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Pyrrolidinedithiocarbamate ammonium (1-Pyrrolidinedithiocarboxylic acid ammonium salt) 是一种选择性的、能透过血脑屏障的NF-κB 抑制剂。
Pyrrolidinedithiocarbamate ammonium (1-Pyrrolidinedithiocarboxylic acid ammonium salt) 是一种选择性的、能透过血脑屏障的NF-κB 抑制剂。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
100 mg | ¥ 286 | 现货 | |
200 mg | ¥ 397 | 现货 | |
500 mg | ¥ 672 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 185 | 现货 |
产品描述 | Pyrrolidinedithiocarbamate ammonium (1-Pyrrolidinedithiocarboxylic acid ammonium salt), a selective NF-κB inhibitor, inhibits translation of nitric oxide synthase mRNA to prevent induction. |
体外活性 | 细胞预处理PDTC(3-1000 mM)剂量依赖性地减少IL-8产生。此外,PDTC(100 mM)抑制IL-8 mRNA的积累。PDTC通过抑制NF-kB DNA结合及其依赖的转录活性,从而阻止NF-kB的激活。综合我们的数据表明,通过PDTC抑制NF-kB可以降低肠上皮细胞IL-8的产生[1]。 |
体内活性 | DSS+PDTC处理的第二组表现出抑制小肠长度缩短和DAI得分降低。该组中活化的NF-κB水平以及IL-1β和TNF-α水平显著低于对照组。这些发现表明,通过PDTC抑制NF-κB活性可以延缓由炎症引起的粘膜组织缺陷(侵蚀或溃疡)的愈合,但它能强烈抑制炎症细胞因子(IL-1β和TNF-α)的表达,从而显著缓解结肠炎。PDTC对于治疗溃疡性结肠炎具有重要价值[2]。 |
激酶实验 | All binding studies are performed in an HTRF assay buffer consisting of dPBS supplemented with 0.1% (with v) bovine serum albumin and 0.05% (v/v) Tween-20. For the PD-l-Ig/PD-Ll-His binding assay, inhibitors are pre-incubated with PD-Ll-His (10 nM final) for 15 m in 4 μL of assay buffer, followed by addition of PD-l-Ig (20 nM final) in 1 μL of assay buffer and further incubation for 15 m. PD-L1 from either human, cyno, or mouse are used. HTRF detection is achieved using europium crypate-labeled anti- Ig (1 nM final) and allophycocyanin (APC) labeled anti-His (20 nM final). Antibodies are diluted in HTRF detection buffer and 5 μL is dispensed on top of binding reaction. The reaction mixture is allowed to equilibrate for 30 minutes and signal (665 nm/620 nm ratio) is obtained using an En Vision fluorometer. Additional binding assays are established between PD-1-Ig/PD-L2-His (20, 5 nM, respectively), CD80-His/PD-Ll-Ig (100, 10 nM, respectively) and CD80-His/CTLA4-Ig (10, 5 nM, respectively). |
细胞实验 | The human colon cancer cell line HT-29 is obtained and cells are grown in modified McCoy's 5A medium supplemented with 10% fetal bovine serum. To study the effect of PDTC on IL-8 production, HT-29 cells in 96-well plates are induced with 20 ng/mL of IL-1b for 18 h. Various concentrations (3-1000 mM) of PDTC or its vehicle (culture medium) are added to the cells 30 min prior to IL-1b stimulation. The concentration of IL-8 in the supernatant is determined using solid-phase enzyme-linked immunosorbent assay, as described previously employing the multiple antibody sandwich principle that specifically detects human IL-8[1]. |
别名 | PDTC, Pyrrolidinedithiocarbamate, 吡咯烷二硫代氨基甲酸铵, APDC, 1-Pyrrolidinedithiocarboxylic acid ammonium salt, Ammonium pyrrolidinedithiocarbamate, 吡咯烷二硫代甲酸铵 |
分子量 | 164.29 |
分子式 | C5H12N2S2 |
CAS No. | 5108-96-3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 75 mg/mL (456.51 mM) 5% DMSO+95% Saline: 0.6 mg/mL (3.65 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. | ||||||||||||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||||||||||||
5% DMSO+95% Saline/DMSO
DMSO
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