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PD98059

PD98059 是一种非ATP竞争性的MEK抑制剂，无细胞试验中IC50为2 μM，特异性抑制MEK-1介导的MAPK激活；不直接抑制ERK1或ERK2。PD98059 是一种aryl hydrocarbon receptor (AHR)的配体并起到拮抗剂的功能。

PD98059 Chemical Structure

PD98059 Chemical Structure

CAS: 167869-21-8

规格 价格 库存 购买数量
10mM (1mL in DMSO) 1570 现货
10mg 1213.08 现货
50mg 3845.73 现货
200mg 5489.52 现货
1g 10401.3 现货
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相关信号通路图

MEK Signaling Pathways

MEK信号通路图

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
NUGC2 Function Assay 50 μM 48 h increases expression of HLA-A02 or HLA-A24 molecules 24244023
SGC-7901  Apoptosis Assay 20 μM 24 h inhibits CP-mediated apoptosis 24241351
MG-63 Function Assay 20 μM 0.5 h blocks the CH-induced phosphorylated ELK1 protein expression 24239640
HCT-15 Apoptosis Assay 1 h abolishes the protective effects of PGE2 against curcumin-induced apoptosis 25431425
786-O Apoptosis Assay 50 μM 24 h potentiates the pro-apoptotic effects of NC 24508476
HepG2  Growth Inhibition Assay 20 μM 24 h suppresses TGF-β1-induced cell proliferation and invasion 25560488
SW480 Function Assay 20 μM 1 h reduces the expression of ATF3 protein 25447816
MDA-MB-231 Function Assay 25 μM 2-3 h decreases p-ERK1/2 and S100A4 expression 25555875
HepG2  Function Assay 10 μM 5 h blocks phosphorylated MAPKs induced by exogenous TGF-β1 25560488
MCF-7  Function Assay 10 μM 1 h inhibits IL-18-enhanced cell migration 25727011
H1355 Function Assay 25 μM 1 h blunts the B[a]P-induced increase in phospho-Chk1 and phospho-ERK expression 25769181
PC12 Function assay Inhibition of nerve growth factor-mediated MAP kinase activity in human PC12 cells, IC50 = 2 μM. 18077363
HT-29 Antiproliferative assay 5 days Antiproliferative activity against human HT-29 cells after 5 days by WST1 assay, IC50 = 4 μM. 25078316
IEC6 Function assay 5 mins Inhibition of MEK1/2 in rat IEC6 cells assessed as reduction in ERK1/2 loop phosphorylation dosed 30 mins before to stimulation with 10% serum for 5 mins by immunoblotting method, IC50 = 4.2 μM. 25078316
NG 108-15 Function assay Concentration required to abolish MAPK activity in mouse neuroblastoma and rat glioma hybrid NG 108-15 cells, Activity = 10 μM. 15537354
PC12 Function assay 10 uM 5 hrs Activation of Nrf2/ARE in rat PC12 cells assessed as HO-1 protein induction at 10 uM after 5 hrs pretreated with JNK inhibitor SP600125 for 1 hr before compound addition by Western blot analysis 21345685
SW480 Function Assay 10 μM 20 h suppresses the CRT activity 24324366
HEK 293 Function Assay 10 μM 5 h inhibits Wnt-induced β-catenin/TCF4 activity and nuclear β-catenin accumulation 24324366
HEK 293 Function Assay 10 μM 5 h suppresses the CRT activity 24324366
HL-60  Function Assay 10/20 μM 1 h inhibits the N. chinensisextract induced differentiation into granulocytes 24357020
HL-60 Function Assay 2 µM 16 h inhibits the association of pS621 Raf-1 and NFATc3, and the RA-induced phosphorylation of nuclear NFATc3 24330068
HeLa Function Assay 50 μM 0.5 h blocks TRX-1 nuclear migration and TXNIP down-regulation 24376827
HUVECs Function Assay 10 μM 1 h inhibits the HDL reduced COX-2 expression and PGI-2 release 24385109
MCF-7 Function Assay 10 μM 10/30 min reduces the UTP-dependent ERK phosphorylation 24390819
HGC-27 Apoptosis Assay 1 µM 1 h suppresses RAD001 plus MK-2206-induced cell viability loss 24416349
PC3  Apoptosis Assay 50 μM 0.5 h inhibits MHY-449-induced apoptosis  24424889
HPAEpiCs  Function Assay 30 μM 1 h inhibits TNF-α stimulated p42/p44 MAPK phosphorylation 24441870
BeWo Function Assay 10 μM 2 h inhibits ERK1/2 24433846
A498 Apoptosis Assay 50 μM 24 h potentiates the pro-apoptotic effects of NC 24508476
NHBE Function Assay 2/20 μM 2 h attenuates IL-33 stimulated CXCL8/IL-8 secretion 24479526
A375 Cell Invasion Assay 10–20 µM 24 h reduces melanoma cell invasion 24466036
HBMEC Function Assay 10 μM 1 h blocks VEGF-induced EphA2 expression 24458982
