Stattic | STAT3 Inhibitor V | STAT | AmBeed-信号通路专用抑制剂

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产品名称	STAT1 ↓ ↑	STAT3 ↓ ↑	STAT5 ↓ ↑	纯度
Nifuroxazide	✔			98%
Fludarabine	✔			98%
Artesunate		✔		98%
BP-1-102		+++ STAT3, Kd: 504 nM		99%+
Niclosamide		++ STAT3, IC50: 0.7 μM		98%
Napabucasin		✔		98%
Cryptotanshinone		++ STAT3, IC50: 4.6 μM		98%
Stattic		+ STAT3, IC50: 5.1 μM		98%
NSC 74859		+ STAT3, IC50: 86 μM		99%+
Ochromycinone		✔		98%
HO-3867		✔		97%
C188-9		++++ STAT3, Kd: 4.7 nM		99%+
HJC0152		✔		99%
SH5-07		✔		95%
SH-4-54		++++ STAT3, Kd: 300 nM	+++ STAT5, Kd: 464 nM	99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Cell Line CD11b+Ly6G− cells BMDMs THP-1 cells MDA-MB-231 cells MCF-7 cells T47D cells HT-29 cells Caco-2 cells HPV-KER cells RAW264.7 macrophages Raw264.7 cells 786-O cells MDA-MB-436 cells HGC-27 cells	Concentration	Treated Time	Description	References
CD11b+Ly6G− cells	10 μM	2 h	inhibits STAT3 activation and nuclear translocation	J Am Heart Assoc. 2020 Sep 15;9(18):e017071.
BMDMs	10 μM	24 h	Inhibited STAT3 activation and downregulated CD206 and Il-10 expression	Gut Microbes. 2022 Jan-Dec;14(1):2145843.
THP-1 cells	5 μM	1 hour	Stattic inhibited TNC-induced STAT3 activation and TNF-α production	Cancer Res. 2019 May 15;79(10):2697-2708.
MDA-MB-231 cells	10 μmol/ml	12 h	Stattic treatment significantly inhibited CAF-induced MDA-MB-231 cell colony formation and reversed CAF-induced radioresistance	Cell Death Discov. 2023 Jan 13;9(1):6.
MCF-7 cells	10 μmol/ml	12 h	Stattic treatment significantly inhibited CAF-induced MCF-7 cell colony formation and reversed CAF-induced radioresistance	Cell Death Discov. 2023 Jan 13;9(1):6.
T47D cells	10 μmol/ml	12 h	Stattic treatment significantly inhibited CAF-induced T47D cell colony formation and reversed CAF-induced radioresistance	Cell Death Discov. 2023 Jan 13;9(1):6.
HT-29 cells	10 μM	24 h	To examine the effect of Stattic on STAT3 activity, results showed that Stattic inhibited STAT3 activity.	Theranostics. 2018 Apr 30;8(11):3022-3037.
Caco-2 cells	10 μM	24 h	To examine the effect of Stattic on STAT3 activity, results showed that Stattic inhibited STAT3 activity.	Theranostics. 2018 Apr 30;8(11):3022-3037.
HPV-KER cells	5 µM	1 hour	To study the effect of Stattic on the STAT3 signaling pathway in HPV-KER cells	Front Immunol. 2018 Sep 24;9:2155.
RAW264.7 macrophages	10 nmol/mL	1 hour	Stattic almost entirely abrogated TGF-β1–induced PD-1 expression in macrophages	JCI Insight. 2024 Mar 5;9(7):e165544.
Raw264.7 cells	10 μM	24 h	Inhibited STAT3 activation and downregulated CD206 and Il-10 expression	Gut Microbes. 2022 Jan-Dec;14(1):2145843.
786-O cells	5 μM	24 h	Stattic effectively inhibited STAT3 in the presence of BEZ235, significantly enhancing the anti-proliferative effects of BEZ235 on PTEN-deficient cancer cells.	Oncogenesis. 2021 Jan 5;10(1):8.
MDA-MB-436 cells	5 μM	24 h	Stattic effectively inhibited STAT3 in the presence of BEZ235, significantly enhancing the anti-proliferative effects of BEZ235 on PTEN-deficient cancer cells.	Oncogenesis. 2021 Jan 5;10(1):8.
HGC-27 cells	5 μM	24 h	Stattic effectively inhibited STAT3 in the presence of BEZ235, significantly enhancing the anti-proliferative effects of BEZ235 on PTEN-deficient cancer cells.	Oncogenesis. 2021 Jan 5;10(1):8.

