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PD98059.

MEK抑制剂,PD98059 是一种 MEK 抑制剂，IC50 为 5 μM，也抑制TCDD结合到芳香烃受体 (AHR)，IC50 为 4 μM。

目录号: PC11746 纯度: ≥98%

CAS No. :167869-21-8

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PC11746-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥539.00	请登录

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中文名称	PD98059.
中文别名	2-(2-氨基-3-甲氧苯基)色酮;PD 098,059 (2-(2-氨基-3-甲氧基苯基)- 4H-1-苯吡喃-4-酮;1,3,5-环己三酸;2-(2-Amino-3-methoxyphenyl)chromone 2-(2-氨基-3-甲氧苯基)色酮;2-(2-氨基-3-甲氧基苯基)-4H-1-苯并吡喃-4-酮;MEK1抑制剂(PD98059);PD98059 抑制剂;2-(2-氨基-3-甲氧苯基)-4H-1-苯并呋喃-4-酮;2-(2-氨基-3-甲氧苯基)-4H-1-苯并吡喃-4-酮;2-(2-氨基-3-甲氧基苯基)-4H-1-苯并吡喃-4-酮, 一种非ATP竞争性的MEK抑制剂
英文名称	PD98059
英文别名	2-(2-Amino-3-methoxyphenyl)-4H-chromen-4-one;2-(2-Amino-3-methoxyphenyl)chromone;2-(2-amino-3-methoxyphenyl)chromen-4-one;4H-1-Benzopyran-4-one,2-(2-amino-3-methoxyphenyl)-;PD 98059 (PD98059,PD 0980599);PD-98059;2-(2-Amino-3-methoxyphenyl)-4H-1-benzopyran-4-one;2-(2-Amino-3-methoxyphenyl)-4H-1-benzopyran-4-one PD98059;2-(2-Amino-3-methoxyphenyl)-chromen-4-one;2'-AMINO-3'-METHOXYFLAVONE;4H-1-Benzopyran-4-one,2-(2-Amino-3-methoxyphenyl);PD 98059;PD090859;PD 098,059;PD 98059 in Solution;InSolution? PD 98059;PD98059;PD 98059, 99+%;PD 98059, >=98%;PD-98059/PD98059;PD 98,059;SJE1IO5E3I;4H-1-Benzopyran-4-one, 2-(2-Amino-3-methoxyphenyl)-;2′-Amino-3′-methoxyflavone;2-(2-amino-3-methoxy-phenyl)chromen-4-one;2-(2-Amino-3-methoxy-ph
Cas No.	167869-21-8
分子式	C₁₆H₁₃NO₃
分子量	267.28
包装储存	Sealed and stored at 4℃ *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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 Mycobacterium bovis Bacillus CalmetteGuerin (BCG)-induced autophagy.

性状

Solid

IC50 & Target[1][2]

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.
PD98059 (10 μM; 22 hours) results in concentration-dependent reductions in the dually phosphorylated forms of ERK1 and ERK2. PD98059 both prevents ERK activation and blocks formation of TDP-43 and HuR-positive SGs.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis

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

Western Blot Analysis

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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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

运输条件

Room temperature or refrigerated transportation.

储存方式

Sealed and stored at 4℃

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

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. [Information]

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

[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. [Information]

[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. [Information]

[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. [Information]

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

溶解度数据

体外研究:

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

H₂O : < 0.1 mg/mL (insoluble)

配制储备溶液

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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： 50% PEG300 50% saline
Solubility: 10 mg/mL (37.41 mM); Suspended solution; Need ultrasonic
2.

建议依照次序添加每种溶剂： 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

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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