SH5-07 - STAT 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESH5-07Cat. No.: HY-100494CAS No.: 1456632-41-9分式: CHFNOS分量: 625.61作靶点: STAT作通路: JAK/STAT Signaling; Stem Cell/Wnt储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 50 mg/mL (79.92 mM; Need ult

2、rasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (4.00 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (4.00 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 SH5-07种基于异羟肟酸的 Stat3 抑制剂，在体外实验中的 IC50 值为 3.9 M。IC50

3、& Target STAT33.9 M (IC50)体外研究 SH5-07 is a hydroxamic acid analog of BP-1-102. SH5-07 dose-dependently inhibits Stat3 activity with anIC50 of 3.90.6 M in in vitro assay. It preferentially inhibits Stat3:Stat3 DNA-binding activity, ahead ofinhibiting Stat1:Stat3 activity, with minimal effects on Stat

4、1:Stat1 activity. SH5-07 binds Stat3, disrupts Stat3association with growth factor receptor, and thereby inhibits Stat3 phosphorylation. It induces antitumor celleffects against malignant cells harboring constitutively-active Stat3. SH5-07 inhibits the expression of knownStat3-regulated genes. Bcl-2

5、, Bcl-xL, c-Myc, Survivin, Cyclin D1 and Mcl-1 expression is reduced in responseto 24 h, 5 M SH5-07 treatment 1.体内研究 Tail vein injection or oral gavage delivery of SH5-07 or SH4-54 inhibits growth of 90-150 mm3 establishedsubcutaneous mouse xenografts of human glioma (U251MG) and breast (MDA-MB-231)

6、 tumors that harboraberrantly-active Stat3, associated with decreased c-Myc, Mcl-1 and Cyclin D1 expression. No significantchanges in body weights, blood cell counts, or the gross anatomy of organs, or obvious signs of toxicity areobserved 1.PROTOCOLCell Assay 1 Cells are treated with 0-8 M agent fo

7、r 24-48 h. For cell cycle profile analysis, cells are harvested and fixedwith 70% ice-cold ethanol and stained with propidium iodide (PI). For apoptosis analysis, cells are collectedand stained with FITC-Annexin V using Apoptosis Detection Kit. Both the DNA content of cells and theAnnexin V-positive

8、 cells are analyzed by FACScan flow cytometer. Cell cycle phase distribution is analyzedusing the Cell-Fit program. Data acquisition is gated to exclude cell doublets 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice: Mice are injected subcu

9、taneously in the left flank area with U251MG cells in 200 L of PBS/MatrigelAdministration 1 matrix, or MDA-MB-231 cells in 100 L of PBS. Mice with tumors of 90-150 mm3 (MDA-MB-231) or 150 mm3(U251MG) are grouped for identical mean tumor sizes, administered 3, 5 or 6 mg/kg SH5-07 or SH4-54 viaoral ga

10、vage daily or tail vein injection every 2 or 3 days, and monitored every 3-7 days. Tumor sizes aremeasured with calipers and converted to tumor volume 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Yue P,et al. Hydroxamic Acid and Benzoic Acid-Based STAT3 Inhibitors Suppress Human Glioma and Breast Cancer Phenotypes InVitro and In Vivo. Cancer Res. 2016 Feb 1;76(3):652-63.McePdfHei t Caution: Product has not been fully