PD98059

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PD98059  纯度: 98.22%

PD98059 是一种有效的选择性的 MEK 抑制剂，IC50 为 5 µM。PD98059 与 MEK 的无活性形式结合，从而阻止上游激酶激活 MEK1 (IC50 为 2-7 µM) 和 MEK2 (IC50 为 50 µM)。PD98059 是一种 ERK1/2 信号的抑制剂。PD98059 是一种芳烃受体 (AHR) 的配体，可抑制细胞中 TCDD 结合 (IC50 为 4 µM) 和 AHR 转化 (IC50 为 1 µM)。PD98059 还可抑制细胞自噬 (autophagy)。

PD98059

PD98059 Chemical Structure

CAS No. : 167869-21-8

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Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥825 In-stock
5 mg ￥750 In-stock
10 mg ￥1083 In-stock
50 mg ￥3100 In-stock
100 mg ￥4100 In-stock
200 mg   询价  
500 mg   询价  

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生物活性

PD98059 is a potent and selective MEK inhibitor with an IC50 of 5 µM. PD98059 binds to the inactive form of MEK, thereby preventing the activation of MEK1 (IC50 of 2-7 µM) and MEK2 (IC50 of 50 µM) by upstream kinases. PD98059 is a ERK1/2 signaling inhibitor. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR), and suppresses TCDD binding (IC50 of 4 μM) and AHR transformation (IC50 of 1 μM). PD98059 also inhibits autophagy[1][2][3].

IC50 & Target[1][3]

MEK1

2-7 μM (IC50)

MEK2

50 μM (IC50)

ERK1

 

ERK2

 

Autophagy

 

体外研究
(In Vitro)

PD98059 (20 μM; 24 hours) causes G1-phase cell cycle arrest in OCI-AML-3 cells[4].
PD98059 (10 μM; 22 hours) results in concentration-dependent reductions in the dually phosphorylated forms of ERK1 and ERK2[1]. PD98059 both prevents ERK activation and blocks formation of TDP-43 and HuR-positive SGs[7].

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.

Cell Cycle Analysis[4]

Cell Line: OCI-AML-3 cells
Concentration: 20 μM
Incubation Time: 24 hours
Result: Caused G1-phase cell cycle arrest.

Western Blot Analysis[1]

Cell Line: MCF10A-Neo, MCF10ANeoT cells
Concentration: 10 μM
Incubation Time: 22 hours
Result: Phosphorylated ERK forms were almost completely eliminated in both cell lines.

体内研究
(In Vivo)

PD98059 (10 mg/kg; i.p.; 1 and 6 hours after Zymosan) significantly reduces the level of p-ERK1/2 in zymosan-injected mice[3].

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: Male CD mice[3]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection; 1 and 6 hours after Zymosan
Result: Significantly reduced the level of p-ERK1/2.

分子量

267.28

Formula

C16H13NO3
CAS 号

167869-21-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶解性数据
In Vitro: 

DMSO : 33.33 mg/mL (124.70 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.7414 mL 18.7070 mL 37.4139 mL
5 mM 0.7483 mL 3.7414 mL 7.4828 mL
10 mM 0.3741 mL 1.8707 mL 3.7414 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 (protect from light)。-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    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (7.78 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (7.78 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 20.8 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
*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]. Reiners JJ Jr, et al. PD98059 is an equipotent antagonist of the aryl hydrocarbon receptor and inhibitor of mitogen-activated protein kinase kinase. Mol Pharmacol. 1998 Mar;53(3):438-45.

    [2]. Alessi DR, et al. PD 098059 is a specific inhibitor of the activation of mitogen-activated protein kinase kinase in vitro and in vivo. J Biol Chem, 1995, 270(46), 27489-27494.

    [3]. Jia Luo, et al. DUSP5 (dual-specificity protein phosphatase 5) suppresses BCG-induced autophagy via ERK 1/2 signaling pathway.

    [4]. Di Paola R, et al. PD98059, a specific MAP kinase inhibitor, attenuates multiple organ dysfunction syndrome/failure (MODS) induced by zymosan in mice. Pharmacol Res. 2010 Feb;61(2):175-87.

    [5]. Kojima K, et al. Mitogen-activated protein kinase kinase inhibition enhances nuclear proapoptotic function of p53 in acute myelogenous leukemia cells. Cancer Res. 2007 Apr 1;67(7):3210-9.

    [6]. Kim KY, et al. Inhibition of Autophagy Promotes Salinomycin-Induced Apoptosis via Reactive Oxygen Species-Mediated PI3K/AKT/mTOR and ERK/p38 MAPK-Dependent Signaling in Human Prostate Cancer Cells. Int J Mol Sci. 2017 May 18;18(5). pii: E1088.

    [7]. Sarah J Parker, et al. Inhibition of TDP-43 accumulation by bis(thiosemicarbazonato)-copper complexes. PLoS One. 2012;7(8):e42277.

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