PD98059

Catalog No.S1177

Molecular Weight(MW): 267.28

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.

Cited by 190 Publications

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J Transl Med, 2015, 13(1):42

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Purity & Quality Control

Choose Selective MEK Inhibitors

Biological Activity

Description

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.

Features

Does not inhibit c-Raf phosphorylated MEK1.

Targets

MEK1 ^[1]
(Cell-free assay)

2 μM

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]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
H1355	NIrHd5BHfW6ldHnvckBCe3OjeR?=	NEX3dIszPSEQvF2=	MVGxJIg>		NV7HTGJ2[my3boTzJJRp\SCEW3HdVE1qdmS3Y3XkJIlv[3KnYYPlJIlvKHCqb4PwbI8uS2itMTDhcoQheGixc4Doc{1GWktiZYjwdoV{e2mxbh?=	M{PVXVI2PzZ7MUix
MCF-7	MnLLSpVv[3Srb36gRZN{[Xl?	MmK4NVAh\|ryP	MX2xJIg>		NHrB[m1qdmirYnn0d{BKVC1zOD3lcohidmOnZDDj[YxtKG2rZ4LheIlwdg>?	NFrsUnQzPTd{N{CxNS=>
HepG2	NWLXbJk{TnWwY4Tpc44hSXO\|YYm=	NGS1OIkyOCEQvF2=	NUXvNZI1PSCq		NYPsWWxy[myxY3vzJJBpd3OyaH;yfYxifGWmIF3BVGt{KGmwZIXj[YQh[nliZYjv[4Vvd3W\|IGTHSk3PujF?	Mmm2NlU2PjB2OEi=
HepG2	NYDsdo1OT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NEDsVmgzOCEQvF2=	MWCyOEBp		MYXzeZBxemW\|c3XzJHRITi4QskGtbY5lfWOnZDDj[YxtKHC{b3zp[oVz[XSrb36gZY5lKGmwdnHzbY9v	NFuyepMzPTV4MES4PC=>
MDA-MB-231	MXHGeY5kfGmxbjDBd5NigQ>?	NE\IPWwzPSEQvF2=	NEjiZZczNTNiaB?=		NVHz[28y\GWlcnXhd4V{KHBvRWLLNU8zKGGwZDDTNVAxSTRiZYjwdoV{e2mxbh?=	Mlf4NlU2PTV6N{W=
SW480	M1XxSGZ2dmO2aX;uJGF{e2G7	M3fhOlIxyqEQvF2=	NFXUVFUyyqCq		MV\y[YR2[2W\|IITo[UBmgHC{ZYPzbY9vKG:oIFHUSlMheHKxdHXpci=>	NWHTc5k{OjV2NEe4NVY>
HCT-15	M2PZRWZ2dmO2aX;uJGF{e2G7		NHToS5EyKGh?		NI\2XYFifHSnboXheIV{KFCJRUKtbY5lfWOnZDDwbI9{eGixconsZZRqd25ib3[gSZJsyqB?	NIjWelEzPTR\|MUSyOS=>
HCT-15	NHv5UlJCeG:ydH;zbZMhSXO\|YYm=		NXHwUYM4OSCq		NGnSS2ti[m:uaYPo[ZMhfGinIIDyc5Rm[3SrdnWg[YZn\WO2czDv[kBRT0V{wrDh[4FqdnO2IHP1doN2dWmwLXnu[JVk\WRiYYDvdJRwe2m\|	MWCyOVQ{OTR{NR?=
