PD98059

PD98059 is a non-ATP competitive MEK inhibitor with IC50 of 2 μM in a cell-free assay, specifically inhibits MEK-1-mediated activation of MAPK; does not directly inhibit ERK1 or ERK2. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR) and functions as an AHR antagonist.

CAS No. 167869-21-8

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
10mg	JPY 22000	国内在庫あり
50mg	JPY 70500	国内在庫あり
200mg	JPY 100500	国内在庫あり
1g	JPY 190500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（482）

製品安全説明書

現在のバッチを見る：純度： 99.92%

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PD98059関連製品

関連ターゲット	MEK1 MEK1/2 MEK2 MEK5	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library MAPK Inhibitor Library Cell Cycle compound library TGF-beta/Smad compound library Anti-alzheimer Disease Compound Library	もっと見る

シグナル伝達経路

MEKシグナル伝達経路

MEK阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
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
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生物活性

製品説明

PD98059 is a non-ATP competitive MEK inhibitor with IC50 of 2 μM in a cell-free assay, specifically inhibits MEK-1-mediated activation of MAPK; does not directly inhibit ERK1 or ERK2. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR) and functions as an AHR antagonist.

特性

Does not inhibit c-Raf phosphorylated MEK1.

Targets

AhR ^[1] (Cell-free assay)	MEK1 ^[1] (Cell-free assay)
1 μM	2 μM

In Vitro
In vitro	PD98059 inhibits either basal MEK1 or a partially activated MEK produced by mutation of serine at residues 218 and 222 to glutamate (MEK-2E) with IC50 of 2 μM. PD98059 does not inhibit the MAPK homologues JNK and P38. PD98059 is highly selective against MEK, as it does not inhibit a number of other kinase activities including Raf kinase, cAMP-dependent kinase, protein kinase C, v-Src, epidermal growth factor (EGF) receptor kinase, insulin receptor kinase, PDGF receptor kinase, and phosphatidylinositol 3-kinase. PD98059 inhibits PDGF-stimulated activation of MAPK and thymidine incorporation into 3T3 cells with IC50 of ~10 μM and ~7 μM, respectively. ^[1] PD98059 potently prevents the activation of MEK1 by Raf or MEK kinase with IC50 of 4 μM, and weakly inhibits the activation of MEK2 by Raf with IC50 of 50 μM. PD98059 does not inhibit the activation of MEK homologues MKK4 and RK kinase that participate in stress and interleukin-1-stimulated kinase cascades in KB and PC12 cells, and the activation of p70 S6 kinase by insulin or epidermal growth factor in Swiss 3T3 cells. ^[2] PD98059 completely blocks the nerve growth factor (NGF)-induced differentiation of PC12 cells without altering cell viability. ^[3] PD98059 inhibits the proliferation of RAW264.7 cells in the culture containing RANKL in a dose-dependent manner, resulting in an apparent decrease of TRAP-positive cells. ^[4]
Kinase Assay	In vitro MEK-inhibitory activity
Kinase Assay	Incorporation of ³²P into myelin basic protein (MBP) is assayed in the presence of glutathione S-transferase (GST) fusion proteins containing the 44-kDa MAPK (GST-MAPK) or the 45-kDa MEK (GST-MEK1). Assays are conducted in 50 μL of 50 mM Tris, pH 7.4/10 mM MgCl₂/2 mM EGTA/10 μM [γ-³²P]ATP containing 10 μg of GST-MEK1, 0.5 μg of GST-MAPK, and 40 μg of MBP. After incubation at 30°C for 15 minutes, reactions are stopped by addition of Laemmli SDS sample buffer. Phosphorylated MBP is resolved by SDS/10% PAGE.
細胞実験	細胞株	K-Balb, KNRK, v-raf-3Y1, SRA/3Y1, EGFR/3T3, and K562
	濃度	Dissolved in DMSO, final concentrations ~100 μM
	反応時間	3 dyas, or 7-10 days
	実験の流れ	For monolayer growth, cells are plated into multi-well plates at 10,000-20,000/mL. Forty-eight hours later, various concentrations of PD98059 are added to the cell growth medium and incubation is continued for an additional 3 days. Cells are then removed from the wells by incubation with trypsin and enumerated with a Coulter Counter. For growth in soft agar, cells are seeded into 35-mm dishes at 5,000-10,000 cells per dish with growth medium containing 0.3% agar and desired concentrations of PD98059. After 7-10 days of growth, visible colonies are manually enumerated with the aid of a dissecting microscope.
実験結果図	Methods	Biomarkers	結果図	PMID
実験結果図	Western blot	c-Jun / α-tubulin / p-ERK / ERK / p-AKT / AKT p-JNK / JNK / Cyclin D1 p-HER2 / HER2 MMP9 / XIAP / VEGF		17482134

In Vivo
In Vivo	Treatment of mice 30 minutes before focal cerebral ischemia with PD98059 protects against damage, resulting in a decrease in infarct volume. ^[5] Pretreated with PD98059 (10 mg/kg per i.v. injection) 30 minutes before and then together with hourly cerulein injections for 3 hours significantly ameliorates cerulein-induced acute pancreatitis ipancreatitis on the basis of pancreatic wet weight and histology. ^[6] Administration of PD98059 (10 mg/kg) in mice 1 hour after carrageenan causes a reduction in all the parameters of inflammation measured. ^[7]
動物実験	動物モデル	Male Sprague–Dawley rats with acute pancreatitis
	投与量	10 mg/kg
	投与経路	Injection i.v.

参考
[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. + 展開

参考

+ 展開

化学情報

分子量	267.28	化学式	C₁₆H₁₃NO₃
CAS No.	167869-21-8	SDF	Download PD98059 SDFをダウンロードする
Smiles	COC1=CC=CC(=C1N)C2=CC(=O)C3=CC=CC=C3O2
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 46 mg/mL ( (172.1 mM)； Warmed with 50℃ water bath; 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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):