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6-硝基苯并[b] 噻吩-1,1-二氧化物

选择性STAT3抑制剂
    级别和纯度:
  • ≥98%
有货

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货号 (SKU) 包装规格 是否现货 价格 数量
S129623-25mg
25mg 现货 Stock Image
S129623-100mg
100mg 现货 Stock Image
S129623-250mg
250mg 现货 Stock Image
S129623-1g
1g 期货 Stock Image

基本描述

英文别名 C8H5NO4S | FT-0621264 | HY-13818 | PB27460 | CCG-222352 | DTXSID70381575 | EC-000.2451 | HMS556B22 | 6-nitro-1lambda6-benzothiophene-1,1-dione | Z595059248 | Maybridge1_005148 | SW219435-1 | CHEBI:86989 | 6-nitro-1 | BCP13194 | HMS3263A18 | Q27159314 | SC
规格或纯度 ≥98%
英文名称 Stattic
生化机理 Stat3 抑制剂 V,Stattic 是一种小分子,可通过阻断磷酸化和二聚化事件选择性地抑制 Stat3 转录因子的激活。Stattic已被用作探测该因子上游活化的工具,该因子在许多癌细胞系中都有显著表达,在乳腺癌细胞系中中断该通路会导致这些细胞的凋亡率增加。Stat3 抑制剂 V,Stattic 是一种 Stat3 抑制剂。通过与 SH2 结构域相互作用,抑制 STAT3 的活化、二聚化和核转运。对 STAT1、STAT5、c-Myc/Max、Jun/Jun 和 Lck 具有选择性。在体外和体内诱导细胞凋亡。
应用 An inhibitor of Stat3 activation
储存温度 -20°C储存
运输条件 超低温冰袋运输
作用类型 抑制剂
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产品介绍

Stattic是STAT3的有效抑制剂,主要用于癌症的治疗。An inhibitor of Stat3 activation


应用:Stattic 是一种有效的 STAT3 抑制剂,可以抑制 STAT3 磷酸化 (磷酸化位点为 Y705 和 S727)。Stattic 抑制高亲和力磷酸肽与 STAT3 的 SH2 域结合。Stattic 可改善 Alport 综合征 (AS) 小鼠的肾功能不全。

Stattic is a potent inhibitor of STAT3, used for cancer treatment.
An inhibitor of Stat3 activation

纯度 ≥98%

关联靶点(人)

HIF1A Tchem 缺氧诱导因子1-α(Hypoxia-inducible factor 1-alpha) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
VDR Tclin Vitamin D receptor (26531 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SRC Tclin Tyrosine-protein kinase SRC (10310 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
APP Tclin Amyloid-beta A4 protein (8510 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ARSA Tbio Cerebroside-sulfatase (655 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
JAK2 Tclin Tyrosine-protein kinase JAK2 (12915 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MTOR Tclin Serine/threonine-protein kinase mTOR (13850 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
STAT3 Tchem Signal transducer and activator of transcription 3 (3313 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DU-145 (51482 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MCF-10A (2462 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MCF7 (126967 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MDA-MB-453 (1139 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MDA-MB-468 (9477 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SH-SY5Y (11521 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
A549 (127892 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HCT-116 (91556 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HEK293 (82097 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HEL (6614 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HepG2 (196354 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MDA-MB-231 (73002 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HIF1A Tchem Hypoxia-inducible factor 1 alpha (6027 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ASPC1 (1310 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
APEX1 Tchem DNA-(apurinic or apyrimidinic site) lyase (38016 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
STAT1 Tchem Signal transducer and activator of transcription 1-alpha/beta (808 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
EHMT2 Tchem Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 (93046 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SNCA Tchem Alpha-synuclein (10960 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
NPC1 Tchem Niemann-Pick C1 protein (18985 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
RAB9A Tbio Ras-related protein Rab-9A (22488 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CBX1 Tbio Chromobox protein homolog 1 (92434 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ATAD5 Tbio ATPase family AAA domain-containing protein 5 (122566 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HSPA5 Tchem 78 kDa glucose-regulated protein (3319 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ATXN2 Tbio Ataxin-2 (54410 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
USP1 Tchem Ubiquitin carboxyl-terminal hydrolase 1 (22556 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
RGS4 Tchem Regulator of G-protein signaling 4 (13867 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MAPK3 Tchem Mitogen-activated protein kinase; ERK1/ERK2 (651 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MEN1 Tchem Menin/Histone-lysine N-methyltransferase MLL (48157 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
L02 (4864 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

关联靶点(其它种属)

