Home JAK/STAT STAT inhibitor - Apoptosis related activator Stattic 仅限科研使用

Stattic

Stattic 是第一个非肽类STAT3小分子抑制剂，有效抑制STAT3激活和核易位，IC50为5.1 μM，其作用于STAT3的选择性远高于STAT1。Stattic 可诱导凋亡。

Stattic Chemical Structure

Stattic Chemical Structure

CAS: 19983-44-9

规格 价格 库存 购买数量
10mM (1mL in DMSO) 1170 现货
25mg 901.23 现货
100mg 2375.1 现货
1g 6470.1 现货
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Stattic相关产品

相关信号通路图

STAT Signaling Pathways

STAT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
CNE2 Function Assay 0-20 μM 0-4 h inhibits Stat3 activation in a dose- and time-dependent manner 23382914
CNE1 Function Assay 0-20 μM 0-4 h inhibits Stat3 activation in a dose- and time-dependent manner 23382914
HONE1 Function Assay 20 µM 48 h blocks the IL-6 increased phosphorylation of Stat3 23382914
CNE2 Function Assay 20 µM 48 h blocks the IL-6 increased phosphorylation of Stat3 23382914
CNE1 Function Assay 20 µM 48 h blocks the IL-6 increased phosphorylation of Stat3 23382914
T24 Function Assay 2/10/20 μM 24 h causes dose-dependent inhibition of the CXCL12-induced increase of invading cells 23526079
SW837 Function Assay 2.5/10 μM 30 min sensitizes cells to chemoradiotherapy in a dose-dependent manner 23934972
W480  Function Assay 2.5/10 μM 30 min sensitizes cells to chemoradiotherapy in a dose-dependent manner 23934972
OV2008 Apoptosis Assay 0-10 μM 24/48 h induces apoptosis in a dose and time dependent manner 23962558
C13* Apoptosis Assay 0-10 μM 24/48 h induces apoptosis in a dose and time dependent manner 23962558
HTR8/SVneo Function Assay 1 μM  48 h significantly increases migration by OSM  24060241
HTR8/SVneo Function Assay 0.5/1 μM  48 h restores the expression of E-cadherin suppressed by OSM 24060241
HTR8/SVneo Function Assay 1 μM  1 h suppressed OSM-induced STAT3 phosphorylation 24060241
HMECs  Function Assay 10 μM 2 h inhibits IFNα mediated phosphorylation of STAT1, STAT2 and STAT3 24211327
MCF7-HER2 Growth Inhibition Assay 5 μM 24 h enhances cell growth inhibition combined with Herceptin 24297508
MCF7-HER2 Function Assay 5 μM 24 h decreases the expression levels of EMT markers, vimentin and slug 24297508
MCF7-HER2 Function Assay 5 μM 24 h diminishes Sox-2, Oct-4, and slug expression 24297508
MCF7-HER2 Growth Inhibition Assay 0-10 μM 48 h induces cell death dose dependently 24297508
SK-BR-3 Function Assay 10 µM 24 h reduces P-STAT3 expression 24376586
SUM-159 Function Assay 10 µM 24 h reduces P-STAT3 expression 24376586
MDA-MB-231 Function Assay 10 µM 24 h reduces P-STAT3 expression 24376586
HaCaT Apoptosis Assay 10 µM 20 min enhances the apoptotic effects of everolimus 24423131
HaCaT Growth Inhibition Assay 10 µM 20 min enhances everolimus-induced cell growth inhibition 24423131
MCF-7/LCC9 Growth Inhibition Assay 0.469-3.75 μM 5 d reduces cell number significantly 24728078
MCF-7/LCC1 Growth Inhibition Assay 0.469-3.75 μM 5 d reduces cell number significantly 24728078
MCF-7 Growth Inhibition Assay 0.469-3.75 μM 5 d reduces cell number significantly 24728078
CD4+ Apoptosis Assay 10 μm 24 h induces apoptosis strongly 24756111
HuT-78 Cell Viability Assay 1-10 μM 72 h causes a dose-dependent inhibition of the viability  24756111
SeAx  Cell Viability Assay 1-10 μM 72 h causes a dose-dependent inhibition of the viability  24756111
