| 名称 | PS-1145 |
| 描述 | PS-1145 (IKK Inhibitor X) is a specific IKK inhibitor with IC50 of 88 nM. |
| 细胞实验 | The inhibitory effect of PS-1145 on MM growth is assessed by measuring MTT dye absorbance of the cells. Cells from 48-h cultures are pulsed with 10 μL of 5 mg/ml MTT to each well for the last 4 h of 48-h cultures, followed by 100 μl of isopropanol containing 0.04N HCl. Absorbance is measured at 570 nm using a spectrophotometer. (Only for Reference) |
| 激酶实验 | Kinase assay: PS-1145 are dissolved in DMSO and stored at ?20?°C until use. Ki value of PS-1145 against the IKK complex is determined by measuring Km ,?ATP against varying fixed concentration of the inhibitor. Briefly, partially purified IKK complex obtained from unstimulated HeLa S3 cells are pre-activated using the catalytic domain of MEKK1 expressed in sf9. Kinase activity is assessed using a biotinylated IκBα peptide (250 μM, RHDSGLDSMKD,Km ,peptide = 30 μM,K m ,?ATP = 10 μM) and phospho-[Ser32]-phosphoantibodies in an ELISA format with appropriate standard curve for quantification. For PS-1145 Ki measurement, the activated IKK complex is first preincubated in varying fixed concentration of the inhibitor (0.1–1 μM) at 25 °C for 1 h. Then apparentK m measurement for MgATP is performed at each discrete inhibitor concentration. |
| 体外活性 | Administering 50 mg/kg of PS-1145 intravenously in male Wistar rats with DMBA-induced skin tumors resulted in the upregulation of p53 and activation of caspases, coupled with the downregulation of NF-κB and VEGF factors, thereby enhancing apoptosis in tumor cells. |
| 体内活性 | PS-1145 inhibits the proliferation of primary human CD4(+) T cells and impedes the activation of NF-κB and AP-1 transcription factors through the cooperative engagement of CD3 and CD28 co-receptors. Additionally, PS-1145 blocks TNFalpha-induced NF-kappaB activation by inhibiting the phosphorylation of IkappaBalpha and disrupting the protective effect of IL-6 on Dex-induced apoptosis. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 50 mg/mL (154.92 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 2 mg/mL (6.19 mM), Heating is recommended.
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| 关键字 | I kappa B kinase | PS1145 | inhibit | Apoptosis | IKK | PS 1145 | PS-1145 | IκB kinase | Inhibitor |
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| 相关库 | 细胞凋亡化合物库 | 经典已知活性库 | 神经退行性疾病化合物库 | 激酶抑制剂库 | 抑制剂库 | 抗前列腺癌化合物库 | 抗衰老化合物库 | 已知活性化合物库 | 抗癌化合物库 | 抗癌活性化合物库 |
United States
