SH-4-54
SH-4-54是一种高效的STAT抑制剂，其作用STAT3和STAT5的KD分别为300 nM和464 nM。
SH-4-54 Chemical Structure
CAS: 1456632-40-8
产品质控
批次：
纯度：
99.96%
99.96
SH-4-54相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| 147EF | Apoptosis assay | 0.1 to 1 uM | 3 hrs | Induction of apoptosis in human 147EF cells assessed as PARP cleavage at 0.1 to 1 uM after 3 hrs by Western blotting analysis | 24900612 |
| 147EF | Function assay | 0.1 to 1 uM | 3 hrs | Inhibition of AKT phosphorylation in human 147EF cells at 0.1 to 1 uM after 3 hrs by Western blotting analysis | 24900612 |
| 147EF | Function assay | 0.1 to 1 uM | 3 hrs | Inhibition of STAT3 phosphorylation at Y705 in human 147EF cells at 0.1 to 1 uM after 3 hrs by Western blotting analysis | 24900612 |
| BT73 | Function assay | 10 mg/kg | 3 days | In vivo inhibition of STAT3 phosphorylation in tumor of NOD-SCID mouse xenografted with human BT73 cells at 10 mg/kg, ip administered as 4 days on/3 days off schedule measured 2 hrs post last dose | 24900612 |
| BT73 | Antitumor assay | 10 mg/kg | 3 days | Antitumor activity against human BT73 cells xenografted in NOD-SCID mouse assessed as decrease in tumor size at 10 mg/kg, ip administered as 4 days on/3 days off schedule measured 2 hrs post last dose by hematoxylin/eosin staining | 24900612 |
| BT73 | Antitumor assay | 10 mg/kg | 3 days | Antitumor activity against human BT73 cells xenografted in NOD-SCID mouse assessed as induction of apoptosis in tumor at 10 mg/kg, ip administered as 4 days on/3 days off schedule measured 2 hrs post last dose by TUNEL assay | 24900612 |
| BT73 | Antitumor assay | 10 mg/kg | 3 days | Antitumor activity against human BT73 cells xenografted in NOD-SCID mouse assessed as tumor growth inhibition by measuring downregulation of Ki67 protein expression at 10 mg/kg, ip administered as 4 days on/3 days off schedule measured 2 hrs post last dos | 24900612 |
| 73M | Function assay | 1 uM | Inhibition of STAT3 phosphorylation at Y705 in human 73M cells at 1 uM | 24900612 | |
| 25EF | Cytotoxicity assay | 3 days | Cytotoxicity against human 25EF cells assessed as cell viability after 3 days by Alamar Blue assay, IC50=0.234μM. | 24900612 | |
| 73EF | Cytotoxicity assay | 3 days | Cytotoxicity against human 73EF cells assessed as cell viability after 3 days by Alamar Blue assay, IC50=0.162μM. | 24900612 | |
| 67EF | Cytotoxicity assay | 3 days | Cytotoxicity against human 67EF cells assessed as cell viability after 3 days by Alamar Blue assay, IC50=0.106μM. | 24900612 | |
| 84EF | Cytotoxicity assay | 3 days | Cytotoxicity against human 84EF cells assessed as cell viability after 3 days by Alamar Blue assay, IC50=0.102μM. | 24900612 | |
| 30M | Cytotoxicity assay | 3 days | Cytotoxicity against human 30M cells assessed as cell viability after 3 days by Alamar Blue assay, IC50=0.1μM. | 24900612 | |
| 127EF | Cytotoxicity assay | 3 days | Cytotoxicity against human 127EF cells assessed as cell viability after 3 days by Alamar Blue assay, IC50=0.066μM. | 24900612 | |
