PD 169316

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PD 169316  纯度: 98.0%

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。PD169316 选择性地抑制磷酸化 p38 的激酶活性,但不阻碍上游激酶磷酸化 p38。PD169316 显示对 Enterovirus71 有抗病毒活性。

PD 169316

PD 169316 Chemical Structure

CAS No. : 152121-53-4

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥990 In-stock
10 mg ¥900 In-stock
50 mg ¥2500 In-stock
100 mg ¥4500 In-stock
500 mg ¥14500 In-stock
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5 g   询价  

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PD 169316 相关产品

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生物活性

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.

IC50 & Target

IC50: 89 nM (p38 MAPK)[5]

体外研究
(In Vitro)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: Ishikawa PRB or PRA cells.
Concentration: 10 μM.
Incubation Time: 30 min.
Result: Did not inhibit MEKK1-induced p38 phosphorylation.

体内研究
(In Vivo)

PD169316 (1 mg/kg, intramuscular injection every day for 14 consecutive days) shows antiviral activity in a suckling mouse model[5].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

360.34

Formula

C20H13FN4O2

CAS 号

152121-53-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 12.5 mg/mL (34.69 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7752 mL 13.8758 mL 27.7516 mL
5 mM 0.5550 mL 2.7752 mL 5.5503 mL
10 mM 0.2775 mL 1.3876 mL 2.7752 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 1.25 mg/mL (3.47 mM); Suspended solution; Need ultrasonic

    此方案可获得 1.25 mg/mL (3.47 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 1.25 mg/mL (3.47 mM); Suspended solution; Need ultrasonic

    此方案可获得 1.25 mg/mL (3.47 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 1.25 mg/mL (3.47 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (3.47 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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.

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