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ML281

货号 T3423Cas号 1404437-62-2 一键复制产品信息纯度: 99.87%
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ML281是高效的STK33选择性抑制剂(IC50:14 nM)。

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)。

ML281
TargetMol

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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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TargetMol的所有产品仅用作科学研究或药证申报,不能被用于人体,我们不向个人提供产品和服务。请您遵守承诺用途,不得违反法律法规规定用于任何其他用途。

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常见问题解答
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选择批次:
纯度: 99.87%
颜色: 白色
性状: Solid
资源下载: COA LCMS HPLC HNMR产品操作手册

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

Shipping with blue ice/Shipping at ambient temperature.

实际储存温度请以COA为准

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
该溶液配制表仅适用于固体产品。对于液体产品,请根据标明的浓度或密度计算稀释方案。

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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