化合物 Stattic|T6308|TargetMol

Stattic
19983-44-9

￥257 5mg 起订

￥389 10mg 起订

￥663 25mg 起订

上海更新日期：2024-12-02

TargetMol中国（陶术生物）

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联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 化合物 Stattic

英文名称：: Stattic

CAS号：: 19983-44-9

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.76%

产品类别：: 抑制剂

货号：: T6308

Product Introduction

Bioactivity

名称	Stattic
描述	Stattic (STAT3 Inhibitor V) is a STAT3 inhibitor (IC50=5.1 μM) that selectively inhibits STAT3 activation, dimerization, and nuclear translocation. Stattic has antitumor activity and induces apoptosis.
细胞实验	MDA-MB-231, MDA-MB-435S, and MDA-MB-453 cells were seeded. at 5 × 10^4 cells in 6-well plates, grown for 24 hr before adding DMSO or Stattic (final DMSO concentration 0.1%) and then incubated with the inhibitor for 24 hr. All cells were collected and resuspended in buffer (0.1% sodium citrate, 0.1% Triton X-100, 20 μM propidium iodide) and incubated for 3 hr before 10^4 cells per sample were analyzed by flow cytometry with a FACSCalibur equipped with a 488 nm laser [1].
激酶实验	The screening was performed at approximately 30C. The specificity of screening hits was validated in analogous assays for binding of the test compounds to the SH2 domains of STAT1, STAT5, and Lck. The final concentration of buffer components used for all FP assays was 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 were: 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. Peptides were >95% pure. For specificity analysis at 30°C, proteins were used at 150 nM (STAT1, STAT3, and STAT5). For specificity analysis at 37°C, proteins were used at 370 nM (STAT3) or 100 nM (Lck). Proteins were incubated with test compounds in tubes at the indicated temperatures for 60 min prior addition of the respective 5-carboxyfluorescein labeled peptides (final concentration: 10 nM). Analysis of c-Myc/Max and Jun/Jun dimerization and DNA binding at 37°C was performed as described but in the absence of DTT. Before measurement at room temperature, the mixtures were allowed to equilibrate for at least 30 min. Test compounds were used at the indicated concentrations diluted from 20× stock in DMSO. Binding curves and inhibition curves were fitted with SigmaPlot. All competition curves were repeated three times in independent experiments. For the analysis of time dependence of the inhibition, the components were mixed from stock solutions kept at 0C and then incubated at 37C. Aliquots were taken at the indicated time points [1].
体外活性	方法：人胰腺癌细胞 PANC-1 和 BxPc-3 用 Stattic (1-10 μM) 处理 12-48 h，使用 CCK-8 方法检测细胞活力。结果：Stattic 以浓度和时间依赖的方式降低 PANC-1 和 BxPc-3 细胞增殖。Stattic 处理 24 h 后对 BxPc-3 和 PANC-1 细胞的 IC50 分别为 3.135-5.296 μM 和 3.835-4.165 μM。[1] 方法：人肝癌细胞 HepG2 用 Stattic (5-20 μM) 处理 1 h，随后用 IL-6 或 IFN-γ刺激，使用 Western Blot 方法检测靶点蛋白表达水平。结果：Stattic 的预孵育导致 STAT3 Tyr705 的磷酸化选择性降低，而 STAT1 Tyr701 的激活保持不变。[2]
体内活性	方法：为检测体内抗肿瘤活性，将 Stattic (10 mg/kg) 腹腔注射给携带人胰腺癌肿瘤 PANC-1 的 BALB/c nude 小鼠，每天一次，持续四周。结果：Stattic 通过灭活 STAT3 来抑制裸鼠肿瘤模型中的 PC 生长。[1] 方法：为研究在急性肝损伤中的作用，将 Stattic (5 mg/kg in DMSO:olive oil = 1:19) 单次腹腔注射给 LPS/d-GalN 诱导急性肝损伤的 BALB/c 小鼠。结果：Stattic 对 LPS/d-GalN 诱导的肝损伤具有保护作用，其保护作用可能与其抗炎和抗凋亡作用有关。[3]
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	Ethanol : 1.1 mg/mL (5 mM) 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1.06 mg/mL (5.02 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. DMSO : 55 mg/mL (260.43 mM)
关键字	inhibit \| Alport \| PC3M-1E8 \| cancer \| p-STAT3 \| prostate \| Stattic \| S727 \| Apoptosis \| syndrome \| Inhibitor \| P-ERK1/2 \| SH2 \| STAT \| S phase \| Y705
相关产品	L-Glutamic acid \| Metronidazole \| 5-Fluorouracil \| Dextran sulfate sodium salt (MW 4500-5500) \| Stavudine \| Tributyrin \| Myricetin \| Sorafenib \| L-Ascorbic acid \| Acetylcysteine \| Salicylic acid \| Sodium 4-phenylbutyrate
相关库	抑制剂库 \| 经典已知活性库 \| 已知活性化合物库 \| 细胞凋亡化合物库 \| 高选择性抑制剂库 \| 抗衰老化合物库 \| 干细胞分化化合物库 \| 癌细胞分化化合物库 \| 抗肺癌化合物库 \| 表型筛选靶点鉴定库

STAT3 Inhibitor V|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子