PD 169316

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PD 169316

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

152121-53-4

包装与价格：

包装	价格(元)
10mM (in 1mL DMSO)	电议
10mg	电议
50mg	电议

产品介绍

PD 169316 是一种有效的、细胞渗透性和选择性的 p38 MAP 激酶抑制剂，IC50 为 89 nM。 PD169316 选择性抑制磷酸化 p38 的激酶活性，而不阻碍上游激酶磷酸化 p38。 PD169316 显示出针对 Enterovirus71 的抗病毒活性。 PD169316 显示出针对 Enterovirus71 的抗病毒活性。

Cas No.	152121-53-4
别名	4-[4-(4-氟苯基)-2-(4-硝基苯基)-1H-咪唑-5-基]吡啶
化学名	4-[4-(4-fluorophenyl)-2-(4-nitrophenyl)-1H-imidazol-5-yl]pyridine
Canonical SMILES	C1=CC(=CC=C1C2=NC(=C(N2)C3=CC=NC=C3)C4=CC=C(C=C4)F)[N+](=O)[O-]
分子式	C₂₀H₁₃FN₄O₂
分子量	360.34
溶解度	≥ 15.3mg/mL in DMSO
储存条件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	IC50: A potent, selective and cell-permeable suppressor of p38 MAP kinase, with the IC50 value of 89 nM. PD169316, a specific p38 MAPK inhibitor, blocks signal transduction mediated by both TGF-β and Activin A, but not bone morphogenetic protein (BMP) 4. Suppression on TGF-β signaling in a dose-dependent manner may then reduce Smad2 and Smad3 phosphorylation, block nuclear translocation and increase the expression of TGF-β target gene. [1] In vitro: It was reported that pretreatment of CaOV3 cells with 10 M PD169316 caused a significant decrease in Smad2 and Smad3 phosphorylation which was mediated by TGF-β. The inhibitory effect of PD 169316 was proved to act in a dose-dependent manner. Study also demonstrated that PD169316 at 5 M or higher dose directly suppressed TGF-β signaling activity. [1] In vivo: Based on an amyloid β (Aβ) rat model of Alzheimer's disease, the effect of PD 169316 on apoptosis induced by amyloid beta was examined. It was demonstrated that caspase-3 and Bax/Bcl-2 ratio, two marks of apoptosis, were significantly decreased in the rats pre-treated with PD169316 intracerebroventricularly. This study suggested the potential neuroprotective role of PD 169316 against the neuronal toxicity induced by Aβ. [2] Clinical trial: So far, no clinical trial has been conducted. References: [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.