|6-硝基苯并[b]噻吩 1,1-二氧化物|CsnPharm

CAS No.: 19983-44-9

6-硝基苯并[b] 噻吩-1,1-二氧化物 Catalog No. CSN10157

Synonyms: STAT3 Inhibitor V

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

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 STAT3

IC50:5.1μM
描述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.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

更多
动物研究
剂量
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.)

给药途径
i.p., s.c., p.o.

动物研究
剂量	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.)
给药途径	i.p., s.c., p.o.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.7350 mL
- 23.6748 mL
- 47.3497 mL
- 5 mM
- 0.9470 mL
- 4.7350 mL
- 9.4699 mL
- 10 mM
- 0.4735 mL
- 2.3675 mL
- 4.7350 mL

技术信息

CAS号

19983-44-9

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C8H5NO4S

运输

蓝冰

分子量

211.19

别名

STAT3 Inhibitor V

溶解度

DMSO	40.0 mg/mL (189.4 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

5% DMSO+40% PEG 300+5% Tween 80+50% water

10 mg/mL

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

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

6-硝基苯并[b] 噻吩-1,1-二氧化物 Catalog No. CSN10157

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