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ML281

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纯度: 99.87%

货号 T3423Cas号 1404437-62-2

ML281是高效的STK33选择性抑制剂(IC50:14 nM)。

ML281
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ML281

一键复制产品信息
Rating icon 很棒

纯度: 99.87%

货号 T3423Cas号 1404437-62-2

ML281是高效的STK33选择性抑制剂(IC50:14 nM)。

规格价格库存数量
1 mg
¥ 297
现货
5 mg
¥ 679
现货
10 mg
¥ 993
现货
25 mg
¥ 1,820
现货
50 mg
¥ 2,920
现货
100 mg
¥ 4,130
现货
200 mg
¥ 5,880
现货
1 mL x 10 mM (in DMSO)
¥ 579
现货
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纯度: 99.87%
颜色: 白色
性状: Solid
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产品介绍


ML281 AI Summary
ML281 exhibits significant bioactivity and selectivity features, comprising metabolic stability with degradation rates of 10.0% in mouse plasma and 80.3% in human plasma after 5 hours. It shows high plasma protein binding in both mouse (99.9%) and human (99.6%) plasma. The solubility of ML281 in PBS at pH 7.4 is 5800.0 nM. In terms of enzymatic inhibition, ML281 demonstrates potent inhibition of N-terminal 6His-tagged full-length human recombinant STK33 with an IC50 value of 14.0 nM, using myelin basic protein as substrate. It also inhibits human KDR and FLT3 at 1 µM, with inhibition percentages of ≥25.0% for each. The compound shows a high IC50 value (>10,000.0 nM) for inhibition of His-tagged recombinant catalytic fragment of PKA, translating to a selectivity ratio of IC50 for PKA to STK33 of >700.0. Additionally, it shows selectivity for STK33 over Aurora kinase B with a ratio IC50 of 550.0. Regarding its antiviral activity, ML281 inhibits SARS-CoV-2 induced cytotoxicity of Caco-2 cells at 10 µM after 48 hours, showing 5.22% inhibition as determined by high content imaging. It also exhibits SARS-CoV-2 3CL-Pro protease inhibition activity with 6.1% and 31.01% inhibition at a concentration of 20 µM. However, its inhibition of SARS-CoV-2 induced cytotoxicity in VERO-6 cells at 10 µM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus shows minimal effects with percentages of 0.19% and -0.06% in different assays. Furthermore, ML281 shows significant inhibition of the human HDAC6 enzyme, particularly demonstrating 40.5% inhibition using a commercial peptide substrate and 4.16% inhibition using a custom peptide substrate..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
ML281 is a potent and selective STK33 inhibitor with IC50 of 14 nM.
靶点活性
STK33:14 nM.
化学信息
分子量389.47
分子式C22H19N3O2S
CAS No.1404437-62-2
SmilesCC(C)c1ccc(NC(=O)c2cccs2)c(c1)-c1nc2ccccc2[nH]c1=O
密度no data available
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
溶解度信息
DMSO: 50 mg/mL (128.38 mM), Sonication is recommended.
H2O: < 1 mg/mL (insoluble or slightly soluble)
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM2.5676 mL12.8380 mL25.6759 mL128.3796 mL
5 mM0.5135 mL2.5676 mL5.1352 mL25.6759 mL
10 mM0.2568 mL1.2838 mL2.5676 mL12.8380 mL
20 mM0.1284 mL0.6419 mL1.2838 mL6.4190 mL
50 mM0.0514 mL0.2568 mL0.5135 mL2.5676 mL
100 mM0.0257 mL0.1284 mL0.2568 mL1.2838 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL, 一共给药动物10只,您使用的配方为 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline / PBS / ddH2O, 那么您的工作液浓度为2 mg/mL
母液配置方法:2 mg 药物溶于 100 μL DMSO ( 母液浓度为 20 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:100 μL DMSO 母液, 添加 400 μL PEG300 混匀澄清, 再加 50 μL Tween 80, 混匀澄清, 再加 450 μL Saline / PBS / ddH2O 混匀澄清
以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。
方案所需的各类助溶剂如: DMSOPEG300PEG400Tween 80SBE-β-CD玉米油等, 均可在TargetMol网站点击购买。
1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

剂量转换

对于不同动物的给药剂量换算,您也可以参考 更多

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