| 名称 | Pyrrolidinedithiocarbamate ammonium |
| 描述 | Pyrrolidinedithiocarbamate ammonium (1-Pyrrolidinedithiocarboxylic acid ammonium salt), a selective NF-κB inhibitor, inhibits translation of nitric oxide synthase mRNA to prevent induction. |
| 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]. |
| 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). |
| 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]。 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 247.5 mg/mL (1506.48 mM), Sonication is recommended.
5% DMSO+95% Saline : 0.6 mg/mL (3.65 mM), Solution.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 10 mg/mL (60.87 mM), Solution.
10% DMSO+90% Saline : < 10 mg/mL (60.87 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.
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| 关键字 | ulcerative | Pyrrolidinedithiocarbamate ammonium | PDTC | NF-κB | NFκB | NF-kB | NFkB | colitis | 1-Pyrrolidinedithiocarboxylic acid ammonium |
| 相关产品 | D-Psicose | Uridine | Sodium propionate | Ethyl palmitate | 1,4-Naphthoquinone | Glucosamine | Undecane | Fumaric acid | Kojic acid | Magnesium sulfate | Ethyl linoleate | N,N-Dimethylacetamide |
| 相关库 | 抑制剂库 | 经典已知活性库 | 抗癌活性化合物库 | 已知活性化合物库 | 抗衰老化合物库 | 抗肝癌化合物库 | 抗肺癌化合物库 | 免疫/炎症分子化合物库 | 药物功能重定位化合物库 | NF-κB 通路分子库 | 抗癌临床化合物库 | 抗癌药物库 |