SS Cell Viability Assay 1-10 μM 72 h causes a dose-dependent inhibition of the viability  24756111
ELL-primed hNSCs Cell Viability Assay 0.02-5 μM 72 h leads to the loss of cell viability at high concentration 24945434
FHL-primed hNSCs Cell Viability Assay 0.02-5 μM 72 h leads to the loss of cell viability at high concentration 24945434
HaCaT  Apoptosis Assay 10 µM 20 min increases proportions of apoptotic cells due to treatment with sorafenib or sunitinib 25013907
Caki-1 Growth Inhibition Assay 10 µM 20 min enhances sorafenib- and sunitinib-induced growth inhibition 25013907
HaCaT  Growth Inhibition Assay 10 µM 20 min enhances sorafenib- and sunitinib-induced growth inhibition 25013907
H9c2 Function Assay 20 µM 30 min abolishes propofol-induced AKT phosphorylation at both ser473 and thr308 25105067
MDA-MB-231 Function Assay 20 μM 2 h exhibits Snail and E-cadherin expression 25153349
PC3M-1E8 Function Assay 10 μM 24 h inhibits IL-6 induced STAT3 activation and the IL-6-induced STAT3 activation 25261365
PC3M-1E8 Function Assay 10 μM 24 h downregulates Bcl-xL, survivin and c-Myc 25261365
PC3M-1E8 Function Assay 2.5/5/10 μM 0-4 h inhibits the STAT3 activation in a dose- and time-dependent manner  25261365
ECA109 Function Assay 0.5 μM 24 h  enhances IR-induced generation of DSBs 25492480
KYSE150  Clonogenic Survival Assay 0.5 μM 24 h  suppresses the clonogenic formation 25492480
TE13 Clonogenic Survival Assay 0.5 μM 24 h  suppresses the clonogenic formation 25492480
ECA109 Clonogenic Survival Assay 0.5 μM 24 h  suppresses the clonogenic formation 25492480
KYSE150  Growth Inhibition Assay 0-20 μM 24 h  IC50=12.64 μM 25492480
TE13 Growth Inhibition Assay 0-20 μM 24 h  IC50=6.15 μM 25492480
ECA109 Growth Inhibition Assay 0-20 μM 24 h  IC50=5.50 μM 25492480
SiHa Function Assay 5-75 nM 24 h  reduces the phosphorylation at the tyrosine residue 705  25539644
SiHa Cell Viability Assay 5-75 nM 24 h  shows morphology of a typical apoptotic cell and dose-dependent loss of cell viability  25539644
A431 Growth Inhibition Assay 2 μM 2 h increases in apoptosis induced by shikonin 25720435
A431 Growth Inhibition Assay 2 μM 2 h blocks EGF-reversed decreases in cell viability 25720435
H9c2  Function Assay 2/10 μM 2 h abrogates the cytoprotective effects of IL-27 against SH 25820907
HASMC Function Assay 1.25-5 μM 20 min inhibits p-(Y)-STAT-1,3,5 signals  25849622
H9c2 Function Assay 10 μM 4 h reverses the effects of IL-27 26339633
HONE1 Function Assay 0-20 μM 0-4 h inhibits Stat3 activation in a dose- and time-dependent manner 23382914
CNE1 Cell Viability Assay 0.5-64 μM 48 h suppresses cell viability in a dose- and time-dependent manner 23382914
CNE2 Cell Viability Assay 0.5-64 μM 48 h suppresses cell viability in a dose- and time-dependent manner 23382914
HONE1 Cell Viability Assay 0.5-64 μM 48 h suppresses cell viability in a dose- and time-dependent manner 23382914
C666-1  Cell Viability Assay 0.5-64 μM 48 h suppresses cell viability in a dose- and time-dependent manner 23382914
CNE1 Apoptosis Assay 10 µM  48 h induces apoptosis  23382914
CNE2 Apoptosis Assay 10 µM  48 h induces apoptosis  23382914
HONE1 Apoptosis Assay 10 µM  48 h induces apoptosis  23382914
CNE2 Cell Viability Assay 1/2 μM 48 h sensitize cells to radiotherapy 23382914
HONE1 Cell Viability Assay 1/2 μM 48 h sensitize cells to radiotherapy 23382914