786-O	MknvRZBweHSxc3nzJGF{e2G7	MoPlOVDDqM7:TR?=	M4HRd\|I1KGh?		NFmxN2Fxd3SnboTpZZRme8LidHjlJJBzdy2jcH;weI91cWNiZX\m[YN1eyCxZjDORy=>	NYDUOHpQOjR3MEi0O\|Y>
A498	NXKwTYRzSXCxcITvd4l{KEG\|c3H5	M3XwW\|UxyqEQvF2=	MUmyOEBp		MWfwc5RmdnSrYYTld:KhfGinIIDyc{1ieG:ydH;0bYMh\W[oZXP0d{Bw\iCQQx?=	Mni0NlQ2ODh2N{[=
NHBE	NH34RpdHfW6ldHnvckBCe3OjeR?=	MXuyM\|IxKM7:TR?=	NI\2XmIzKGh?		NF76doVifHSnboXheIV{KEmOLUOzJJN1cW23bHH0[YQhS1iFTEivTWwuQCC\|ZXPy[ZRqd25?	MlWzNlQ1Pzl3Mk[=
A375	NH32Z3VE\WyuIFnueoF{cW:wIFHzd4F6	NW\YepA6OTEkgKOyNEDDvU1?	NYfyRnptOjRiaB?=		M4e0cpJm\HWlZYOgcYVt[W6xbXGgZ4VtdCCrbo\hd4lwdg>?	NWnHcGl4OjR2Nk[wN\|Y>
HBMEC	MXPGeY5kfGmxbjDBd5NigQ>?	NX:4XVdnOTBizszN	MkP5NUBp		MV3icI9kc3NiVlXHSk1qdmS3Y3XkJGVxcEF{IHX4dJJme3Orb36=	MoPNNlQ1PTh7OEK=
HPAEpiCs	MlnMSpVv[3Srb36gRZN{[Xl?	Ml3JN\|Ah\|ryP	NUXhSXY3OSCq		NHvwTINqdmirYnn0d{BVVkZvzsGgd5RqdXWuYYTl[EBxPDJxcES0JG1CWEticHjvd5Bpd3K7bHH0bY9v	MVeyOFQ1OTh5MB?=
BeWo	NHzm[nBHfW6ldHnvckBCe3OjeR?=	NXruc4JGOTEEoN88US=>	MYqyJIg>		MmDqbY5pcWKrdIOgSXJMOS9{	MXuyOFQ{Ozh2Nh?=
PC3	Mn3WRZBweHSxc3nzJGF{e2G7	NXzhPJNtPTBizszN	M1LB[FAvPSCq		NYfXcI8{cW6qaXLpeJMhVUi\LUS0PU1qdmS3Y3XkJIFxd3C2b4Ppd:Kh	M4K4WlI1PDJ2OEi5
HGC-27	M3eyZWFxd3C2b4Ppd{BCe3OjeR?=	MV:xJOK2VQ>?	Mn:3NUBp		M3XOU5N2eHC{ZYPz[ZMhWkGGMECxJJBtfXNiTVutNlIxPi2rbnT1Z4VlKGOnbHygeoli[mmuaYT5JIxwe3N?	MUmyOFQyPjN2OR?=
MCF-7	NYXZeJg3TnWwY4Tpc44hSXO\|YYm=	MX2xNOKh\|ryP	M1XjS\|ExNzNyIH3pci=>		Mn;XdoVlfWOnczD0bIUhXVSSLXTldIVv\GWwdDDFVmsheGixc4Doc5J6dGG2aX;u	M2DPUVI1OzlyOEG5
HUVECs	MU\GeY5kfGmxbjDBd5NigQ>?	MXqxNOKh\|ryP	NHrwSI4yKGh?		MV\pcohq[mm2czD0bIUhUESOIILl[JVk\WRiQ1;YMVIh\XiycnXzd4lwdiCjbnSgVGdKNTJicnXs[YF{\Q>?	NXvQU2trOjR\|OEWxNFk>
HeLa	M1L5V2Z2dmO2aX;uJGF{e2G7	MUi1NEDPxE1?	MnXYNE42KGh?		NV2xT4Z1[myxY3vzJHRTYC1zIH71Z4xm[XJibXnndoF1cW:wIHHu[EBVYE6LUDDkc5dvNXKnZ4XsZZRqd25?	MVSyOFM4Pjh{Nx?=
HL-60	MXPGeY5kfGmxbjDBd5NigQ>?	NW[xZlhVOTBxMkCg{txO	NYnH[IdNOSCq		NEfnco9qdmirYnn0d{B1cGYEoF6uJINpcW6nboPpd4V5fHKjY4VCpIlv\HWlZXSg[Iln\mW{ZX70bYF1cW:wIHnueI8h\3KjboXsc4N6fGW\|	NV2wU5ZVOjR\|NUewNlA>
