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StemRegenin 1

StemRegenin 1

产品编号 T1831   CAS 1227633-49-9
别名: SR1

StemRegenin 1 (SR1) 是一种芳香烃受体拮抗剂,IC50为 127 nM。

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StemRegenin 1 Chemical Structure
StemRegenin 1, CAS 1227633-49-9
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
其他形式的 StemRegenin 1:
药物设计专题培训
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
产品目录号及名称: StemRegenin 1 (T1831)
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纯度: 99.78%
纯度: 99.66%
纯度: 99.06%
纯度: 98%
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生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 80 mg/mL (186.2 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

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

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TargetMol Library Books参考文献

1. Boitano AE, et al. Science, 2010, 329(5997), 1345-1348. 2. Gao H, et al. J Biol Chem, 2012, 287(35), 219979-291987. 3. Gori JL, et al. Blood, 2012, 120(13), e35-44. 4. Jin H, Ji C, Ren F, et al. AHR-Mediated Oxidative Stress Contributes to the Cardiac Developmental Toxicity of Trichloroethylene in Zebrafish Embryos[J]. Journal of Hazardous Materials. 2020, 385: 121521.

TargetMol Library Books文献引用

1. Jin H, Ji C, Ren F, et al. AHR-Mediated Oxidative Stress Contributes to the Cardiac Developmental Toxicity of Trichloroethylene in Zebrafish Embryos. Journal of Hazardous Materials. 2020, 385: 121521
(-)-Perillaldehyde YL-109 Potassium 1H-indol-3-yl sulfate D-Kynurenine BAY-218 WAY-605471 Leflunomide ITE

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 药物功能重定位化合物库 核受体化合物库 NO PAINS 化合物库 已知活性化合物库 临床期小分子药物库 抗衰老化合物库 人代谢物化合物库 非甾体类抗炎化合物库 活性脂质化合物库

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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。

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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。

Keywords

StemRegenin 1 1227633-49-9 Immunology/Inflammation Metabolism Aryl Hydrocarbon Receptor AhR StemRegenin-1 SR1 StemRegenin1 inhibit Inhibitor SR-1 SR 1 inhibitor

 

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