Species Mice Mice Mice Nude mice	Animal Model Myocardial infarction model TGF-β1-induced chronic inflammation model DSS-induced acute colitis model HGC-27 and MDA-MB436 xenograft models	Administration	Dosage	Frequency	Description	References
Mice	Myocardial infarction model	Intraperitoneal injection	20 mg/kg	Daily for 3 days	Inhibits STAT3 phosphorylation, reduces the number of MerTK+ galectin-3hi macrophages	J Am Heart Assoc. 2020 Sep 15;9(18):e017071.
Mice	TGF-β1-induced chronic inflammation model	Intraperitoneal injection	75 μg/mouse	For 5 consecutive days	Stattic completely abrogated TGF-β1–induced PD-1 expression on peritoneal macrophages	JCI Insight. 2024 Mar 5;9(7):e165544.
Mice	DSS-induced acute colitis model	Intraperitoneal injection	4 mg/kg	Once every two days for 14 days	Inhibited STAT3 activation and attenuated the anti-inflammatory effect of L. johnsonii	Gut Microbes. 2022 Jan-Dec;14(1):2145843.
Nude mice	HGC-27 and MDA-MB436 xenograft models	Intra-peritoneally	3.75 mg/kg	Daily for 20 days	Combination treatment with BEZ235 and Stattic significantly inhibited the growth of HGC-27 and MDA-MB436 xenograft tumors, and the combination was more effective than BEZ235 alone.	Oncogenesis. 2021 Jan 5;10(1):8.

细胞研究

细胞系	浓度	检测类型	检测时间	活性说明	数据源

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

靶点	STAT3 STAT3, IC50:5.1 μM
描述	Stattic acts as a potent inhibitor of STAT3 and impedes STAT3 phosphorylation at Y705 and S727 ^[1]. Stattic hampers the binding of a high-affinity phosphopeptide for the SH2 domain of STAT3 ^[2]. Stattic improves renal function in Alport syndrome (AS) mice ^[3].
体内研究	Stattic (10 mg/kg, intraperitoneally, three times per week for 10 weeks) improves renal function in Alport syndrome (AS) mice ^[3].
体外研究	Stattic (20 μM; 24 hours) inhibits STAT3 phosphorylation at Y705 and selectively inhibits P-STAT3, as evidenced by the lack of inhibition of P-ERK1/2 in ALDH⁺ and D44⁺/CD24⁺ subpopulations of Panc-1 and HPAC pancreatic cancer cell lines ^[1]. Stattic (2.5, 5, 10 μM; for 4 h) significantly decreases the nuclear levels of pSTAT3 and survivin at 10 μM. Stattic (2.5-10 μM; for 24 h) dose-dependently inhibits IL-6-induced STAT3 activation in PC3M-1E8 cells ^[2]. Stattic (2.5, 5, 10 μM; for 48 h) suppresses both the growth and induces apoptosis in prostate cancer cells (PC3M-1E8 cells) at 10 μM. However, no significant cell apoptosis is induced with 2.5 μM or 5 μM ^[2]. Stattic (2.5, 5, 10 μM; for 48 h) results in significant accumulation of cells in the S phase ^[2]. Stattic does not induce significant morphological changes or apoptosis and exhibits minimal STAT3 phosphorylation in A2780 cells and HUVECs ^[2].

Dose	Mice: 10 mg/kg^[3] (i.p.), 1 mg/kg^[4] (i.p.); 10 mg/kg^[5] (s.c.); 50 mg/kg^[6] (p.o.)
Administration	i.p., s.c., p.o.

CAS号	19983-44-9
分子式	C₈H₅NO₄S
分子量	211.19
SMILES Code	O=[N+](C1=CC=C(C=CS2(=O)=O)C2=C1)[O-]
MDL No.	MFCD00173799

别名	STAT3 Inhibitor V
运输	蓝冰
InChI Key	ZRRGOUHITGRLBA-UHFFFAOYSA-N
Pubchem ID	2779853

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