HL-60	NGfxUJFHfW6ldHnvckBCe3OjeR?=	NVz1VWFxOiEEtV2=	MmjlNVYhcA>?	NYrsXoZpTE2VTx?=	NEDyWWFqdmirYnn0d{B1cGViYYPzc4Nq[XSrb36gc4YheFN4MkGgVoFnNTFiYX7kJG5HSVSlMzygZY5lKHSqZTDSRU1qdmS3Y3XkJJBpd3OyaH;yfYxifGmxbjDv[kBvfWOuZXHyJG5HSVSlMx?=	MlfnNlQ{OzByNki=
HEK 293	M3\SOmZ2dmO2aX;uJGF{e2G7	NXyy[mVHOTBizszN	M1eydlUhcA>?	MkLKSG1UVw>?	M1XyV4lvcGmkaYTzJHdvfC2rbnT1Z4VlKM7{LXPheIVvcW5xVFPGOEBi[3Srdnn0fUBidmRiboXjcIVieiEQsj3jZZRmdmmwIHHjZ5VufWyjdHnvci=>	NGfEN2QzPDN{NEO2Oi=>
HEK 293	NVzxfXlETnWwY4Tpc44hSXO\|YYm=	M{\QeFExKM7:TR?=	MojrOUBp	M1O2[mROW09?	M2[wRpN2eHC{ZYPz[ZMhfGinIFPSWEBi[3Srdnn0fS=>	MVWyOFMzPDN4Nh?=
SW480	NI\yTHdHfW6ldHnvckBCe3OjeR?=	MnjMNVAh\|ryP	NVG0e3RDOjBiaB?=	MXzEUXNQ	NYLqZm1Pe3WycILld5NmeyC2aHWgR3JVKGGldHn2bZR6	NEfudHozPDN{NEO2Oi=>
HCSMCs	NUeyblNsT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NF\Ne3UyOCEQvF2=	MUWyOEBp		MnniZoxw[2u\|IF\BRnA1NWmwZIXj[YQhUEODU13DJJBzd2yrZnXyZZRqd25?	NVjx[nlkOjR\|MUKzPFE>
PANC-1	NWXldJc4TnWwY4Tpc44hSXO\|YYm=	M3fW[VIxKM7:TR?=	NXzpUJZKPDhiaB?=		NH;5UJpqdmirYnn0d{B1cGViZYjwdoV{e2mxbjDv[kDPnD[GIHnuJJJme3CxboPlJJRwKHSqZTDQVGFT\|rUEoHHnc45qe3UEoB?=	MX6yOFI6PDF\|Mx?=
A549	MmDmSpVv[3Srb36gRZN{[Xl?	NFnsTZY{OCEQvF2=	MnTWNE42KGh?	NVPZR3JqTE2VTx?=	NVj4W4xIcW6qaXLpeJMhfGinIITodo9u[mmwLXnu[JVk\WRiSVytPE9EYEOOOD3MeYMh[WO2aY\peJk>	NFrTfG0zPDJ5N{[5Oi=>
A549	M4XJbmZ2dmO2aX;uJGF{e2G7	MYSzNEDPxE1?	MnrzNE42KGh?	MonZSG1UVw>?	NVLtS25LcW6qaXLpeJMhfGi{b33ibY4ucW6mdXPl[EBEN0WEUN8yJHRpejJ\|NdMgdIhwe3Cqb4L5cIF1cW:w	NH61VZUzPDJ5N{[5Oi=>
MC-3	MX;BdI9xfG:\|aYOgRZN{[Xl?	MV[xNEDPxE1?	MkiwNlQhcA>?		NH;2OY1xd3SnboTpZZRm\CCPRWPDMYlv\HWlZXSgZZBweHSxc3nzJIlvKCClZXzsdy=>	NV;rWZdxOjR{N{C1NlM>
Raji	MWDGeY5kfGmxbjDBd5NigQ>?	MkLyNVAh\|ryP	MYCxJIg>		NYLSTI9G[myxY3vzJIh{SkGIRjDpcoR2[2WmIFXyb\|EwOiCyaH;zdIhwenmuYYTpc44>	MUWyOFI3QTZ\|MB?=
Raji	NFexVFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NYrFO5hXOTBizszN	NVfwbFFjOSCq		Ml3zbY5pcWKrdIOgeIhmKGKjc3HsJI9zKGi\|QlHGSk1{fGmvdXzheIVlKGOnbHygdJJwdGmoZYLheIlwdiCjbnSgeoli[mmuaYT5	MlvHNlQzPjl4M{C=
HT29	NIj4SXJHfW6ldHnvckBCe3OjeR?=	NIe5bY8yOCEQvF2=	MXiyJIg>		M{GzTYlvcGmkaYTzJI9nKEqDS{KsJGVTUzFxMjDhcoQhW1SDVEOgdIhwe3Cqb4L5cIF1cW:w	MmCwNlQzPjV{OUO=