Hdac6 Histone deacetylase 6 (222 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Saccharomyces cerevisiae (19171 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Schistosoma japonicum (780 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Schistosoma mansoni (6170 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
B16-F10 (4610 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
GCN5 Histone acetyltransferase GCN5 (89 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
pfk 6-phospho-1-fructokinase (7870 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Txnrd1 Thioredoxin reductase 1, cytoplasmic (45279 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
TGR Thioredoxin glutathione reductase (28579 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Nfe2l2 Nuclear factor erythroid 2-related factor 2 (214 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Rorc Nuclear receptor ROR-gamma (89407 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ffp 4'-phosphopantetheinyl transferase ffp (24982 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Schistosoma haematobium (58 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SARS-CoV-2 (38078 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

作用机制

作用机制 Action Type target ID Target Name Target Type Target Organism Binding Site Name 参考文献

名称和识别符

PubChem SID 504762051
分子类型 小分子
IIUPAC Name 6-nitro-1-benzothiophene 1,1-dioxide
INCHI 1S/C8H5NO4S/c10-9(11)7-2-1-6-3-4-14(12,13)8(6)5-7/h1-5H
InChi Key ZRRGOUHITGRLBA-UHFFFAOYSA-N
Smiles C1=CC(=CC2=C1C=CS2(=O)=O)[N+](=O)[O-]
Isomeric SMILES C1=CC(=CC2=C1C=CS2(=O)=O)[N+](=O)[O-]
PubChem CID 2779853
分子量 211.19

化学和物理性质

溶解性 DMSO 42 mg/mL Water <1 mg/mL Ethanol <1 mg/mL
密度 1.6
折光率 1.67
沸点 461.1° C
熔点 186 - 188 °C
分子量 211.200 g/mol
XLogP3 0.700
氢键供体数Hydrogen Bond Donor Count 0
氢键受体数Hydrogen Bond Acceptor Count 4
可旋转键计数Rotatable Bond Count 0
精确质量Exact Mass 210.994 Da
单同位素质量Monoisotopic Mass 210.994 Da
拓扑极表面积Topological Polar Surface Area 88.300 Ų
重原子数Heavy Atom Count 14
形式电荷Formal Charge 0
复杂度Complexity 375.000
同位素原子数Isotope Atom Count 0
定义的原子立体中心计数Defined Atom Stereocenter Count 0
未定义的原子立体中心计数Undefined Atom Stereocenter Count 0
定义的键立体中心计数Defined Bond Stereocenter Count 0
未定义的键立体中心计数Undefined Bond Stereocenter Count 0
所有立体化学键的总数The total count of all stereochemical bonds 0
共价键合单元计数Covalently-Bonded Unit Count 1

安全和危险性(GHS)

象形图 GHS07
信号词 警告
危险声明

H302: 吞食有害

H315: 引起皮肤刺激

H319: 引起严重眼睛刺激

H335: 可能引起呼吸道刺激

预防措施声明

P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾

P264: 处理后要彻底洗手。

P270: 使用本产品时,请勿进食、饮水或吸烟。

P271: 仅在室外或通风良好的地方使用。

P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。

P321: 特殊处理(请参阅此标签上的...)。

P330: 漱口

P302+P352: 如皮肤沾染:用水充分清洗。

P304+P340: 如误吸入:将人转移到空气新鲜处,保持呼吸舒适体位。

P305+P351+P338: 如进入眼睛:用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出,取出隐形眼镜。继续冲洗。

P362+P364: 脱掉沾污的衣服,清洗后方可重新使用。

P405: 密闭存放

P403+P233: 存放在通风良好的地方。保持容器密闭。

P501: 将内容物/容器处理到。。。

P264+P265: 处理后彻底洗手[和…]。不要触摸眼睛。

P301+P317: 如果被吞咽:请寻求医疗帮助。

P337+P317: 如果眼睛刺激持续:寻求医疗帮助。

P332+P317: 如果出现皮肤刺激:请寻求医疗帮助。

P319: 如果你感到不适,请寻求医疗帮助。

WGK Germany 3
个人防护装备 dust mask type N95 (US), Eyeshields, Gloves

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批号(Lot Number) 证书类型 货号
K2328088 分析证书 S129623
A2206700 分析证书 S129623
C2512631 分析证书 S129623
C2512635 分析证书 S129623
C2512640 分析证书 S129623
C2512641 分析证书 S129623
C2512642 分析证书 S129623
H2223523 分析证书 S129623
H2223521 分析证书 S129623
F2220028 分析证书 S129623
E1718062 分析证书 S129623

