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Stattic

Stattic, the first nonpeptidic small molecule, potently inhibits STAT3 activation and nuclear translocation with IC50 of 5.1 μM in cell-free assays, highly selectivity over STAT1. Stattic induces apoptosis.

Stattic化学構造

CAS No. 19983-44-9

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 29500 国内在庫あり
JPY 22000 国内在庫なし(納期7~10日)
JPY 55500 国内在庫あり
JPY 145500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール：[email protected]
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Stattic関連製品

シグナル伝達経路

STAT Signaling Pathways

STATシグナル伝達経路

STAT阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
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

製品説明 Stattic, the first nonpeptidic small molecule, potently inhibits STAT3 activation and nuclear translocation with IC50 of 5.1 μM in cell-free assays, highly selectivity over STAT1. Stattic induces apoptosis.
特性 Stattic is the first non-peptide small molecule with inhibitory activity against STAT3 SH2 domain regardless of the STAT3 phosphorylation state in vitro.
Targets
STAT3 [1]
(Cell-free assay)
5.1 μM
In Vitro
In vitro

Stattic inhibits binding of a phosphotyrosine-containing peptide derived from the gp130 receptor to the STAT3 SH2 domain in a strongly temperature-dependent manner. Stattic only has a very weak effect on binding of a tyrosinephosphorylated peptide to the SH2-domain of the tyrosine kinase Lck. And it doesn’t inhibit dimerization of two other dimeric transcription factors (c-Myc/Max and Jun/Jun). It also inhibits fluorescein-labeled phosphopeptides to the SH2 domains of STAT1 and STAT5b. Stattic selectively inhibits DNA binding of STAT3 homodimers at a concentration of 10 μM. Shown to inhibit cellular phosphorylation of STAT3 at Tyr705 with little effect towards STAT1 phosphorylation at Tyr701 (in HepG2 cells) or the phosphorylation of JAK1, JAK2, and c-Src (in MDA-MB-231 and MDA-MB-235S cells). Stattic increases the apoptotic rate of STAT3-dependent breast cancer cell lines. [1]
Kinase Assay High-Throughput Screening and FluorescencePolarization Assays
Screening is performed at approximately 30 °C. The specificity ofscreening hits is validated in analogous assays for binding of thetest compounds to the SH2 domains of STAT1, STAT5, and Lck. The final concentration of buffer components used for all FP assays is 10 mM HEPES (pH 7.5), 1 mM EDTA, 0.1% Nonidet P-40, 50 mM NaCl, and 10% DMSO. The absence of dithiothreitol is essential for inhibitory activity. The sequences of the peptides are: STAT3, 5-carboxyfluorescein-GY(PO3H2)LPQTV-NH2; STAT1, 5-carboxyfluorescein-GY(PO3H2)DKPHVL; STAT5, 5-carboxyfluorescein-GY(PO3H2)LVLDKW; and Lck, 5-carboxyfluorescein-GY(PO3H2)EEIP. For specificity analysis at 30 °C, proteins are used at 150 nM (STAT1, STAT3, and STAT5). For specificity analysis at 37 °C, proteins are used at 370 nM (STAT3) or 100 nM (Lck). Proteins are incubated with test compounds in Eppendorf tubes at the indicated temperatures for 60 min prior addition of therespective 5-carboxyfluorescein labeled peptides (final concentration: 10 nM).Before measurement at room temperature, the mixtures are allowed to equilibrate for at least 30 min. Test compounds are used at the indicated concentrations diluted from a 20× stock in DMSO. Binding curves and inhibition curves are fitted with SigmaPlot. All competition curves are repeated three times in independent experiment
細胞実験 細胞株 Ly3 cells
濃度 ~2.5 μM
反応時間 48 h
実験の流れ

MTS
実験結果図 Methods Biomarkers 結果図 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

化学情報

分子量 211.19 化学式

C8H5NO4S
CAS No. 19983-44-9 SDF Download Stattic SDFをダウンロードする
Smiles C1=CC(=CC2=C1C=CS2(=O)=O)[N+](=O)[O-]
保管

In vitro
Batch:

DMSO : 42 mg/mL ( (198.87 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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Handling Instructions

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