HepG2	NWX1TVZxSXCxcITvd4l{KEG\|c3H5	NWXlcnR7OjBizszN	MUeyOEBp		NETVOnJqdmirYnn0d{BGWktzL{KgdIhwe3Cqb4L5cIF1cW:wIHHu[EBmdmijbnPld{BXSjFvaX7keYNm\CCjcH;weI9{cXN?	Mk\nNlQzPDd7MEm=
HepG2	M1LWZ2Z2dmO2aX;uJGF{e2G7	M2i1WFIxKM7:TR?=	Mk\DNkBp		NVP3[I9I\W6qYX7j[ZMhXkJzLXnu[JVk\WRiRl;YU\|NiKHS{YX7zZ5JqeHSrb37hcEBi[3Srdnn0fS=>	MlqzNlQzPDd7MEm=
TE4	M{DUVWZ2dmO2aX;uJGF{e2G7	M1jVVlIxNzVyL{GwNEDPxE1?	MkXmOFghcA>?	MV3EUXNQ	M{HZ[YlvcGmkaYTzJJAuTXKtIHHu[EB4d3K2bXHucolvKGSxd37y[Yd2dGG2ZXSgdE1Cc3RiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ?	Moi0NlQzPDRyMkO=
TE1	Mm[xSpVv[3Srb36gRZN{[Xl?	NWfqRm5VOjBxNUCvNVAxKM7:TR?=	NFfTfYM1QCCq	MYTEUXNQ	M4m5WYlvcGmkaYTzJJAuTXKtIHHu[EB4d3K2bXHucolvKGSxd37y[Yd2dGG2ZXSgdE1Cc3RiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ?	NHy1SI8zPDJ2NECyNy=>
KYSE30	MVvGeY5kfGmxbjDBd5NigQ>?	MVOyNE82OC9zMECg{txO	NHXHOJA1QCCq	MlT6SG1UVw>?	M{\TR4lvcGmkaYTzJJAuTXKtIHHu[EB4d3K2bXHucolvKGSxd37y[Yd2dGG2ZXSgdE1Cc3RiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ?	MVeyOFI1PDB{Mx?=
TE1	M1jTNmZ2dmO2aX;uJGF{e2G7	MVq1NEDPxE1?	M2LUd\|Q5KGh?	MXHEUXNQ	Mkn3eZBz\We3bHH0[ZMhfGinIHX4dJJme3Orb36gc4YhUEyDIHPsZZN{KEl?	MVuyOFI1PDB{Mx?=
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KYSE30	NWrr[nhOTnWwY4Tpc44hSXO\|YYm=	NYC0UVloPTBizszN	M174SVQ5KGh?	NGnGfFVFVVOR	M1XzOpVxemWpdXzheIV{KHSqZTDlfJBz\XO\|aX;uJI9nKEiOQTDjcIF{eyCL	MViyOFI1PDB{Mx?=
MKN7	MXnGeY5kfGmxbjDBd5NigQ>?	M2TYUlUxKM7:TR?=	MV60PEBp	NXrhN3gxTE2VTx?=	MYHpcoNz\WG\|ZYOg[ZhxemW\|c3nvckBw\iCKTFGtRVAzKG:{IFjMRU1COjRibX;s[YN2dGW\|	MmixNlQzPDRyMkO=
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KATOIII	MlXhSpVv[3Srb36gRZN{[Xl?	MUe1NEDPxE1?	M4exUlQ5KGh?	MWfEUXNQ	MWHpcoNz\WG\|ZYOg[ZhxemW\|c3nvckBw\iCKTFGtRVAzKG:{IFjMRU1COjRibX;s[YN2dGW\|	MoPiNlQzPDRyMkO=
NCI-N87	MWnGeY5kfGmxbjDBd5NigQ>?	MWS1NEDPxE1?	M{W4fFQ5KGh?	NF7Z[mRFVVOR	MWnpcoNz\WG\|ZYOg[ZhxemW\|c3nvckBw\iCKTFGtRVAzKG:{IFjMRU1COjRibX;s[YN2dGW\|	NEn3e3EzPDJ2NECyNy=>
