|2-(2-氨基-3-甲氧基苯基)-4H-1-苯并吡喃-4-酮|CsnPharm

CAS No.: 167869-21-8

PD98059 Catalog No. CSN11663

Synonyms: NSC 679828;PD098059

PD98059 is a non-ATP competitive MEK inhibitor with IC50 of 2 μM, specifically inhibits MEK-1-mediated activation of MAPK and does not directly inhibit ERK1 or ERK2.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 MEK

IC50:2μM
描述MEKs, which are members of the MAPKK family, can activate both ERK1 and ERK2 by catalyzing the phosphorylation on T202/Y204. Also MEK itself can be phosphorylated and activated through Ras when the upstream signaling is activated by extracellular stimuli, including growth factors, hormones etc.. PD98059 is MEK1/2-specific inhibitor with IC50=~10uM (measured by phosphorylation level of MAPK-KA catalyzed by GST-MEK1) with no effect on ERK. Pre-incubation of PD98059 can inhibit PDGF-stimulated tyrosine phosphorylation of MAPK while preventing thymidine incorporation with an IC50 of 7 uM in 3T3 cells. PD98059 did not show significant inhibitory activity on Raf kinase, cAMP-dependent kinase, protein kinase C, v-Src, EGF receptor kinase, insulin receptor kinase, PDGFreceptor kinase, and PI3Ks, which shows the high selectivity of it ^[1]. PD98059 is the first generation small molecule inhibitors of MEK1/2. PD98059 does not interfere with Raf access to MEK1/2 for it did not affect serum-induced MEK1/2 phosphorylation ^[2].
作用机制PD 098059 does not complete for ATP binding or MAPK binding to MEK and most likely inhibits through an allosteric mechanism.^[1]
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
7402	30 μM	Apoptosis Assay	5 d	decreases cell proliferation	24211253
7721	30 μM	Apoptosis Assay	5 d	decreases cell proliferation	24211253
786-O	50 μM	Apoptosis Assay	24 h	potentiates the pro-apoptotic effects of NC	24508476

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动物研究
剂量
Mice: 10 mg/kg^[3]

给药途径
i.v.

动物研究
剂量	Mice: 10 mg/kg^[3]
给药途径	i.v.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.7414 mL
- 18.7070 mL
- 37.4140 mL
- 5 mM
- 0.7483 mL
- 3.7414 mL
- 7.4828 mL
- 10 mM
- 0.3741 mL
- 1.8707 mL
- 3.7414 mL

技术信息

CAS号

167869-21-8

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H13NO3

运输

蓝冰

分子量

267.28

别名

NSC 679828;PD098059

溶解度

DMSO	25.0 mg/mL (93.5 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+30% PEG300+water	0.5 mg/mL	clear
PO	0.5% CMC-Na	20 mg/mL	suspension