C666-1  Cell Viability Assay 1/2 μM 48 h sensitize cells to radiotherapy 23382914
HEC-1A Function Assay 1 μM  24 h blocks the MUC20-enhanced invasion triggered by 10% FBS 23262208
RL95-2 Function Assay 1 μM  24 h blocks the MUC20-enhanced invasion triggered by 10% FBS 23262208
HEC-1A Function Assay 1 μM  24 h blocks the MUC20-enhanced invasion triggered by EGF  23262208
RL95-2 Function Assay 1 μM  24 h blocks the MUC20-enhanced invasion triggered by EGF  23262208
CT26 Function Assay 20 mM 1 h suppresses HGF-induced VEGF expression  23233163
UM-SCC-17B Function Assay 0-30 μM 0-24 h inhibits STAT3 activation dose and time dependently 22770899
OSC-19 Function Assay 0-30 μM 0-24 h inhibits STAT3 activation dose and time dependently 22770899
Cal33 Function Assay 0-30 μM 0-24 h inhibits STAT3 activation dose and time dependently 22770899
UM-SCC-22B Function Assay 0-30 μM 0-24 h inhibits STAT3 activation dose and time dependently 22770899
U-87MG Cell Viability Assay 0-10 μM 72 h inhibits cell viability dose dependently 25436682
U-373MG Cell Viability Assay 0-10 μM 72 h inhibits cell viability dose dependently 25436682
SH-SY5Y Cell Viability Assay 0-10 μM 72 h inhibits cell viability dose dependently 25436682
Tu-9648 Cell Viability Assay 0-10 μM 72 h inhibits cell viability dose dependently 25436682
Neuro-2a Cell Viability Assay 0-10 μM 72 h inhibits cell viability dose dependently 25436682
PCNs Cell Viability Assay 0-10 μM 72 h inhibits cell viability dose dependently 25436682
PGCs Cell Viability Assay 0-10 μM 72 h inhibits cell viability dose dependently 25436682
RAW264.7 Function Assay 10 μM 12 h abrogates the mRNA expressions of JAK2, STAT1, STAT2, and STAT3 induced by DON and T-2 toxin 22454431
RAW264.7 Apoptosis Assay 5/10 μM 45 min enhances toxins induced apoptosis and MMP loss 22454431
SW480 Cell Viability Assay 5/10/20 μM 72 h inhibits cell viability of the ALDH+/CD133+ cells 21900397
HCT116 Cell Viability Assay 5/10/20 μM 72 h inhibits cell viability of the ALDH+/CD133+ cells 21900397
DLD-1  Cell Viability Assay 5/10/20 μM 72 h inhibits cell viability of the ALDH+/CD133+ cells 21900397
SNU387  Cell Viability Assay 20 μM  24 h reduces cell viability 21311975
SNU398 Cell Viability Assay 20 μM  24 h reduces cell viability 21311975
HepG2 Cell Viability Assay 20 μM  24 h reduces cell viability 21311975
Huh-7 Cell Viability Assay 20 μM  24 h reduces cell viability 21311975
VSMC Growth Inhibition Assay 3/5/10 μM 30 min prevents PDGF- and thrombin-mediated VSMC proliferation in a dose-dependent manner 20847306
MDA-MB-231 Apoptosis Assay 10 μM 24 h induces apoptosis 17114005
MDA-MB-435S Apoptosis Assay 10 μM 24 h induces apoptosis 17114005
MDA-MB-231 Function assay 1 to 10 uM 12 hrs Inhibition of STAT3 phosphorylation at Tyr705 in human MDA-MB-231 cells at 1 to 10 uM after 12 hrs by western blot analysis 24904966
MDA-MB-231 Anticancer assay 1 to 10 uM 48 hrs Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition, apoptosis and cellular morphological changes at 1 to 10 uM after 48 hrs by light microscopy 24904966
MDA-MB-231 Function assay 1 to 10 uM 12 hrs Decrease in STAT3 protein expression in human MDA-MB-231 cells at 1 to 10 uM after 12 hrs by western blot analysis 24904966
CNE1 Growth Inhibition Assay 4 μM significantly reduces cell viability 23382914