A549 Function Assay 30 μM 0.5 h inhibits thrombin-induced C/EBPβ Thr235 phosphorylation 24277696
HCSMCs Growth Inhibition Assay 10 μM 24 h blocks FABP4-induced HCASMC proliferation 24312381
PANC-1 Function Assay 20 μM 48 h inhibits the expression of Δ6D in response to the PPARδ agonist  24294133
Raji  Function Assay 10 μM 1 h blocks hsBAFF induced Erk1/2 phosphorylation 24269630
Raji  Growth Inhibition Assay 10 μM 1 h inhibits the basal or hsBAFF-stimulated cell proliferation and viability 24269630
TE5 Function Assay 50 μM 48 h upregulates the expression of HLA class I 24244023
TE1 Function Assay 50 μM 48 h upregulates the expression of HLA class I 24244023
TE3 Function Assay 50 μM 48 h upregulates the expression of HLA class I 24244023
KYSE30 Function Assay 20/50/100 μM 48 h inhibits p-Erk and wortmannin downregulated p-Akt in a dose-dependent manner 24244023
TE1 Function Assay 20/50/100 μM 48 h inhibits p-Erk and wortmannin downregulated p-Akt in a dose-dependent manner 24244023
TE4 Function Assay 20/50/100 μM 48 h inhibits p-Erk and wortmannin downregulated p-Akt in a dose-dependent manner 24244023
HT29 Function Assay 10 μM 2 h inhibits of JAK2, ERK1/2 and STAT3 phosphorylation 24265293
HepG2 Apoptosis Assay 20 μM 24 h inhibits ERK1/2 phosphorylation and enhances VB1-induced apoptosis 24247909
HepG2 Function Assay 20 μM 2 h enhances VB1-induced FOXO3a transcriptional activity 24247909
MDA-MB-231 Function assay 50 uM Downregulation of MMP9 in human MDA-MB-231 cells at 50 uM by Western blot analysis 22926226
MKN45 Apoptosis Assay 10 μM  24 h increases the DAPT-induced cell apoptosis 23792588
BxPC-3 cells Growth Inhibition Assay 20 μM 0.5 h inhibits VEGF-A-regulated HUVEC growth and tube formation induced by PAR-2 AP 23764046
NB4  Apoptosis Assay 10/20/60 μM 1.5 h decreases cell viability co-treated 23735541
HepG2  Function Assay 20 μM 24 h inhibits the HO-1 protein expression co-treated 23707609
HUVECs Apoptosis Assay 2/4 μM 24/48 h induces cell death 23707520
KG-1  Apoptosis Assay 20 μM 12 h enhances cell apoptosis induced by S1 23706691
AML 1# Apoptosis Assay 20 μM 12 h enhances cell apoptosis induced by S1 23706691
A2780  Function Assay 20 μM 1 h blocks DTCD-induced DR5 expression 23696862
KYSE30 Function Assay 50 μM 48 h upregulates the expression of HLA class I 24244023
MKN45 Growth Inhibition Assay 10 μM  24/48/72 h inhibits cell growth co-treated with DAPT 23792588
SGC7901 Growth Inhibition Assay 10 μM  24/48/72 h inhibits cell growth co-treated with DAPT 23792588
MKN45 Function Assay 10 μM  24 h inhibits the expression of phosphorylated ERK1/2 23792588
SGC7901 Apoptosis Assay 10 μM  24 h increases the DAPT-induced cell apoptosis 23792588
HUASMCs Function Assay 10 μM  24 h diminishes Ang II-caused SOCS3 mRNA and protein expression  23816468
SGC7901 Function Assay 10 μM  24 h inhibits the expression of phosphorylated ERK1/2 23792588
HUASMCs Function Assay 10 μM  24 h inhibits Ang II-induced ERK1/2 phosphorylation level 23816468
LNCaP  Function Assay 10 μM  1 h decreases the EGF upregulated p-YB-1 23838318
HUVECs Function Assay 25 μM 1 h increase NF-κB p65 nuclear translocation 23901008
HL60  Function Assay 20 μM 72 h inhibits -induced CD11b expression 23825585
NB4  Function Assay 10 μM  72 h inhibits -induced CD11b expression 23825585
EPOR/CR3 Function Assay 50 μM 3 h reduces EPO and/or IL-3-induced the tyrosine phosphorylation  23820731
COLO205 Apoptosis Assay 10/20/40 μM 24 h induces DNA ladder formation 24019108
BxPC-3 Function Assay 10 μM  6 h increase miR-143 expression 23973710
HPAF-II Function Assay 10 μM  6 h increase miR-143 expression 23973710
HepG2 Function Assay 40 μM 6/12 h inhibits the increase of p-ERK1 and p-c-Jun protein expression by PL 23942851
HL-60 Apoptosis Assay 50 μM 1 h rescues BA145 mediated apoptosis 23948751
SGC7901 Apoptosis Assay 20 μM 1 h inhibits apoptosis induced by IFN-α and 5′-DFUR 24027750
