化合物SH5-07 TQ0052

Product Introduction
Bioactivity


英文名: SH5-07

描述: SH5-07 是一种基于异羟肟酸的 Stat3 抑制剂，IC50值为 3.9 μM。

细胞实验: Cells are treated with 0-8 μM agent for 24-48 h. For cell cycle profile analysis, cells are harvested and fixed with 70% ice-cold ethanol and stained with propidium iodide (PI). For apoptosis analysis, cells are collected and stained with FITC-Annexin V using the Apoptosis Detection Kit. Both the DNA content of cells and the Annexin V-positive cells are analyzed by the flow cytometer. Cell cycle phase distribution is analyzed using the Cell-Fit program. Data acquisition is gated to exclude cell doublets.

动物实验: Mice are injected subcutaneously in the left flank area with U251MG cells in 200 μL of PBS/Matrigel matrix, or MDA-MB-231 cells in 100 μL of PBS. Mice with tumors of 90-150 mm^3 (MDA-MB-231) or 150 mm^3 (U251MG) are grouped for identical mean tumor sizes, administered 3, 5 or 6 mg/kg SH5-07 via oral gavage daily or tail vein injection every 2 or 3 days, and monitored every 3-7 days. Tumor sizes are measured with calipers and converted to tumor volume.

体外活性: SH5-07是BP-1-102的羟胺酸类似物。SH5-07剂量依赖性抑制Stat3活性（IC50: 3.9±0.6 μM，体外实验）。它优先抑制Stat3:Stat3 DNA结合活性，而不是Stat1:Stat3活性，并对Stat1:Stat1活性影响最小。SH5-07与Stat3结合，破坏Stat3与生长因子受体的关联，从而抑制Stat3磷酸化。SH5-07对携带持续活跃Stat3的恶性细胞产生抗肿瘤细胞效应。SH5-07能够抑制已知的Stat3调控基因的表达。经过24小时，5 μM SH5-07处理后，Bcl-xL、Bcl-2、c-Myc、Survivin、Cyclin D1和Mcl-1的表达减少。

体内活性: 通过尾静脉注射或口服灌胃方式给予SH5-07能够抑制已建立的皮下小鼠异种移植的人类胶质瘤（U251MG）和乳腺（MDA-MB-231）肿瘤的生长，其大小范围为90-150 mm^3，这些肿瘤中存在异常活跃的Stat3，与之相关的是Mcl-1、c-Myc和Cyclin D1表达的降低。未观察到体重、血细胞计数或器官的总体解剖结构有显著变化，也没有明显的毒性迹象。

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

溶解度: DMSO : 50 mg/mL (79.92 mM)
H2O : Insoluble


关键字: Inhibitor | SH5 07 | inhibit | STAT | SH5-07 | SH507 | SH-5-07

相关产品: STAT3-IN-8 | (R)-Lisofylline | Stafia-1 | AS2863619 | 2-Methoxystypandrone | Ginkgetin | NT157 | Manassantin B | TLC1566-0618 | Kurarinone

相关库: Anti-Aging Compound Library | Anti-Liver Cancer Compound Library | Anti-Cancer Metabolism Compound Library | Immuno-Oncology Compound Library | Cancer Cell Differentiation Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Anti-Pancreatic Cancer Compound Library | NO PAINS Compound Library | Bioactive Compound Library

化合物SH5-07 TQ0052信息由TargetMol中国为您提供，如您想了解更多关于化合物SH5-07 TQ0052报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途