeleton;PI3K/Akt/mTOR |
背景说明 |
mL-9 hydrochloride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。 |
生物活性 |
ML-9 is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity. ML-9 inhibits inhibits MLCK, PKA and PKC activity with Ki values of 4, 32 and 54 μM, respectively. ML-9 induces autophagy by stimulating autophagosome formation and inhibiting their degradation[1-3]. |
In Vitro |
ML-9 inhibited both the increase in [Ca2+]i and the contraction induced by 60 mM K+, 1 microM methacholine or 1 microM thapsigargin, an inhibitor of the sarcoplasmic reticulum Ca2+-ATPase.ML-9 acts as a potent inhibitor of Ca2+-permeable channels independently of MLCK inhibition in tracheal smooth muscle.[1] ML9 was found to induce cell death in cultured neonatal rat cardiomyocytes.Treatment with ML9 significantly increased levels of the Autophagy marker LC3-II, without altering Beclin1 or p62 protein levels.ML9-induced cardiomyocyte death is triggered by a ML9-dependent disruption of autophagic flux due to lysosomal dysfunction.[2] |
细胞实验 |
ML9 (0-100?μM; 0-24?hours) has no reduction in cardiomyocyte viability, 50-100?μM significantly induces cell death[2]. |
数据来源文献 |
[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. |
规格 |
1mg 5mg |
单位 |
瓶 |