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
MDA-MB-231 Function assay 50 uM Downregulation of MMP2 in human MDA-MB-231 cells at 50 uM by Western blot analysis 22926226
PC12 Function assay 10 uM 5 hrs Activation of Nrf2/ARE in rat PC12 cells assessed as HO-1 protein induction at 10 uM after 5 hrs pretreated with MEK1 inhibitor PD98059 for 1 hr before compound addition by Western blot analysis 21345685
HeLa Function assay 20 uM 3 hrs Inhibition of ERK1/2 phosphorylation in human HeLa cells at 20 uM after 3 hrs by Western blotting analysis 23570615
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
PC12 Function assay 10 uM 5 hrs Activation of Nrf2/ARE in rat PC12 cells assessed as HO-1 protein induction at 10 uM after 5 hrs pretreated with MEK2 inhibitor U0126 for 1 hr before compound addition by Western blot analysis 21345685
MCF-7 Function Assay 20 μM 1 h abolishes expression of phosphorylated ERK co-treatment with conjugate 24216289
7402 Apoptosis Assay 30 μM 5 d decreases cell proliferation 24211253
HT-29 Function Assay 20 μM 48 h reduces the BNIP3 expression pre-treated with 5-aza-dC 24211581
DLD-1  Function Assay 20 μM 48 h reduces the BNIP3 expression pre-treated with 5-aza-dC 24211581
7721 Apoptosis Assay 30 μM 5 d decreases cell proliferation 24211253
SGC7901  Apoptosis Assay 50 μM 24/48/72 h induces apoptosis combined with JAK2 shRNA 24178240
SMMC7721 Function Assay 25/50 μM 24 h suppresses the expression of p-Akt or p-ERK1/2  24168056
MCF-7 Growth Inhibition Assay 10 μM 48h reverses BNF-induced cell cycle arrest 24163404
Caco-2 Function Assay 50 μM 48h enhances the mRNA levels of SCNN1A,FXYD3, LCT, LOX, HIF3A, ZG16, PDE6A and LGALS16 genes co-treated with Dex 24161695
HAECs Function Assay 10 μM 1 h  attenuates TNF-α-stimulated ICAM-1 and VCAM-1 expression 24134657
Ca9-22 Function Assay 3 μM 1 h abolishes the ability of HbR to induce IL-8 production 24126532
Ca9-22 Function Assay 3 μM 1/2 h reduces HbR-induced ATF-2 phosphorylation 24126532
AGS Function Assay 10 μM  0.5 h inhibits the upregulation of the IL-8 gene 24106166
Caco-2  Apoptosis Assay 10 μM 24 h decreases cell apoptosis induced by 5-FU 24095863
A549 Function Assay 50 μM 2 h blocks ERK phosphorylation mediated by 1,2-NQ 24067727
HPMC Function Assay 10 μM 48 h reverses the changes in cell morphology induced by HGPDS 24042838
HCT-8 Apoptosis Assay 10 μM 24 h decreases cell apoptosis induced by 5-FU 24095863
HPMC Apoptosis Assay 10 μM 24 h reverses decrease in cell viability induced by HGPDS 24042838
CRL-2302 Function Assay 20 μM 0.5 h inhibits Apelin-induced phosphorylation of Erk and Akt 24227918
MCF-7 Apoptosis Assay 20 μM 1 h increases caspase-9 enzyme activity 24216289
HCT-15 Function Assay 1 h attenuates PGE2-induced phosphorylation of Erk  25431425
A549 Function Assay 30 μM 0.5 h inhibits the thrombin-induced IL-8/CXCL8-Luc activity 24277696
MC-3 Apoptosis Assay 10 μM 24 h potentiated MESC-induced apoptosis in cells 24270523
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells 29435139
G292  Apoptosis Assay 30 μM 2 h restores capsaicin-induced cell death 24012930
MGC803  Apoptosis Assay 20 μM 1 h inhibits apoptosis induced by IFN-α and 5′-DFUR 24027750
ARPE-19 Function Assay 20 μM 0.5 h inhibits Apelin-induced phosphorylation of Erk and Akt 24227918
NUGC3 Function Assay 50 μM 48 h increases expression of HLA-A02 or HLA-A24 molecules 24244023
OE19 Function Assay 50 μM 48 h increases expression of HLA-A02 or HLA-A24 molecules 24244023
NCI-N87  Function Assay 50 μM 48 h increases expression of HLA-A02 or HLA-A24 molecules 24244023
KATOIII  Function Assay 50 μM 48 h increases expression of HLA-A02 or HLA-A24 molecules 24244023
MKN7 Function Assay 50 μM 48 h increases expression of HLA-A02 or HLA-A24 molecules 24244023
TE4 Function Assay 50 μM 48 h upregulates the expression of HLA class I 24244023
点击查看更多细胞系数据

