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Stattic

Stattic 是第一個非肽類STAT3小分子抑制劑，有效抑制STAT3激活和核易位，IC50為5.1 μM，其作用于STAT3的選擇性遠高于STAT1。Stattic 可誘導(dǎo)凋亡。

Stattic Chemical Structure

Stattic Chemical Structure

CAS: 19983-44-9

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 1170 現(xiàn)貨
25mg 901.23 現(xiàn)貨
100mg 2375.1 現(xiàn)貨
1g 6470.1 現(xiàn)貨
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Stattic相關(guān)產(chǎn)品

相關(guān)信號通路圖

STAT Signaling Pathways

STAT信號通路圖

細胞實驗數(shù)據(jù)示例

細胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻信息
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
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生物活性

產(chǎn)品描述 Stattic 是第一個非肽類STAT3小分子抑制劑，有效抑制STAT3激活和核易位，IC50為5.1 μM，其作用于STAT3的選擇性遠高于STAT1。Stattic 可誘導(dǎo)凋亡。
特性 Stattic是第一個非肽類小分子，抑制STAT3 SH2結(jié)構(gòu)域的功能，無論在體外STAT3磷酸化狀態(tài)。
靶點
STAT3 [1]
(Cell-free assay)
5.1 μM
體外研究(In Vitro)
體外研究活性

Stattic抑制gp130受體衍生的含磷酸化酪氨酸的肽結(jié)合到STAT3 SH2結(jié)構(gòu)域，這種作用存在強烈的溫度依賴性。Stattic對酪氨酸磷酸化的肽結(jié)合到酪氨酸激酶Lck的SH2結(jié)構(gòu)域只有很微弱的作用效果。Stattic不抑制其他兩個二聚體轉(zhuǎn)錄因子(c-Myc/Max 和 Jun/Jun)的二聚化。Stattic抑制熒光素標記的磷酸化肽段結(jié)合到STAT1和STAT5b的SH2域。Stattic濃度為10 μM，選擇性抑制DNA與STAT3二聚體結(jié)合。Stattic抑制STAT3在Tyr705位點磷酸化，而對STAT1在Tyr701(HepG2細胞)位點磷酸化或 JAK1, JAK2, 和c-Src(MDA-MB-231和MDA-MB-235S細胞)磷酸化幾乎沒有抑制效果。Stattic增加STAT3依賴性的乳腺癌細胞系的凋亡率。[1]
激酶實驗 高通量篩選和熒光偏振檢測
在約30°C下進行篩選。通過實驗化合物與STAT1, STAT5, 和 Lck 的SH2結(jié)構(gòu)域結(jié)合的類似實驗驗證篩選的特異性。所有FP實驗的Buffer組分的終濃度為10 mM HEPES(pH 7.5),1 mM EDTA,0.1% Nonidet P-40,50 mM NaCl,和10% DMSO。二硫蘇糖醇的存在對抑制活性是必不可少的。肽序列為: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下進行特異性分析, 使用150 nM蛋白(STAT1,STAT3,和STAT5)。在37°C下進行分析，使用370 nM 蛋白(STAT3)或100 nM蛋白 (Lck)。蛋白與實驗化合物在Eppendorf管中在指定溫度環(huán)境下溫育60分鐘，然后加入相應(yīng)的5-carboxyfluorescein標記的肽（終濃度為10 nM）?；旌衔镏辽倨胶?0分鐘，然后在室溫下測量。實驗化合物在20×stock在DMSO中稀釋到指定濃度。使用 SigmaPlot繪制結(jié)合曲線和抑制曲線。獨立實驗中，所有競爭曲線都需重復(fù)三次。
細胞實驗 細胞系 Ly3細胞
濃度 ~2.5 μM
孵育時間 48小時
方法

MTS
實驗圖片 檢測方法 檢測指標 實驗圖片 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

化學(xué)信息&溶解度

分子量 211.19 分子式

C8H5NO4S
CAS號 19983-44-9 SDF Download Stattic SDF
Smiles C1=CC(=CC2=C1C=CS2(=O)=O)[N+](=O)[O-]
儲存條件(自收到貨起)

體外溶解度
批次：

DMSO : 42 mg/mL ( (198.87 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

 動物體內(nèi)配方計算器

實驗計算

摩爾濃度計算器

質(zhì)量 濃度 體積 分子量

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

mg/kg g μL 只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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