PC3M-1E8 Clonogenic Survival Assay 2.5/5/10 μM inhibits the colony formation significantly 25261365
NPC  Function Assay 0-7.5 µM abolishes EMT-like molecular alterations, and cell migration and invasion induced by RKIP knockdown 25915430
OV2008 Apoptosis Assay 24/48 h enhances cisplatin-induced apoptosis 23962558
C13* Apoptosis Assay 24/48 h enhances cisplatin-induced apoptosis 23962558
AsPC1 Antiproliferative assay 72 hrs Antiproliferative activity against human AsPC1 cells assessed as inhibition of cell proliferation after 72 hrs by MTS assay, IC50 = 1.32 μM. 24904966
MDA-MB-231 Antiproliferative assay 72 hrs Antiproliferative activity against ER-negative and triple-negative human MDA-MB-231 cells assessed as inhibition of cell proliferation after 72 hrs by MTS assay, IC50 = 2.89 μM. 24904966
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against ER-positive human MCF7 cells assessed as inhibition of cell proliferation after 72 hrs by MTS assay, IC50 = 3.6 μM. 24904966
PANC1 Antiproliferative assay 72 hrs Antiproliferative activity against human PANC1 cells assessed as inhibition of cell proliferation after 72 hrs by MTS assay, IC50 = 3.77 μM. 24904966
MDA-MB-231 Cytotoxicity assay 48 hrs Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50 = 1.56 μM. 26396689
MDA-MB-435S Cytotoxicity assay 48 hrs Cytotoxicity against human MDA-MB-435S cells assessed as growth inhibition after 48 hrs by MTT assay, IC50 = 1.87 μM. 26396689
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50 = 2.16 μM. 26396689
A549 Cytotoxicity assay 48 hrs Cytotoxicity against human A549 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50 = 2.5 μM. 26396689
DU145 Cytotoxicity assay 48 hrs Cytotoxicity against human DU145 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50 = 2.5 μM. 26396689
PANC1 Cytotoxicity assay 48 hrs Cytotoxicity against human PANC1 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50 = 2.9 μM. 26396689
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 1.08 μM. 27718470
MDA-MB-231 Antiproliferative assay 72 hrs Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50 = 1.68 μM. 27718470
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 2.36 μM. 27718470
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50 = 4.4 μM. 27718470
AD293 Function assay 6 hrs Inhibition of IFNgamma-stimulated GFP/FLAG-tagged STAT3 dimerization in human AD293 cells incubated for 6 hrs by Western blot analysis, IC50 = 5.1 μM. 30228000
MCF7 Function assay 12 hrs Inhibition of STAT3 phosphorylation at Y705 in human MCF7 cells after 12 hrs by Western blot analysis 26396689
MDA-MB-435S Function assay 12 hrs Inhibition of STAT3 phosphorylation at Y705 in human MDA-MB-435S cells after 12 hrs by Western blot analysis 26396689
MDA-MB-231 Function assay 12 hrs Inhibition of STAT3 phosphorylation at Y705 in human MDA-MB-231 cells after 12 hrs by Western blot analysis 26396689
UM-SCC-17B Growth Inhibition Assay IC50=2.562 ± 0.409 μM, GI50=1.279 ± 0.194 μM 22770899
OSC-19 Growth Inhibition Assay IC50=3.481 ± 0.953 μM, GI50=1.366 ± 0.770 μM 22770899
Cal33 Growth Inhibition Assay IC50=2.282 ± 0.423 μM, GI50=1.349 ± 0.363 μM 22770899
UM-SCC-22B Growth Inhibition Assay IC50=2.648 ± 0.542 μM, GI50=1.320 ± 0.204 μM 22770899
点击查看更多细胞系数据