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

7402	30 μM	Apoptosis Assay	5 d	decreases cell proliferation	24211253
7721	30 μM	Apoptosis Assay	5 d	decreases cell proliferation	24211253
786-O	50 μM	Apoptosis Assay	24 h	potentiates the pro-apoptotic effects of NC	24508476
A2780	20 μM	Function Assay	1 h	blocks DTCD-induced DR5 expression	23696862
A375	10–20 µM	Cell Invasion Assay	24 h	reduces melanoma cell invasion	24466036
A498	50 μM	Apoptosis Assay	24 h	potentiates the pro-apoptotic effects of NC	24508476
A549	30 μM	Function Assay	0.5 h	inhibits the thrombin-induced IL-8/CXCL8-Luc activity	24277696
A549	30 μM	Function Assay	0.5 h	inhibits thrombin-induced C/EBPβ Thr235 phosphorylation	24277696
A549	50 μM	Function Assay	2 h	blocks ERK phosphorylation mediated by 1,2-NQ	24067727
AGS	10 μM	Function Assay	0.5 h	inhibits the upregulation of the IL-8 gene	24106166
AML 1#	20 μM	Apoptosis Assay	12 h	enhances cell apoptosis induced by S1	23706691
ARPE-19	20 μM	Function Assay	0.5 h	inhibits Apelin-induced phosphorylation of Erk and Akt	24227918
BeWo	10 μM	Function Assay	2 h	inhibits ERK1/2	24433846
BxPC-3	10 μM	Function Assay	6 h	increase miR-143 expression	23973710
BxPC-3 cells	20 μM	Growth Inhibition Assay	0.5 h	inhibits VEGF-A-regulated HUVEC growth and tube formation induced by PAR-2 AP	23764046
Ca9-22	3 μM	Function Assay	1 h	abolishes the ability of HbR to induce IL-8 production	24126532
Ca9-22	3 μM	Function Assay	1/2 h	reduces HbR-induced ATF-2 phosphorylation	24126532
Caco-2	50 μM	Function Assay	48h	enhances the mRNA levels of SCNN1A,FXYD3, LCT, LOX, HIF3A, ZG16, PDE6A and LGALS16 genes co-treated with Dex	24161695
Caco-2	10 μM	Apoptosis Assay	24 h	decreases cell apoptosis induced by 5-FU	24095863
COLO205	10/20/40 μM	Apoptosis Assay	24 h	induces DNA ladder formation	24019108
CRL-2302	20 μM	Function Assay	0.5 h	inhibits Apelin-induced phosphorylation of Erk and Akt	24227918
DLD-1	20 μM	Function Assay	48 h	reduces the BNIP3 expression pre-treated with 5-aza-dC	24211581
EPOR/CR3	50 μM	Function Assay	3 h	reduces EPO and/or IL-3-induced the tyrosine phosphorylation	23820731
G292	30 μM	Apoptosis Assay	2 h	restores capsaicin-induced cell death	24012930
H1355	25 μM	Function Assay	1 h	blunts the B[a]P-induced increase in phospho-Chk1 and phospho-ERK expression	25769181
HAECs	10 μM	Function Assay	1 h	attenuates TNF-α-stimulated ICAM-1 and VCAM-1 expression	24134657
HBMEC	10 μM	Function Assay	1 h	blocks VEGF-induced EphA2 expression	24458982
HCSMCs	10 μM	Growth Inhibition Assay	24 h	blocks FABP4-induced HCASMC proliferation	24312381
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
HCT-8	10 μM	Apoptosis Assay	24 h	decreases cell apoptosis induced by 5-FU	24095863
HEK 293	10 μM	Function Assay	5 h	inhibits Wnt-induced β-catenin/TCF4 activity and nuclear β-catenin accumulation	24324366
HEK 293	10 μM	Function Assay	5 h	suppresses the CRT activity	24324366
HeLa	50 μM	Function Assay	0.5 h	blocks TRX-1 nuclear migration and TXNIP down-regulation	24376827
HepG2	10 μM	Function Assay	5 h	blocks phosphorylated MAPKs induced by exogenous TGF-β1	25560488
HepG2	20 μM	Growth Inhibition Assay	24 h	suppresses TGF-β1-induced cell proliferation and invasion	25560488
HepG2	20 μM	Apoptosis Assay	24 h	inhibits ERK1/2 phosphorylation and enhances VB1-induced apoptosis	24247909
HepG2	20 μM	Function Assay	2 h	enhances VB1-induced FOXO3a transcriptional activity	24247909
HepG2	40 μM	Function Assay	6/12 h	inhibits the increase of p-ERK1 and p-c-Jun protein expression by PL	23942851
HepG2	20 μM	Function Assay	24 h	inhibits the HO-1 protein expression co-treated with metformin	23707609
HGC-27	1 µM	Apoptosis Assay	1 h	suppresses RAD001 plus MK-2206-induced cell viability loss	24416349
HL60	20 μM	Function Assay	72 h	inhibits dasatinib-induced CD11b expression	23825585
HL-60	10/20 μM	Function Assay	1 h	inhibits the N. chinensisextract induced differentiation into granulocytes	24357020
HL-60	2 µM	Function Assay	16 h	inhibits the association of pS621 Raf-1 and NFATc3, and the RA-induced phosphorylation of nuclear NFATc3	24330068
HL-60	50 μM	Apoptosis Assay	1 h	rescues BA145 mediated apoptosis	23948751
HPAEpiCs	30 μM	Function Assay	1 h	inhibits TNF-α stimulated p42/p44 MAPK phosphorylation	24441870
HPAF-II	10 μM	Function Assay	6 h	increase miR-143 expression	23973710
HPMC	10 μM	Function Assay	48 h	reverses the changes in cell morphology induced by HGPDS	24042838
HPMC	10 μM	Apoptosis Assay	24 h	reverses decrease in cell viability induced by HGPDS	24042838
HT29	10 μM	Function Assay	2 h	inhibits of JAK2, ERK1/2 and STAT3 phosphorylation	24265293
