PD 169316
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50值:一种强效的、选择性的及细胞可透过性的p38 MAP激酶抑制剂,IC50值为89 nM。
PD169316是一种特异性的p38 MAPK抑制剂,阻止TGF-β和Activin A,而非骨形态发生蛋白(BMP)4介导的信号转导。对TGF-β信号转导剂量依赖性的抑制随后可减少Smad2和Smad3磷酸化,阻止核易位,增加TGF-β靶基因的表达[1]。
体外实验:经报道,用10 μM的PD169316预处理CaOV3细胞可显著减少TGF-β介导的Smad2和Smad3磷酸化。经证明,PD 169316的抑制效果呈剂量依赖性方式。研究也表明,5 μM或更高剂量的PD169316直接抑制TGF-β信号转导活性[1]。
体内实验:在基于阿尔茨海默病的β淀粉样蛋白(Aβ)大鼠模型中,检测PD 169316对β淀粉样蛋白诱发的细胞凋亡的作用。其表明,PD169316经侧脑室给药预处理的大鼠中,两种细胞凋亡标志物caspase-3和Bax/Bcl-2比率显著减少。该研究表明,PD 169316对Aβ诱发的神经元毒性具有潜在的神经保护作用[2]。
临床试验:到目前为止,还未进行临床试验。
参考文献:
[1]Fu YX, O’Connor LM, Shepherd TG and Nachtigal MW. The p38 MAPK inhibitor, PD169316, inhibits transforming growth factor β-induced Smad signaling in human ovarian cancer cells. Biochem Bioph Res Co. 2003. 310: 3917.
[2]Ashabi G, Alamdary SZ, Ramin M and Khodagholi F. Reduction of hippocampal apoptosis by intracerebroventricular administration of extracellular signal-regulated protein kinase and/or P38 inhibitors in amyloid beta rat model of Alzheimer’s disease: involvement of nuclear-related factor-2 and nuclear factor-κb. Basic Clin. Pharmacol. Toxicol. 2013 Aug. 112: 145–55.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 360.34 |
Cas No. | 152121-53-4 |
Formula | C20H13FN4O2 |
Solubility | insoluble in EtOH; insoluble in H2O; ≥15.3 mg/mL in DMSO |
Chemical Name | 4-[4-(4-fluorophenyl)-2-(4-nitrophenyl)-1H-imidazol-5-yl]pyridine |
SDF | Download SDF |
Canonical SMILES | C1=CC(=CC=C1C2=NC(=C(N2)C3=CC=NC=C3)C4=CC=C(C=C4)F)[N+](=O)[O-] |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
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