紫铆因 T6427
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
5 mg | 487-52-5 | ¥698.00 | 询底价 |
50 mg | 487-52-5 | ¥3,680.00 | 询底价 |
25 mg | 487-52-5 | ¥1,960.00 | 询底价 |
10 mg | 487-52-5 | ¥963.00 | 询底价 |
100 mg | 487-52-5 | ¥5,290.00 | 询底价 |
2 mg | 487-52-5 | ¥429.00 | 询底价 |
1 mL | 487-52-5 | ¥683.00 | 询底价 |
1 mg | 487-52-5 | ¥296.00 | 询底价 |
Product Introduction
Bioactivity
英文名: Butein
描述: Butein (2’,3,4,4’-tetrahydroxy Chalcone) 是一种 cAMP 特异性PDE 抑制剂,也是蛋白酪氨酸激酶抑制剂,还是一种SIRT1激活剂。它通过 AKT 和 ERK/p38 MAPK 通路,靶向 FoxO3a 使 HeLa 细胞对 Cisplatin 敏感。
细胞实验: The cells (5× 103/mL) are incubated in triplicate in a 96-well plate in the presence or absence of indicated concentration of Butein in a final volume of 0.2 mL for different time intervals at 37 ℃. Thereafter, 20 μL MTT solution (5 mg/mL in PBS) is added to each well. After a 2-hour incubation at 37 ℃, 0.1 mL lysis buffer (20% SDS, 50% dimethylformamide) is added, incubation is continued overnight at 37 ℃, and then the optical density at 570 nm is measured by plate reader. (Only for Reference)
体外活性: Butein inhibits the epidermal growth factor (EGF)-stimulated auto-phosphotyrosine level of EGF receptor in HepG2 cells, and also inhibits tyrosine-specific protein kinase activities of EGF receptor and p60c-src with IC50 of 65 μM in vitro. The inhibition is competitive to ATP and non-competitive to the phosphate acceptor, poly (Glu, Ala, Tyr) 6:3:1 for EGF receptor tyrosine kinase. In contrast, Butein non-significantly inhibits the activities of serine- and threonine-specific protein kinases such as PKC or PKA. [1] Butein inhibits Nuclear Factor(NF)-κB and NF-κB-regulated gene expression through direct inhibition of IκBα Kinase β on Cysteine 179 Residue. [2] Butein (10 μM) inhibits over 90% iNOS and COX-2 expression, as well as nitrite and TNF-α production in LPS-stimulated RAW 264.7 cells. Butein (10 μM) inhibits LPS-induced DNA binding activity of NF-κB, which is mediated through inhibition of the degradation of inhibitory factor-κB and phosphorylation of Erk1/2 MAP kinase, as well as increases binding of the osteopontin a vb3 integrin receptor. [3] Butein (20 μM) treatment induces morphologic changes of bladder cancer cells BLS(M) from elongated morphology to rounded epithelial-like cells, accompanied by downregulation of vimentin, and gaining of E-cadherin compared to untreated control cells, indicating the reversal of mesenchymal-like phenotype. Butein (20 μM) suppresses motility and invasion capacity of BLS(M) cells, and reverts EMT-like phenotype induced by TNF-α, through the ERK1/2 and NF-κB signaling pathways. [4]
体内活性: Butein at 2 mg/kg induces significant inhibition of hepatocellular tumor growth compared with the corn oil-treated controls. At necropsy on day 22 after initial treatment, there is more than 2-fold decrease in tumor growth in the Butein-treated group (mean relativetumor burden, 3.90) compared with the control group (8.46), associated with reduced constitutive p-STAT3 (9% vs 81% of vehicle group), Bcl-2 levels (26% vs 96% of vehicle group), and increased caspase-3 level (98% vs 21% of vehicle group) in HCC tumor tissues. [5] Butein shows antifibrogenic activity. Butein (25 mg/kg/day) reduces serum AST and ALT activation to 35% and 69%, respectively, of control CCl4-induced rat levels. Butein (25 mg/kg/day) reduces liver hydroxyproline contents and TBAR4 concentration to 54% and 54%, respectively. α1(I) collagen and TIMP-1 expression in Butein-treated rats is 28% and 20.3% compared with the values for the respective CCl4-treated control. [7]
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 51 mg/mL (187.3 mM)
Ethanol : 51 mg/mL (187.3 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
关键字: PDE4 | Epidermal growth factor receptor | Inhibitor | EGFR | MAPK | ErbB-1 | Apoptosis | Autophagy | FoxO3a | inhibit | cell | Butein | SIRT1 | Phosphodiesterase (PDE) | ERK | PKB | AKT | HeLa | HER1 | p38 | HepG2
相关产品: Thioridazine hydrochloride | Neferine | CAY10404 | Verteporfin | Ginkgetin | Tributyrin | Glycochenodeoxycholic Acid | Lorlatinib | HS-173 | Abacavir sulfate
相关库: Anti-Aging Compound Library | Anti-Neurodegenerative Disease Compound Library | Anti-Colorectal Cancer Traditional Chinese Medicine Compound Library | Membrane Protein-targeted Compound Library | Ferroptosis Compound Library | Kinase Inhibitor Library | Inhibitor Library | Tyrosine Kinase Inhibitor Library | Traditional Chinese Medicine Monomer Library | Anti-Alzheimer's Disease Compound Library
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途