HT-29	20 μM	Function Assay	48 h	reduces the BNIP3 expression pre-treated with 5-aza-dC	24211581
HUASMCs	10 μM	Function Assay	24 h	diminishes Ang II-caused SOCS3 mRNA and protein expression	23816468
HUASMCs	10 μM	Function Assay	24 h	inhibits Ang II-induced ERK1/2 phosphorylation level	23816468
HUVECs	10 μM	Function Assay	1 h	inhibits the HDL reduced COX-2 expression and PGI-2 release	24385109
HUVECs	25 μM	Function Assay	1 h	increase NF-κB p65 nuclear translocation	23901008
HUVECs	2/4 μM	Apoptosis Assay	24/48 h	induces cell death	23707520
KATOIII	50 μM	Function Assay	48 h	increases expression of HLA-A02 or HLA-A24 molecules	24244023
KG-1	20 μM	Apoptosis Assay	12 h	enhances cell apoptosis induced by S1	23706691
KYSE30	20/50/100 μM	Function Assay	48 h	inhibits p-Erk and wortmannin downregulated p-Akt in a dose-dependent manner	24244023
KYSE30	50 μM	Function Assay	48 h	upregulates the expression of HLA class I	24244023
LNCaP	10 μM	Function Assay	1 h	decreases the EGF upregulated p-YB-1	23838318
MC-3	10 μM	Apoptosis Assay	24 h	potentiated MESC-induced apoptosis in cells	24270523
MCF-7	10 μM	Function Assay	1 h	inhibits IL-18-enhanced cell migration	25727011
MCF-7	10 μM	Function Assay	10/30 min	reduces the UTP-dependent ERK phosphorylation	24390819
MCF-7	20 μM	Function Assay	1 h	abolishes expression of phosphorylated ERK co-treatment with conjugate	24216289
MCF-7	20 μM	Apoptosis Assay	1 h	increases caspase-9 enzyme activity	24216289
MCF-7	10 μM	Growth Inhibition Assay	48h	reverses BNF-induced cell cycle arrest	24163404
MDA-MB-231	25 μM	Function Assay	2-3 h	decreases p-ERK1/2 and S100A4 expression	25555875
MG-63	20 μM	Function Assay	0.5 h	blocks the CH-induced phosphorylated ELK1 protein expression	24239640
MGC803	20 μM	Apoptosis Assay	1 h	inhibits apoptosis induced by IFN-α and 5′-DFUR	24027750
MKN45	10 μM	Function Assay	24 h	inhibits the expression of phosphorylated ERK1/2	23792588
MKN45	10 μM	Growth Inhibition Assay	24/48/72 h	inhibits cell growth co-treated with DAPT	23792588
MKN45	10 μM	Apoptosis Assay	24 h	increases the DAPT-induced cell apoptosis	23792588
MKN7	50 μM	Function Assay	48 h	increases expression of HLA-A02 or HLA-A24 molecules	24244023
NB4	10 μM	Function Assay	72 h	inhibits dasatinib-induced CD11b expression	23825585
NB4	10/20/60 μM	Apoptosis Assay	1.5 h	decreases cell viability co-treated with Paclitaxel	23735541
NCI-N87	50 μM	Function Assay	48 h	increases expression of HLA-A02 or HLA-A24 molecules	24244023
NHBE	2/20 μM	Function Assay	2 h	attenuates IL-33 stimulated CXCL8/IL-8 secretion	24479526
NUGC2	50 μM	Function Assay	48 h	increases expression of HLA-A02 or HLA-A24 molecules	24244023
NUGC3	50 μM	Function Assay	48 h	increases expression of HLA-A02 or HLA-A24 molecules	24244023
OE19	50 μM	Function Assay	48 h	increases expression of HLA-A02 or HLA-A24 molecules	24244023
PANC-1	20 μM	Function Assay	48 h	inhibits the expression of Δ6D in response to the PPARδ agonist	24294133
PC3	50 μM	Apoptosis Assay	0.5 h	inhibits MHY-449-induced apoptosis	24424889
Raji	10 μM	Function Assay	1 h	blocks hsBAFF induced Erk1/2 phosphorylation	24269630
Raji	10 μM	Growth Inhibition Assay	1 h	inhibits the basal or hsBAFF-stimulated cell proliferation and viability	24269630
SGC7901	50 μM	Apoptosis Assay	24/48/72 h	induces apoptosis combined with JAK2 shRNA	24178240
SGC7901	20 μM	Apoptosis Assay	1 h	inhibits apoptosis induced by IFN-α and 5′-DFUR	24027750
SGC7901	10 μM	Function Assay	24 h	inhibits the expression of phosphorylated ERK1/2	23792588
SGC7901	10 μM	Growth Inhibition Assay	24/48/72 h	inhibits cell growth co-treated with DAPT	23792588
SGC7901	10 μM	Apoptosis Assay	24 h	increases the DAPT-induced cell apoptosis	23792588
SGC-7901	20 μM	Apoptosis Assay	24 h	inhibits CP-mediated apoptosis	24241351
SMMC7721	25/50 μM	Function Assay	24 h	suppresses the expression of p-Akt or p-ERK1/2	24168056
SW480	20 μM	Function Assay	1 h	reduces the expression of ATF3 protein	25447816
SW480	10 μM	Function Assay	20 h	suppresses the CRT activity	24324366
TE1	20/50/100 μM	Function Assay	48 h	inhibits p-Erk and wortmannin downregulated p-Akt in a dose-dependent manner	24244023
TE1	50 μM	Function Assay	48 h	upregulates the expression of HLA class I	24244023
TE3	50 μM	Function Assay	48 h	upregulates the expression of HLA class I	24244023
TE4	20/50/100 μM	Function Assay	48 h	inhibits p-Erk and wortmannin downregulated p-Akt in a dose-dependent manner	24244023
TE4	50 μM	Function Assay	48 h	upregulates the expression of HLA class I	24244023
TE5	50 μM	Function Assay	48 h	upregulates the expression of HLA class I	24244023

PD98059 Catalog No. CSN11663

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