| 30M | Cytotoxicity assay | 8 days | Cytotoxicity against human 30M cells assessed as cell viability after 8 days by Alamar Blue assay, IC50=0.43μM. | 24900612 | |
| 73M | Cytotoxicity assay | 8 days | Cytotoxicity against human 73M cells assessed as cell viability after 8 days by Alamar Blue assay, IC50=1.03μM. | 24900612 | |
| 147EF | Function assay | 2 to 72 hrs | Inhibition of STAT3 in human 147EF cells assessed as reduction of phosphorylated Bcl-xL level after 2 to 72 hrs by Western blotting analysis | 24900612 | |
| 147EF | Function assay | 2 to 72 hrs | Inhibition of STAT3 in human 147EF cells assessed as reduction of phosphorylated cyclin D1 level after 2 to 72 hrs by Western blotting analysis | 24900612 | |
| Vero | Function assay | Vero cells viability counterscreen for qRT-PCR qHTS assay of selected Zika virus inhibitors | 33229545 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | SH-4-54是一种高效的STAT抑制剂，其作用STAT3和STAT5的KD分别为300 nM和464 nM。 | ||||
|---|---|---|---|---|---|
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | SH-4-54在人恶性胶质瘤脑肿瘤肝细胞(BTSCs)中表现出空前的细胞毒性，而在人类胚胎星形胶质细胞中没有毒性。此外，SH-4-54有效抑制STAT3磷酸化和其下游转录靶点。[1] | |||
|---|---|---|---|---|
| 激酶实验 | 表面等离子体共振(SPR) 研究 | |||
| 结合实验在ProteOn XPR36生物传感器上于25℃下使用HTE传感器芯片进行。传感器芯片的流动池以30微升/分钟镍溶液加载120分钟，使 Ni(II)离子浸透Tris–NTA表面。纯化的组氨酸标记的STAT3 和STAT5在PBST缓冲液(PBS 与 0.005% (v/v) Tween-20 以及 0.001% DMSO pH 7.4)中，分别以垂直方向注射入芯片的第一和第二个通道，以25微克/微升的流量进行300秒，其取得平均~8000的共振单位(RU)。用PBST缓冲液洗涤后，抑制剂与固定化蛋白质的结合通过注射一系列浓度以及空白的样品进行监测，每种小分子以100微升/分钟流量进行200秒。注射小分子抑制剂完成时，使电泳缓冲液溢出固定的底物使非特异性结合抑制剂解离600秒。抑制剂解离后，芯片表面再次注射流量为100微升/毫升的1 M NaCl，进行18秒。Interspot通道参比用于非特异性结合修正，空白通道与每个分析物注射液共同使用作为双重参考以修正可能出现的基线漂移。数据使用3.1版ProteOn Manager软件分析。Langmuir 1:1结合模型用于测定KD值。 | ||||
| 细胞实验 | 细胞系 | BTSC 系 25M，67EF，73EF，84EF 和 127EF | ||
| 浓度 | ~25 μM | |||
| 孵育时间 | 72小时 | |||
| 方法 | BTSC球体解离为单个细胞和酶Accumax，以1500个细胞/96孔接种，接种一天后用药物或载体(DMSO)处理。细胞毒性研究使用BTSC系25M，67EF，73EF，84EF和127EF单独反复进行。BTSC球体解离为单个细胞，重复三份以3000细胞/96孔接种于96孔板。两类实验药物浓度被连续稀释为5 μM 到 100 nM和25 μM到10 nM。根据制造商的说明使用alamarBlue测试法，3天后，对药物处理后的细胞活性进行评估。所有培养基实验以一式三份且每种条件至少存在3个孔进行。 |
|||
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | LMP1 / p-STAT3 / STAT3 |
|
28445949 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | BT73原位异种移植的小鼠体内，SH-4-54 (10 毫克/千克，腹腔注射)表现出BBB渗透性，有效抑制神经胶质肿瘤生长，并抑制pSTAT3。[1] | |
|---|---|---|
| 动物实验 | Animal Models | 负荷 BT73 胶质瘤异种移植物的NOD-SCID |
| Dosages | 悬浮在 50% 聚乙二醇 300 水溶液中 | |
| Administration | 腹腔注射 | |
化学信息&溶解度
| 分子量 | 610.59 | 分子式 | C29H27F5N2O5S |
| CAS号 | 1456632-40-8 | SDF | Download SH-4-54 SDF |
| Smiles | CN(CC(=O)N(CC1=CC=C(C=C1)C2CCCCC2)C3=CC=C(C=C3)C(=O)O)S(=O)(=O)C4=C(C(=C(C(=C4F)F)F)F)F | ||
| 储存条件(自收到货起) | |||
|
体外溶解度 |
DMSO : 100 mg/mL ( (163.77 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 100 mg/mL (163.77 mM) Water : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
技术支持
在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。
如果有其他问题，请给我们留言。
* 必填项
Tags: buy SH-4-54 | SH-4-54 supplier | purchase SH-4-54 | SH-4-54 cost | SH-4-54 manufacturer | order SH-4-54 | SH-4-54 distributor
