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CAS: 152121-53-4
分子式: C20H13FN4O2
分子量: 360.34
中文名称: 
4-(4-氟苯基)-2-(4-硝基苯基)-5-(4-吡啶基)-1h-咪唑
英文名称: 
pd 169316
4-(4-fluorophenyl)-2-(4-nitrophenyl)-5-(4-pyridyl)-1h-imidazole
用途: PD 169316 是一种高效,细胞透过的,有选择性的 p38 MAP kinase 抑制剂,IC50 值为 89 nM。
推荐供应商
货号品牌产品名称规格包装、参考价格详情
P860866MACKLINPD 169316>97%258元/10mg;   998元/50mg;   1694元/100mg;   2613元/250mg;   6348元/1g;   展开
储存:-20℃
状态:浅黄色到棕色粉末到晶体
折射率:yellow solid
P2532TCIPD 169316>98.0%(HPLC)390元/10MG;   1690元/50MG;   展开

基本信息

纯度/分析方法>98.0%(HPLC)
分子式/分子量C20H13FN4O2 = 360.35
外观与形状(20℃)固体
储存温度0-10℃
应避免的情况加热
Reaxys-RN7660816
PubChem物质ID354335509
MDL编号MFCD12405019

技术规格

AppearanceLight yellow to Brown powder to crystal
Purity(HPLC)min. 98.0 area%
Elemental analysis(Nitrogen)14.70 to 16.30 %

安全信息

危险性说明H413 : 可能对水生生物造成长期持续有害影响。
防范说明P501 : 将内装物/容器送到批准的废物处理厂处理。
P273 : 避免释放到环境中。
618810J&KPD 16931698%, 一种高效, 细胞透过的, 有选择性的 p38 MAP kinase 抑制剂, IC50 值为 89 nM1202元/10MG;   3976元/50MG;   展开

基本信息

分子式C20H113FN4O2
分子量360.34
存储条件Freezer -20℃

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.

安全信息

图形或危害标志
提示语Danger
危险说明H301
H315
H318
H335
防范说明P261
P264
P270
P271
P280
P301+P310
P302+P352
P304+P340
P305+P351+P338
P310
P321
P330
P362
P405
P501
UN号码2811
危险分类6.1
包装等级III
513030Sigma-AldrichPD 169316-CAS 152121-53-4-CalbiochemA potent, cell-permeable, reversible, competitive, and selective p38 MAP kinase inhibitor (IC₅₀ = 89 nM).2340.22元/1 MG;   展开

产品说明

一般描述

A potent, cell-permeable, reversible, competitive, and selective p38 MAP kinase inhibitor (IC50 = 89 nM). Inhibition of p38 MAP kinase by PD 169316 blocks apoptosis induced by trophic factor withdrawal in non-neuronal and neuronal cell lines.
A potent, cell-permeable, reversible, competitive, and selective p38 MAP kinase inhibitor (IC50= 89 nM). Inhibition of p38 MAP kinase by PD 169316 blocks apoptosis induced by trophic factor withdrawal in non-neuronal and neuronal cell lines.

包装

1 mg in Plastic ampoule

生化/生理作用

Cell permeable: yes
Product competes with ATP.
Primary Target
p38 MAP kinase
Reversible: yes
Target IC50: 89 nM against p38 MAP kinase

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 4 months at -20°C.

其他说明

Nath, R., et al. 2001. Cell Mol. Biol. Lett.6, 173.
Gallagher, T.F., et al. 1997. Bioorg. Med. Chem. 5, 49.
Kummer, J.L., et al. 1997. J. Biol. Chem. 272, 20490.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

经验(实验)分子式C20H13FN4O2
分子量360.34
MDL编号MFCD12405019

产品性质

质量水平100
测定≥98% (HPLC)
形式solid
manufacturer/tradenameCalbiochem®
储存条件OK to freeze
protect from light
颜色 orange-yellow
溶解性DMSO: 10 mg/mL
运输ambient
储存温度−20℃

安全信息

象形图GHS05GHS06
警示用语:Danger
危险声明H301 - H315 - H318 - H335
预防措施声明P261 - P264 - P280 - P301 + P310 - P302 + P352 - P305 + P351 + P338
危险分类Acute Tox. 3 Oral - Eye Dam. 1 - Skin Irrit. 2 - STOT SE 3
靶器官Respiratory system
储存分类代码6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable
P9248Sigma-AldrichPD 169316≥98% (HPLC), solid2328.49元/5 MG;   7425.04元/25 MG;   展开

产品说明

一般描述

PD 169316是一种吡啶基咪唑化合物。它是p38丝裂原活化蛋白激酶的一种潜在抑制剂。它也对转化生长因子β(TGFβ)的信号转导进行抑制,特别是在人卵巢癌细胞中。

应用

PD 169316已被用于抑制人肝细胞中的p38酶。它已被用于在培养基中促进胚状体的分化。

包装

5, 25 mg in glass bottle

生化/生理作用

有效的细胞通透型选择性p38激酶抑制剂(IC50 = 89 nM)。

特点和优势

该化合物由GlaxoSmithKline开发。要浏览其他药物开发化合物和批准的药物/候选药物列表,单击此处。

基本信息

经验(实验)分子式C20H13FN4O2
分子量360.34
MDL编号MFCD12405019
PubChem化学物质编号24278156
NACRESNA.77

产品性质

质量水平100
测定≥98% (HPLC)
形式solid
颜色faint yellow to dark orange
溶解性DMSO: >10 mg/mL
H2O: insoluble
创始人GlaxoSmithKline
储存温度2-8℃
SMILES string[O-][N+](=O)c1ccc(cc1)-c2nc(-c3ccc(F)cc3)c([nH]2)-c4ccncc4
InChI1S/C20H13FN4O2/c21-16-5-1-13(2-6-16)18-19(14-9-11-22-12-10-14)24-20(23-18)15-3-7-17(8-4-15)25(26)27/h1-12H,(H,23,24)
InChI keyBGIYKDUASORTBB-UHFFFAOYSA-N
Gene Informationhuman ... MAPK14(1432)

安全信息

象形图GHS05GHS06
警示用语:Danger
危险声明H301 - H315 - H318 - H335
预防措施声明P280 - P301 + P310 + P330 - P302 + P352 - P305 + P351 + P338 + P310
危险分类Acute Tox. 3 Oral - Eye Dam. 1 - Skin Irrit. 2 - STOT SE 3
靶器官Respiratory system
储存分类代码6.1D - Non-combustible, acute toxic Cat.3 / toxic hazardous materials or hazardous materials causing chronic effects
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable
个人防护装备dust mask type N95 (US), Eyeshields, Faceshields, Gloves
M02298FluorochemPD 169,316>98%11462元/25mg;   33242元/100mg;   展开

基本信息

CAS Number152121-53-4
MDL NumberMFCD12405019
CAS号首数字顺序排列: 1 2 3 4 5 6 7 8 9