Powder: -20°C for 3 years | In solvent: -80°C for 1 year
StemRegenin 1 (SR1) 是一种芳香烃受体拮抗剂,IC50为 127 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 274 | 现货 | ||
10 mg | ¥ 430 | 现货 | ||
25 mg | ¥ 855 | 现货 | ||
50 mg | ¥ 1,676 | 现货 | ||
100 mg | ¥ 2,480 | 现货 | ||
500 mg | ¥ 4,770 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 295 | 现货 |
产品描述 | StemRegenin 1 (SR1) is an aryl hydrocarbon receptor (AhR) inhibitor. |
靶点活性 | AhR:127 nM |
体外活性 | 在NOD.Cg-Prkdcscid Il2rgtm1Wj1 / SzJ(NSG)小鼠中,通过SR1促进CB CD34 +细胞的增殖,能够有助于在早期进行细胞植入及持续植入. |
体内活性 | 在体外,StemRegenin 1(1 μM)能够促进CD34 +细胞的增殖(EC 50=?120 nM),同时降低VentX的表达水平。StemRegenin 1能够抑制光亲和配体(PAL)结合(IC 50 = 40 nM)。 |
激酶实验 | Kinase assays: PDK1 is assayed in a direct kinase assay and a coupled assay format measuring PDK1- and PtdIns-3,4-P2-mediated activation of AKT2. For the coupled assay, the final assay mixture (60 μL) contained: 15 mM MOPS, pH 7.2, 1 mg/mL bovine serum albumin, 18 mM β-glycerol phosphate, 0.7 mM dithiothreitol, 3 mM EGTA, 10 mM MgOAc, 7.5 μM ATP, 0.2 μCi of [γ-33P]ATP, 7.5 μM biotinylated peptide substrate (biotin-ARRRDGGGAQPFRPRAATF), 0.5 μL of PtdIns-3,4-P2-containing phospholipid vesicles, 60 pg of purified recombinant human PDK1, and 172 ng of purified recombinant human AKT2. After incubation for 2 h at room temperature, the biotin-labeled peptide is captured from 10 μl of the assay mixture on streptavidin-coated SPA beads, and product formation is measured by scintillation proximity in a Wallac MicroBeta counter. The product formed is proportional to the time of incubation and to the amount of PDK1 and inactive AKT2 added. PDK1 is added at suboptimal levels so that the assay could sensitively detect inhibitors of AKT2 activation as well as direct inhibitors of PDK1 or AKT2. To measure PDK1 activity directly, the final assay mixture (60 μL) contained 50 mM Tris-HCl, pH 7.5, 0.1 mM EGTA, 0.1 mM EDTA, 0.1% β-mercaptoethanol, 1 mg/mL bovine serum albumin, 10 mM MgOAc, 10 μM ATP, 0.2 μCi of [γ-33P]ATP, 7.5 μM substrate peptide (H2N-ARRRGVTTKTFCGT), and 60 ng of purified recombinant human PDK1. After 4 h at room temperature, we add 25 mM EDTA and spotted a portion of the reaction mixture on Whatman P81 phosphocellulose paper. The filter paper is washed three times with 0.75% phosphoric acid and once with acetone. After drying, the filter-bound labeled peptide is quantified using a Fuji phosphorimager. |
细胞实验 | StemRegenin 1 (SR1) is prepared in DMSO and stored, and then diluted with appropriate medium before use[1]. A quantity of 250,000 CB-derived CD34+ cells are cultured with control conditions (DMSO, 0.01%) or StemRegenin 1 (0.75 μM) for 3 weeks. At this point control cultures had expanded 1080-fold and StemRegenin 1 treated cells expanded 2024-fold relative to starting cell numbers. A quantity of 30 to 30,000 uncultured CD34+ CB-derived cells or a fraction of the final culture equivalent to 30 to 10,000 starting cells are transplanted. The cells are injected intravenously via the retro-orbital route into sub-lethally irradiated (300 rads, 200 rads) 6- to 10-week-old NSG mice. Engraftment is performed within 24 h after irradiation. Engraftment is monitored by flow cytometric analysis of blood obtained via retro-orbital sinus or bone marrow using anti-human CD45 and anti-mouse CD45 antibodies. The mice are sacrificed between 13-16 weeks posttransplantation; bone marrow (from both femurs and tibiae), spleen and thymus are collected for analysis. For secondary engraftment, 50% of the bone marrow from each recipient mouse is transplanted into one secondary sub-lethally irradiated NSG mouse. Fifteen weeks after transplantation, bone marrow is harvested from the secondary mice and analyzed by flow cytometry[1]. |
别名 | SR1 |
分子量 | 429.54 |
分子式 | C24H23N5OS |
CAS No. | 1227633-49-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 80 mg/mL (186.2 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.3281 mL | 11.6404 mL | 23.2807 mL | 58.2018 mL |
5 mM | 0.4656 mL | 2.3281 mL | 4.6561 mL | 11.6404 mL | |
10 mM | 0.2328 mL | 1.164 mL | 2.3281 mL | 5.8202 mL | |
20 mM | 0.1164 mL | 0.582 mL | 1.164 mL | 2.9101 mL | |
50 mM | 0.0466 mL | 0.2328 mL | 0.4656 mL | 1.164 mL | |
100 mM | 0.0233 mL | 0.1164 mL | 0.2328 mL | 0.582 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。
StemRegenin 1 1227633-49-9 Immunology/Inflammation Metabolism AhR Aryl Hydrocarbon Receptor StemRegenin-1 SR1 StemRegenin1 inhibit Inhibitor SR-1 SR 1 inhibitor