PD98059

目录号 M1822 所有产品仅供科研使用，严禁用于人或动物的治疗等任何其他用途，不为任何个人提供产品和服务

PD98059是一种非ATP竞争性的MEK抑制剂，IC50为2 μM，特异性抑制MEK-1介导的MAPK激活；PD98059 是一种 ERK1/2 信号的抑制剂。PD98059抑制ERK信号通路后，细胞内KAT2B蛋白的表达显着降低。

别名：PD 98059; PD‐98059

规格	价格	库存状态
Free Sample (0.5-1 mg)	¥ 0	中国库存现货
10mM*1mL in DMSO	¥ 780	中国库存现货
5mg	¥ 630	中国库存现货
10mg	¥ 900	中国库存现货
25mg	¥ 1500	中国库存现货

其他规格数量报价？

质量标准及产品资料

纯度： 99.83%
COA
MSDS
H-NMR
HPLC

产品信息

生物活性

PD98059是一种非ATP竞争性的MEK抑制剂，IC50为2 μM，特异性抑制MEK-1介导的MAPK激活；PD98059 是一种 ERK1/2 信号的抑制剂。PD98059 要么抑制本底的MEK1，要么抑制一种被部分激活的MEK突变体，该突变体是 218 和 222号位上丝氨酸突变为谷氨酸后形成的(MEK-2E)， IC50 为2 μM. PD98059 不会抑制JNK和P38这两个 MAPK 的同系物. PD98059会高度选择性的抑制MEK, 因为对其它包括Raf 激酶, cAMP-依赖性激酶, 蛋白激酶C, v-Src, 表皮生长因子 (EGF) 受体激酶, 胰岛素受体激酶, PDGF 受体激酶, 和磷脂酰肌醇(-3)激酶等在内的一系列激酶都没有抑制性。 PD98059 会抑制经过PDGF刺激而活化的MAPK 和胸苷进入 3T3 细胞， IC50分别为 ~10 μM 和 ~7 μM 。PD98059可以有效地阻止 MEK1 被Raf 或者MEK 激酶活化， IC50为4 μM, 可以微弱地抑制MEK2被 Raf 活化， IC50 为50 μM。研究表明，PD98059抑制ERK信号通路后，细胞内KAT2B蛋白的表达显着降低，提示17β-E 2 可通过激活ERK信号通路增加KAT2B蛋白表达，从而增强ER活性，增强雌激素效应的正反馈。

使用AbMole产品发表的文献

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产品使用成果展示

	数据来源	Experimental Eye Research (2018). Figure 3. PD98059 (Abmole Bioscience, Houston, TX, USA)
	方法	Western blot
	细胞系/动物模型	ONH astrocytes
	浓度	25 μM
	处理时间	1 h
	实验结果	PD98059 did not significantly reduce the level of p-S6 kinase phosphorylation, but LY294002 showed a robust blockade of its phosphorylation.

	数据来源	PLoS One (2015). Figure 3. PD98059
	方法	Western blot
	细胞系/动物模型	The rats
	浓度	2.5 mcg/5 mcl
	处理时间	16 h
	实验结果	The increased level of ERK1/2 (44/42kDa) in CCI-exposed rats was not observed in group which received repeated administration PD98059

实验参考

体外实验*
细胞系	C-33 and C-81 cells
方法	Treatment with chemotherapeutic agents. Cells were seeded in 6-well culture plates in regular culture medium at a density of 2.5105 and 1105 cells/well for C-33 and C-81 cells, respectively, for 2 days and then fed with SR medium, i.e., PR-free RPMI-1640 medium containing 5% heat-inactivated CS-FBS, 1% glutamine and 0.5% gentamicin. Two days after steroid starvation, one set of attached cells was harvested and counted as day 0. The remaining cells were fed with fresh SR medium and treated with PD98059, U0126, vinorelbine, docetaxel or various combinations in which the dosage of each reagent was specified. Control cells were maintained in SR medium and received solvent alone without chemotherapeutic agents. Fresh SR medium with or without chemotherapeutic agents was added every 3 days. Treatment was continued for 3 or 6 days, as described in each figure legend. To quantify the inhibition of cell growth, attached cells were trypsinized and the cells counted with a Coulter counter. The number of cells in control sets that received solvent alone was designated as 100% for comparison. All experiments were done in triplicate and repeated at least twice.
浓度	0~10 μM
处理时间	3 or 6 days

*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。

体内实验*
动物模型	acute lung injury in mice
配制	DMSO, then diluted with saline
剂量	10mg/kg
给药处理	i. p.

*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。

化学性质

分子量	267.28
分子式	C16H13NO3
CAS号	167869-21-8
溶解性（25°C）	DMSO 15 mg/mL
储存条件	-20°C, dry, sealed, protect from light
运输方式	冰袋运输，根据产品的不同，可能会有相应调整。

储备液配制

*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前，需考虑其在不同溶剂中的溶解度限制。

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	3.7414 mL	18.707 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

不同实验动物依据体表面积的等效剂量转换表（参考来源于公开文献）

	小鼠	大鼠	兔	豚鼠	仓鼠	狗
重量 (kg)	0.02	0.15	1.8	0.4	0.08	10
体表面积 (m²)	0.007	0.025	0.15	0.05	0.02	0.5
K_m 系数	3	6	12	8	5	20

动物 A (mg/kg) = 动物 B (mg/kg) ×	动物 B的K_m系数
	动物 A的K_m系数

例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的K_m系数（3），再除以大鼠的K_m系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。

参考文献

[1] Di Paola R, et al. Int J Immunopathol Pharmacol. Effect of PD98059, a selective MAPK3/MAPK1 inhibitor, on acute lung injury in mice.

[2] Dokladda K, et al. FEBS Lett. PD98059 and U0126 activate AMP-activated protein kinase by increasing the cellular AMP:ATP ratio and not via inhibition of the MAP kinase pathway.

[3] Zelivianski S, et al. Int J Cancer. ERK inhibitor PD98059 enhances docetaxel-induced apoptosis of androgen-independent human prostate cancer cells.

[4] Hur E, et al. Mol Pharmacol. Mitogen-activated protein kinase kinase inhibitor PD98059 blocks the trans-activation but not the stabilization or DNA binding ability of hypoxia-inducible factor-1alpha.

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