PD 169316, 98%, a potent, cell-permeable and selective p38 MAP kinase inhibitor,PD 169316 , 98% , 一种高效, 细胞透过的, 有选择性的 p38 MAP kinase 抑制剂, IC50 值为 89 nM
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PD 169316 , 98% , 一种高效, 细胞透过的, 有选择性的 p38 MAP kinase 抑制剂, IC50 值为 89 nM
PD 169316, 98%, a potent, cell-permeable and selective p38 MAP kinase inhibitor
品牌: J&K
产品编号: 618810
分子式: C20H113FN4O2
分子量: 360.34
纯度: 98%
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基本信息

安全信息

存储条件Freezer -20℃
Symbolimageimage
Signal WordDanger
Hazard StatementsH301 H315 H318 H335
Precautionary StatementsP270 P321 P330 P405 P501 P280 P261 P271 P319 P301+P316 P302+P352 P332+P317 P362+P364 P264+P265 P305+P354+P338 P304+P340 P403+P233
UN2811
Hazard Class6.1
Packing GroupIII

化学和物理性质

产品描述

产品描述

PD 169316 is a potent, cell-permeable and selective p38 MAP kinase inhibitor, with IC50 of 89 nM. PD169316 selectively inhibits the kinase activity of the phosphorylated p38 without hindering upstream kinases to phosphorylate p38. PD169316 shows antiviral activity against Enterovirus71. PD169316 shows antiviral activity against Enterovirus71.

靶点(IC50 & Targe)

p38

体外研究

PD169316 (10 μM) inhibits TGFβ and Activin A, but not BMP4 signaling in CaOV3 cells. PD169316 (0.2-20 μM) inhibits TGFβ-induced Smad2 nuclear translocation, Smad7 mRNA induction, and reporter gene activity in CaOV3 cells[1]. PD169316 (10 μM) shows a significantly increased rate of proliferation in Nestin knockdown cells, and can rescue the effect of Nestin knockdown on cell viability in the absence of EGF[2]. PD169316 significantly inhibits p38 MAP kinase activity with no significant change in ERK activity in PC12 cells. PD169316 (10 μM) blocks apoptosis induced by trophic factor withdrawal in differentiated PC12 cells[3].PD169316 (10 μM, 30 min) selectively inhibits the kinase activity of the phosphorylated p38 without hindering upstream kinases to phosphorylate p38. Increased phospho p-38 levels in the presence of PD169316 are most likely due to blockade of negative feedback loop of dephosphorylation of p38 MAPK by MAPK phosphatases[4].Western Blot Analysis[1]

体内研究

PD169316 (1 mg/kg, intramuscular injection every day for 14 consecutive days) shows antiviral activity in a suckling mouse model[5].Animal Model: EV71-challenged suckling mouse model (7-day-old Kunming mice)[5].Dosage: 1 mg/kg.Administration: Intramuscular injection every day for 14 consecutive days.Result: Showed antiviral activity.

参考文献

[1]. Fu Y, et al. The p38 MAPK inhibitor, PD169316, inhibits transforming growth factor beta-induced Smad signaling in human ovarian cancer cells. Biochem Biophys Res Commun. 2003 Oct 17;310(2):391-7.

[2]. Hu W, et al. Suppression of Nestin reveals a critical role for p38-EGFR pathway in neural progenitor cell proliferation. Oncotarget. 2016 Dec 27;7(52):87052-87063.

[3]. Kummer JL, et al. Apoptosis induced by withdrawal of trophic factors is mediated by p38 mitogen-activated protein kinase. J Biol Chem. 1997 Aug 15;272(33):20490-4.

[4]. Khan JA, et al. p38 and p42/44 MAPKs differentially regulate progesterone receptor A and B isoform stabilization. Mol Endocrinol. 2011 Oct;25(10):1710-24.

[5]. Zhang Z, et al. PD169316, a specific p38 inhibitor, shows antiviral activity against Enterovirus71. Virology. 2017 Aug;508:150-158.

参考文献