生物活性

产品描述 Stattic 是第一个非肽类STAT3小分子抑制剂，有效抑制STAT3激活和核易位，IC50为5.1 μM，其作用于STAT3的选择性远高于STAT1。Stattic 可诱导凋亡。
特性 Stattic是第一个非肽类小分子，抑制STAT3 SH2结构域的功能，无论在体外STAT3磷酸化状态。
靶点
STAT3 [1]
(Cell-free assay)
5.1 μM
体外研究(In Vitro)
体外研究活性

Stattic抑制gp130受体衍生的含磷酸化酪氨酸的肽结合到STAT3 SH2结构域，这种作用存在强烈的温度依赖性。Stattic对酪氨酸磷酸化的肽结合到酪氨酸激酶Lck的SH2结构域只有很微弱的作用效果。Stattic不抑制其他两个二聚体转录因子(c-Myc/Max 和 Jun/Jun)的二聚化。Stattic抑制荧光素标记的磷酸化肽段结合到STAT1和STAT5b的SH2域。Stattic浓度为10 μM，选择性抑制DNA与STAT3二聚体结合。Stattic抑制STAT3在Tyr705位点磷酸化，而对STAT1在Tyr701(HepG2细胞)位点磷酸化或 JAK1, JAK2, 和c-Src(MDA-MB-231和MDA-MB-235S细胞)磷酸化几乎没有抑制效果。Stattic增加STAT3依赖性的乳腺癌细胞系的凋亡率。[1]
激酶实验 高通量筛选和荧光偏振检测
在约30°C下进行筛选。通过实验化合物与STAT1, STAT5, 和 Lck 的SH2结构域结合的类似实验验证筛选的特异性。所有FP实验的Buffer组分的终浓度为10 mM HEPES(pH 7.5),1 mM EDTA,0.1% Nonidet P-40,50 mM NaCl,和10% DMSO。二硫苏糖醇的存在对抑制活性是必不可少的。肽序列为:STAT3,5-carboxyfluorescein-GY(PO3H2)LPQTV-NH2; STAT1, 5-carboxyfluorescein-GY(PO3H2)DKPHVL;STAT5, 5-carboxyfluorescein-GY(PO3H2)LVLDKW; 和 Lck, 5-carboxyfluorescein-GY(PO3H2)EEIP。在 30°C下进行特异性分析, 使用150 nM蛋白(STAT1,STAT3,和STAT5)。在37°C下进行分析，使用370 nM 蛋白(STAT3)或100 nM蛋白 (Lck)。蛋白与实验化合物在Eppendorf管中在指定温度环境下温育60分钟，然后加入相应的5-carboxyfluorescein标记的肽（终浓度为10 nM）。混合物至少平衡30分钟，然后在室温下测量。实验化合物在20×stock在DMSO中稀释到指定浓度。使用 SigmaPlot绘制结合曲线和抑制曲线。独立实验中，所有竞争曲线都需重复三次。
细胞实验 细胞系 Ly3细胞
浓度 ~2.5 μM
孵育时间 48小时
方法

MTS
实验图片 检测方法 检测指标 实验图片 PMID
Western blot PARP / C-PARP / Caspase-3 / C-Caspse-3 Survivin / c-Myc / Bcl-xl p-STAT3 / STAT3 23382914
Immunofluorescence p-STAT3 / STAT3 / Survivin 25261365
Growth inhibition assay Cell viability 23382914
ELISA BDNF 27456333

化学信息&溶解度

分子量 211.19 分子式

C8H5NO4S
CAS号 19983-44-9 SDF Download Stattic SDF
Smiles C1=CC(=CC2=C1C=CS2(=O)=O)[N+](=O)[O-]
储存条件(自收到货起)

体外溶解度
批次：

DMSO : 42 mg/mL ( (198.87 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解配方
批次：

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

摩尔浓度计算器

质量 浓度 体积 分子量

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。

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