Powder: -20°C for 3 years | In solvent: -80°C for 1 year
TPCA-1 (TPCA1) 是一种选择性IKK-2抑制剂,IC50值为 17.9 nM。它也是反式激活、DNA 结合以及STAT3磷酸化的一种抑制剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 268 | 现货 | ||
2 mg | ¥ 378 | 现货 | ||
5 mg | ¥ 593 | 现货 | ||
10 mg | ¥ 1,080 | 现货 | ||
25 mg | ¥ 1,830 | 现货 | ||
50 mg | ¥ 2,660 | 现货 | ||
100 mg | ¥ 3,830 | 现货 |
产品描述 | TPCA-1 (TPCA1) is an effective and specific IKK-2 inhibitor (IC50: 17.9 nM); shows >22-fold selectivity over IKK-1 and >550-fold selectivity over others kinases and enzymes. |
靶点活性 | IKK2:17.9 nM |
体外活性 | TPCA-1可显著减少体内胶原诱导的T细胞增殖.TPCA-1(3/10/20 mg/kg,i.p.,b.i.d.)预防性给药,使小鼠体内胶原诱导性关节炎的严重程度呈剂量依赖性降低.TPCA-1(20 mg/kg,i.p.,b.i.d.)可明显降低CIA的严重程度,与依那西普(12.5 mg/kg,i.p.)每隔一天给药的效果相同.TPCA-1(10 mg/kg,i.p.,b.i.d.)使疾病严重程度明显降低,并使疾病发作的延迟,这与依那西普(4 mg/kg,i.p.)每隔一天预防性给药的效果相当. |
体内活性 | TPCA-1对TNF-α(IC50:170 nM),IL-6(IC50:290 nM)和IL-8(IC50:320 nM)的产生具有浓度依赖性的抑制作用。 TPCA-1对胶质瘤细胞增殖、TNF诱导的RelA (p65)核转运及NFκB依赖性IL8基因表达均有抑制作用。TPCA-1对IFN诱导的基因表达有抑制效果,并完全抑制MX1和GBP1基因表达,但对ISG15表达的作用很小。此外,TPCA-1对IKK-1(IC50:400 nM)和JNK3(IC50:3600 nM)也有一定抑制效果。 |
激酶实验 | IKK-2 Assay: Recombinant human IKK-2 (residues 1-756) is expressed in baculovirus as an N-terminal GST-tagged fusion protein, and its activity is assessed using a time-resolved fluorescence resonance energy transfer assay. In brief, IKK-2 (5 nM final) diluted in assay buffer (50 mM HEPES, 10 mM MgCl2, 1 mM CHAPS, pH 7.4, with 1 mM DTT and 0.01% w/v BSA) is added to wells containing various concentrations of compound or dimethyl sulfoxide (DMSO) vehicle (3% final). The reaction is initiated by the addition of GST-IκBα substrate (25 nM final)/ATP (1 μM final), in a total volume of 30 μL. The reaction is incubated for 30 min at room temperature, then terminated by the addition of 15 μL of 50 mM EDTA. Detection reagent (15 μL) in buffer (100 mM HEPES, pH 7.4, 150 mM NaCl, and 0.1% w/v BSA) containing antiphosphoserine- IκBα-32/36 monoclonal antibody 12C2, labeled with W-1024 europium chelate, and an allophycocyanin-labeled anti-GST antibody is added, and the reaction is further incubated for 60 min at room temperature. The degree of phosphorylation of GST- IκBαis measured as a ratio of specific 665-nm energy transfer signal to reference europium 620-nm signal, using a Packard Discovery plate reader. |
细胞实验 | Ten microliters of 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) from stock solution (10?mg/mL) is added to each well of 96-well plates containing glioma cells and incubated at 37 °C for 2–4?h. Oxidized MTT is solubilized by adding 100?μL of 10% sodium dodecyl sulfate (SDS) in 0.01?N HCL, and plates are incubated at 37 °C for 4?h in a humidified chamber. Plates are read at 570?nm on a plate reader.(Only for Reference) |
别名 | GW683965, IKK2 Inhibitor IV, TPCA1 |
分子量 | 279.29 |
分子式 | C12H10FN3O2S |
CAS No. | 507475-17-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: Insoluble
Ethanol: 2.8 mg/mL (10 mM)
DMSO: 1 mg/mL, Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol | 1 mM | 3.5805 mL | 17.9025 mL | 35.8051 mL | 89.5127 mL |
5 mM | 0.7161 mL | 3.5805 mL | 7.161 mL | 17.9025 mL | |
10 mM | 0.3581 mL | 1.7903 mL | 3.5805 mL | 8.9513 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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5% DMSO+30% PEG300+5% Tween 80+60% 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 50 μL DMSO (母液浓度为 40 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:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
TPCA-1 507475-17-4 Apoptosis JAK/STAT signaling NF-Κb Stem Cells IκB/IKK STAT GW 683965 Inhibitor TPCA 1 IKK I kappa B kinase GW-683965 GW683965 IKK2 Inhibitor IV IκB kinase TPCA1 inhibit inhibitor