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- 详细信息
- 文献和实验
- 技术资料
- 保存条件:
Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
- 保质期:
Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
- 英文名:
mL-9 Hydrochloride
- 库存:
现询
- 供应商:
北京索莱宝科技有限公司
- CAS号:
105637-50-1
- 规格:
1mg/5mg
| 规格: | 1mg | 产品价格: | ¥196.0 |
|---|---|---|---|
| 规格: | 5mg | 产品价格: | ¥430.0 |
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。
| 基本信息 | |
| 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 |
| 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. |
| 单位 | 瓶 |
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文献和实验2F+DwTquooTcizAj6Sh40arj1e+iWJ2ispgsbT801bWi9OaaVDQ0u7N9Rf22Q7je3ypEkT/aXtAx/4gHh20RbetchuWXizve3YY/3L0LGHHqt8Cva+97zf/vEfvyYb4imWXpTxLz8m4rvgjodswc3X26Xnn2o3LbjZPv/Fv5GGuGa33/ZzO2n2HD17NAEWeUXwmQh44uy32U+uutL+69e+6jjedfsddvSxx3m8xNNFQ67wipqQKHyESZ35
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BL/6J X SJL/J)F1代雌鼠的受精卵中,并引起插入突变(Im),这是Edward H.Birkenmeier (Bir) 实验室命名的第一只转基因小鼠。 根据转基因动物命名的原则,如果转基因动物的遗传背景是由不同的近交系或远交群之间混合而成时,则该转基因符号应不使用动物品系或种群的名称。 转基因符号的缩写:转基因符号可以缩写,即去掉插入片段标示部分,例如TgN(GPDHIm)1 Bir可缩写为TgN 1 Bir。一般在文章中第一次出现时使用全称,以后再出现时可使用缩写名称。
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