PD98059

目录号：S1177 Purity: 99.92%

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

CAS: 167869-21-8

规格	价格	库存
10mM (1mL in DMSO)	RMB 1570	现货
10mg	RMB 1213.08	现货
50mg	RMB 3845.73	现货
200mg	RMB 5489.52	现货
1g	RMB 10401.3	现货
更大包装有超大折扣
400-668-6834 info@selleck.cn

客户使用Selleck的PD98059发表文献482篇

产品质控

批次：纯度： 99.92%

99.92

PD98059相关产品

相关靶点	MEK1 MEK1/2 MEK2 MEK5	点击展开
相关化合物库	激酶抑制剂库 MAPK抑制剂库细胞周期化合物库 TGF-beta/Smad信号通路库抗阿尔茨海默病化合物库	点击展开

MEK抑制剂选择性比较

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
TE4	Function Assay	50 μM	48 h	upregulates the expression of HLA class I	24244023
MKN7	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
NUGC3	Function Assay	50 μM	48 h	increases expression of HLA-A02 or HLA-A24 molecules	24244023
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
ARPE-19	Function Assay	20 μM	0.5 h	inhibits Apelin-induced phosphorylation of Erk and Akt	24227918
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
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
MGC803	Apoptosis Assay	20 μM	1 h	inhibits apoptosis induced by IFN-α and 5′-DFUR	24027750
SGC7901	Apoptosis Assay	20 μM	1 h	inhibits apoptosis induced by IFN-α and 5′-DFUR	24027750
G292	Apoptosis Assay	30 μM	2 h	restores capsaicin-induced cell death	24012930
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
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 dasatinib-induced CD11b expression	23825585
NB4	Function Assay	10 μM	72 h	inhibits dasatinib-induced CD11b expression	23825585
EPOR/CR3	Function Assay	50 μM	3 h	reduces EPO and/or IL-3-induced the tyrosine phosphorylation	23820731
HUASMCs	Function Assay	10 μM	24 h	inhibits Ang II-induced ERK1/2 phosphorylation level	23816468
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
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
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 with Paclitaxel	23735541
HepG2	Function Assay	20 μM	24 h	inhibits the HO-1 protein expression co-treated with metformin	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
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
MC-3	Apoptosis Assay	10 μM	24 h	potentiated MESC-induced apoptosis in cells	24270523
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
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
A549	Function Assay	30 μM	0.5 h	inhibits the thrombin-induced IL-8/CXCL8-Luc activity	24277696
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
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	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
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
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
MDA-MB-231	Function assay	50 uM		Downregulation of MMP2 in human MDA-MB-231 cells at 50 uM by Western blot analysis	22926226
MDA-MB-231	Function assay	50 uM		Downregulation of MMP9 in human MDA-MB-231 cells at 50 uM by Western blot analysis	22926226
HCT-15	Function Assay		1 h	attenuates PGE2-induced phosphorylation of Erk	25431425
HCT-15	Apoptosis Assay		1 h	abolishes the protective effects of PGE2 against curcumin-induced apoptosis	25431425
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
PC12	Function assay			Inhibition of nerve growth factor-mediated MAP kinase activity in human PC12 cells, IC50 = 2 μM.	18077363
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
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD 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
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
点击查看更多细胞系数据

生物活性

产品描述

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
激酶实验	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
实验图片	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

参考文献
[1] Dudley DT, et al. Proc Natl Acad Sci U S A, 1995, 92(17), 7686-7689. [2] Alessi DR, et al. J Biol Chem, 1995, 270(46), 27489-27494. [3] Pang L, et al. J Biol Chem, 1995, 270(23), 13585-13588. [4] Hotokezaka H, et al. J Biol Chem, 2002, 277(49), 47366-47372. [5] Alessandrini A, et al. Proc Natl Acad Sci U S A, 1999, 96(22), 12866-12869. [6] Clemons AP, et al. Pancreas, 2002, 25(3), 251-259. [7] Di Paola R, et al. Int J Immunopathol Pharmacol, 2009, 22(4), 937-950. [8] Mandic A, et al. Melanoma Res, 2001, 11(1), 11-19. [9] Moon DO, et al. Int Immunopharmacol, 2007, 7(1), 36-45. [10] Zelivianski S, et al. Int J Cancer, 2003, 107(3), 478-485. [11] Kojima K, et al. Cancer Res, 2007, 67(7), 3210-3219. [12] J J Reiners Jr, et al. Mol Pharmacol . 1998 Mar;53(3):438-45. + 展开

参考文献

+ 展开

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)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

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
=	×	×

稀释计算器分子量计算器

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）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

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.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):