生物活性

产品描述 PD98059 是一种非ATP竞争性的MEK抑制剂，无细胞试验中IC50为2 μM，特异性抑制MEK-1介导的MAPK激活；不直接抑制ERK1或ERK2。PD98059 是一种aryl hydrocarbon receptor (AHR)的配体并起到拮抗剂的功能。
特性 PD98059不会抑制已经被c-Raf磷酸化的 MEK1
靶点
AhR [1]
(Cell-free assay)		 MEK1 [1]
(Cell-free assay)
1 μM 2 μM
体外研究(In Vitro)
体外研究活性

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 [1]。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。 在KB 和 PC12 细胞中, PD98059 不会抑制MKK4 和RK激酶这两个参与压力和白细胞介素-1介导的激酶级联反应的MEK的同系物的活化，在Swiss 3T3 细胞中也不会通过胰岛素或者表皮生长因子抑制p70 S6 激酶的活化[2]。PD98059会在不改变细胞生存能力的情况下完全阻断 神经生长因子(NGF)诱导的 PC12 细胞的分化[3] 。PD98059会以剂量依赖性的方式抑制培养在含有破骨细胞分化因子培养基中的 RAW264.7细胞的增值，进而导致TRAP阳性细胞数量明显下降[6]。
激酶实验 体外MEK激酶活性测定
在含有44-kDa GST-MAPK 或者45-kDa GST-MEK1的体系中检测32P被掺入蛋白 MBP中的情况。 反应体系50 μL ，含有50 mM Tris, pH 7.4/10 mM MgCl2/2 mM EGTA/10 μM [γ-32P]ATP， 加入10 μg GST-MEK1, 0.5 μg GST-MAPK和 40 μg MBP。30°C 孵育15 分钟, 加入Laemmli SDS 样品缓冲液终止反应。磷酸化的MBP 进行10% SDS-PAGE分析
细胞实验 细胞系 K-Balb, KNRK, v-raf-3Y1, SRA/3Y1, EGFR/3T3, 和K562
浓度 溶于DMSO, 终浓度~100 μM
孵育时间 3 天, 或者7-10天
方法

细胞按10,000-20,000个/mL的密度接种在多孔平板中进行单层生长。48小时后把不同浓度的PD98059 加到细胞培养基孵育3天。 然后通过胰酶将细胞从平板中消化下来并用Coulter 计数器计数。 将细胞按5,000-10,000每皿的浓度接种在35 mm的培养皿中，培养基中含有0.3% 的琼脂和期望浓度的PD98059，让细胞在软琼脂上生长.经过7-10天的生长, 可以借助解剖显微镜将可见的菌落数出来。
实验图片 检测方法 检测指标 实验图片 PMID
Western blot c-Jun / α-tubulin / p-ERK / ERK / p-AKT / AKT p-JNK / JNK / Cyclin D1 p-HER2 / HER2 MMP9 / XIAP / VEGF 17482134
体内研究(In Vivo)
体内研究活性

在大脑缺血前30分钟用PD98059处理小鼠可以明显减轻伤害, 使脑梗塞的体积减小[4]。基于胰腺的湿重和组织学研究发现，提前30分钟用PD98059预处理 (10 mg/kg 静脉注射) 然后每小时注射一次蛙皮素连续三次的小鼠可以明显改善蛙皮素诱导的急性胰腺炎[7]。卡拉胶损伤一小时后用PD98059 (10 mg/kg) 对小鼠进行治疗可以发现与炎症相关的所有指标均有所下降[11]。
动物实验 Animal Models 患有急性胰腺炎的雄性Sprague–Dawley 大鼠
Dosages 10 mg/kg
Administration 静脉注射

化学信息&溶解度

分子量 267.28 分子式

C16H13NO3
CAS号 167869-21-8 SDF Download PD98059 SDF
Smiles COC1=CC=CC(=C1N)C2=CC(=O)C3=CC=CC=C3O2
储存条件(自收到货起)

体外溶解度
批次：

DMSO : 46 mg/mL ( (172.1 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次：

现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂

 动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

mg/kg g μL 只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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常见问题及建议解决方法

问题 1:
How to formulate this inhibitor for i.p. injection?

回答：
You can prepare the stock by the vehicle 30% PEG400/0.5% Tween80/5% Propylene glycol, 0.5% CMC.

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