SID 26681509
![mRNA synthesis](/media/diy/images/page/figure1-mrna.png)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
![Tyramine Signal Amplification (TSA)](/media/diy/images/page/figure2-01.png)
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
![screening library](/media/diy/images/page/figure3-01.png)
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
![Cell Counting Kit-8 (CCK-8)](/media/diy/images/page/CCK-8.jpg)
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
![SYBR Safe DNA Gel Stain](/media/diy/images/page/SYBR Safe DNA Gel Stain.png)
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
![Inhibitor Cocktails](/media/diy/images/page/Inhibitor Cocktails.jpg)
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50: 56 nM
SID 26681509是一种强效的和可逆的人组织蛋白酶L抑制剂。
组织蛋白酶包括溶酶体蛋白酶家族,其主要功能(如蛋白质降解)在正常细胞内环境稳定中发挥关键作用。组织蛋白酶L的过表达和/或异常活性与许多疾病状态有关。
体外:SID 26681509抑制人组织蛋白酶L,IC50为56 nM。底物加入之前的1、2和4小时与酶预孵育后,SID 26681509效力增加,IC50值分别下降到7.5、4.2和1.0 nM,表明抑制的缓慢开始。还观察到达到100 μM的SID 26681509对人主动脉内皮细胞是无毒的。SID 26681509在恶性疟原虫体外繁殖实验中有效,IC50为15.4 μM。此外,thiocarbazate抑制剂对L. major promastigotes具有毒性,IC50为12.5 μM [1]。
体内:在活生物体测定中,100 μM的SID 26681509对斑马鱼缺乏毒性 [1]。
临床试验:N/A
参考文献:
[1] Shah PP,μMyers MC,Beavers MP,Purvis JE,Jing H,Grieser HJ,Sharlow ER,Napper AD,Huryn DM,Cooperman BS,Smith AB 3rd,Diamond SL. Kinetic characterization and molecular docking of a novel, potent, and selective slow-binding inhibitor of human cathepsin L. Mol Pharmacol.2008 Jul;74(1):34-41.
Physical Appearance | White solid |
Storage | Store at -20°C |
M.Wt | 539.65 |
Cas No. | 958772-66-2 |
Formula | C27H33N5O5S |
Solubility | <26.98mg/ml in DMSO; <5.4mg/ml in ethanol |
Chemical Name | (S)-S-(2-((2-ethylphenyl)amino)-2-oxoethyl) 2-(2-((tert-butoxycarbonyl)amino)-3-(1H-indol-3-yl)propanoyl)hydrazinecarbothioate |
SDF | Download SDF |
Canonical SMILES | O=C(NNC(SCC(NC1=CC=CC=C1CC)=O)=O)[C@H](CC2=CNC3=CC=CC=C23)NC(OC(C)(C)C)=O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1]: | |
细胞系 |
人类主动脉内皮细胞 |
溶解方法 |
该化合物在DMSO中的溶解度大于10 mM。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。 |
反应条件 |
100 μM,37°C,24h |
应用 |
SID 26681509(100 μM)对人主动脉内皮细胞无毒性。在针对恶性疟原虫的体外繁殖实验中,SID 26681509具有活性,IC50为15.4 ± 0.6 μM。SID 26681509对L.主要前鞭毛体具有毒性,IC50为12.5 ± 0.6 μM。 |
动物实验 [1]: | |
动物模型 |
斑马鱼 |
给药剂量 |
100 μM |
应用 |
在活体生物实验中,SID 26681509 (100 μM)对斑马鱼没有毒性。 |
注意事项 |
由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。 |
References: [1]. Shah P P, Myers M C, Beavers M P, et al. Kinetic characterization and molecular docking of a novel, potent, and selective slow-binding inhibitor of human cathepsin L[J]. Molecular pharmacology, 2008, 74(1): 34-41. |
Potent and reversible human cathepsin L inhibitor (IC50 = 56 nM). | ||||||
Targets | cathepsin L | |||||
IC50 | 56nM |
化学结构
![SID 26681509](http://www.apexbt.com//media/diy/images/struct/A4424.png)