| 名稱 | StemRegenin 1 |
| 描述 | StemRegenin 1 (SR1) is an aryl hydrocarbon receptor (AhR) inhibitor. |
| 細(xì)胞實(shí)驗(yàn) | 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]. |
| 激酶實(shí)驗(yàn) | 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. |
| 體外活性 | 在NOD.Cg-Prkdcscid Il2rgtm1Wj1 / SzJ（NSG）小鼠中,通過SR1促進(jìn)CB CD34 +細(xì)胞的增殖,能夠有助于在早期進(jìn)行細(xì)胞植入及持續(xù)植入. |
| 體內(nèi)活性 | 在體外,StemRegenin 1（1 μM）能夠促進(jìn)CD34 +細(xì)胞的增殖（EC 50=?120 nM）,同時(shí)降低VentX的表達(dá)水平。StemRegenin 1能夠抑制光親和配體（PAL）結(jié)合（IC 50 = 40 nM）。 |
| 存儲(chǔ)條件 | Pure form: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 123.75 mg/mL (288.1 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.66 mM), Sonication is recommended.
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
|
| 關(guān)鍵字 | StemRegenin-1 | StemRegenin1 | StemRegenin 1 | SR-1 | SR 1 | Inhibitor | inhibit | ArylHydrocarbonReceptor | Aryl Hydrocarbon Receptor | AhR |
| 相關(guān)產(chǎn)品 | Mexiletine hydrochloride | Tryptamine hydrochloride | Benzyl butyl phthalate | Diosmin | Sudan IV | Indole-3-carbinol | Skatole | 2-Mercaptobenzothiazole | CH-223191 | Nimodipine | 1-Hydroxypyrene | Dibenzothiophene |
| 相關(guān)庫 | 抑制劑庫 | 經(jīng)典已知活性庫 | 已知活性化合物庫 | 轉(zhuǎn)錄因子庫 | 抗衰老化合物庫 | NO PAINS 化合物庫 | 干細(xì)胞分化化合物庫 | 臨床期小分子藥物庫 | 免疫/炎癥分子化合物庫 | 藥物功能重定位化合物庫 | 表型篩選靶點(diǎn)鑒定庫 | 人代謝物化合物庫 |