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引用文献

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2. Itcho K et al..  (2019)  Angiotensin 1-7 suppresses angiotensin II mediated aldosterone production via JAK/STAT signaling inhibition..  J Steroid Biochem Mol Biol,  185  (137-141).  [PMID:30125658]
3. Katsurahara K et al..  (2021)  ANO9 regulates PD-L2 expression and binding ability to PD-1 in gastric cancer..  Cancer Sci,  112  (3): (1026-1037).  [PMID:33404124]
4. Miyamoto T et al..  (2022)  B7-H3 Suppresses Antitumor Immunity via the CCL2-CCR2-M2 Macrophage Axis and Contributes to Ovarian Cancer Progression..  Cancer Immunol Res,  10  (56-69).  [PMID:34799346]
5. Liu Q et al..  (2022)  CCL5 Suppresses Klotho Expression via p-STAT3/DNA Methyltransferase1-Mediated Promoter Hypermethylation..  Front Physiol,  13  (856088).  [PMID:35299661]
6. Arimoto-Kobayashi S et al..  (2021)  Chemopreventive effects and anti-tumorigenic mechanisms of 2,6-dimethoxy-1,4-benzoquinone, a constituent of Vitis coignetiae Pulliat (crimson glory vine, known as yamabudo in Japan), toward 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK)-induced lung tumorigenesis in A/J mice..  Food Chem Toxicol,  154  (112319).  [PMID:34087405]
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8. Guo X et al..  (2016)  Inhibition of renalase expression and signaling has antitumor activity in pancreatic cancer..  Sci Rep,  (22996).  [PMID:26972355]
9. Yang Y et al..  (2021)  Integrin a5 promotes migration and invasion through the FAK/STAT3/AKT signaling pathway in icotinib-resistant non-small cell lung cancer cells..  Oncol Lett,  22  (556).  [PMID:34084223]
10. Gunjigake K et al..  (2021)  Interleukin-17A derived from mast cells contributes to fibrosis in gastric cancer with peritoneal dissemination..  Gastric Cancer,  24  (31-44).  [PMID:32488650]
11. Wang Y et al..  (2017)  Long non-coding RNA AK093407 promotes proliferation and inhibits apoptosis of human osteosarcoma cells via STAT3 activation..  Am J Cancer Res,  (4): (892-902).  [PMID:28469961]
12. Tang WG et al..  (2017)  Long non-coding RNA00364 represses hepatocellular carcinoma cell proliferation via modulating p-STAT3-IFIT2 signaling axis..  Oncotarget,  (60): (102006-102019).  [PMID:29254221]
13. Mantsounga CS et al..  (2022)  Macrophage IL-1ß promotes arteriogenesis by autocrine STAT3- and NF-?B-mediated transcription of pro-angiogenic VEGF-A..  Cell Rep,  38  (5): (110309).  [PMID:35108537]
14. Zhang Z et al..  (2021)  Neuritin inhibits astrogliosis to ameliorate diabetic cognitive dysfunction..  J Mol Endocrinol,  66  (4): (259-272).  [PMID:33729996]
15. Son YO et al..  (2017)  Nuclear factor erythroid 2-related factor 2 enhances carcinogenesis by suppressing apoptosis and promoting autophagy in nickel-transformed cells..  J Biol Chem,  292  (20): (8315-8330).  [PMID:28330870]
16. Kuo FY et al..  (2020)  Promotion of Adropin Expression by Hyperglycemia Is Associated with STAT3 Activation in Diabetic Rats..  Diabetes Metab Syndr Obes,  13  (2269-2277).  [PMID:32636661]
17. Jiang H et al..  (2017)  Proprotein convertase subtilisin/kexin type 6 promotes in\xa0vitro proliferation, migration and inflammatory cytokine secretion of synovial fibroblast-like cells from rheumatoid arthritis via nuclear-?B, signal transducer and activator of transcription 3 and extracellular signal regulated 1/2 pathways..  Mol Med Rep,  16  (6): (8477-8484).  [PMID:28944919]
18. Kwofie K et al..  (2015)  Regulation of IL-17A responses in human airway smooth muscle cells by Oncostatin M..  Respir Res,  16  (14).  [PMID:25849622]
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20. Timmons GA et al..  (2021)  The Circadian Clock Protein BMAL1 Acts as a Metabolic Sensor In Macrophages to Control the Production of Pro IL-1ß..  Front Immunol,  12  (700431).  [PMID:34858390]
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溶液计算器