NUGC3	NUPSPFhpTnWwY4Tpc44hSXO\|YYm=	M1\5PFUxKM7:TR?=	MmrhOFghcA>?	M3XmdGROW09?	MXPpcoNz\WG\|ZYOg[ZhxemW\|c3nvckBw\iCKTFGtRVAzKG:{IFjMRU1COjRibX;s[YN2dGW\|	NFHLNGozPDJ2NECyNy=>
NUGC2	MULGeY5kfGmxbjDBd5NigQ>?	M{LKVFUxKM7:TR?=	NFPYb3M1QCCq	MknSSG1UVw>?	M{W5eolv[3KnYYPld{BmgHC{ZYPzbY9vKG:oIFjMRU1CODJib4KgTGxCNUF{NDDtc4xm[3WuZYO=	MUmyOFI1PDB{Mx?=
SGC-7901	M4TiVmFxd3C2b4Ppd{BCe3OjeR?=	NEnjN3EzOCEQvF2=	MX6yOEBp		Mn3MbY5pcWKrdIOgR3AudWWmaXH0[YQh[XCxcITvd4l{	NIrDR5MzPDJ2MUO1NS=>
MG-63	Mn3XSpVv[3Srb36gRZN{[Xl?	MVGyNEDPxE1?	NFLq[3UxNjViaB?=		MkjUZoxw[2u\|IITo[UBEUC2rbnT1Z4VlKHCqb4PwbI9zgWyjdHXkJGVNUzFicILveIVqdiCneIDy[ZN{cW:w	NHfhPFEzPDJ\|OU[0NC=>
ARPE-19	NHfEUnpHfW6ldHnvckBCe3OjeR?=	M4fpOFIxKM7:TR?=	MW[wMlUhcA>?		MUPpcohq[mm2czDBdIVtcW5vaX7keYNm\CCyaH;zdIhwenmuYYTpc44hd2ZiRYLrJIFv\CCDa4S=	NFnGPJQzPDJ{N{mxPC=>
CRL-2302	NVztVW9tTnWwY4Tpc44hSXO\|YYm=	MoLDNlAh\|ryP	M3nHT\|AvPSCq		MWHpcohq[mm2czDBdIVtcW5vaX7keYNm\CCyaH;zdIhwenmuYYTpc44hd2ZiRYLrJIFv\CCDa4S=	NGfNSGwzPDJ{N{mxPC=>
MCF-7	MorLSpVv[3Srb36gRZN{[Xl?	Mn7CNlAh\|ryP	MUmxJIg>		MVPhZo9tcXOqZYOg[ZhxemW\|c3nvckBw\iCyaH;zdIhwenmuYYTl[EBGWktiY3:teJJm[XSvZX70JJdqfGhiY3;ubpVo[XSn	M2rD[lI1OjF4Mki5
MCF-7	M2XiXmFxd3C2b4Ppd{BCe3OjeR?=	MWqyNEDPxE1?	M4LFVVEhcA>?		M3vVVYlv[3KnYYPld{Bk[XOyYYPlMVkh\W68eX3lJIFkfGm4aYT5	MXqyOFIyPjJ6OR?=
DLD-1	MVPGeY5kfGmxbjDBd5NigQ>?	NFXlOmEzOMLizszN	MlHJOFghcA>?		NVq5UHRlemWmdXPld{B1cGViQl7JVFMh\XiycnXzd4lwdiCycnWteJJm[XSnZDD3bZRpKDVvYYrhMYRE	NGXJWogzPDJzMUW4NS=>
HT-29	NXTMPHIxTnWwY4Tpc44hSXO\|YYm=	MXiyNOKh\|ryP	NUDCepAxPDhiaB?=		NUnEb2pTemWmdXPld{B1cGViQl7JVFMh\XiycnXzd4lwdiCycnWteJJm[XSnZDD3bZRpKDVvYYrhMYRE	NY\XOnloOjR{MUG1PFE>
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SGC7901	M4XDUmFxd3C2b4Ppd{BCe3OjeR?=	M2r5UlUxyqEQvF2=	MVuyOE81QC95MjDo	MV\EUXNQ	NYTtSnV3cW6mdXPld{BieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDKRWszKHOqUl7B	M{LvNlI1OTd6MkSw
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Caco-2	MWrGeY5kfGmxbjDBd5NigQ>?	MmSyOVDDqM7:TR?=	MVi0PIg>	M13NS2ROW09?	Mnj3[Y5p[W6lZYOgeIhmKG2UTlGgcIV3\Wy\|IH;mxsBUS06QMVGsSnh[TDNuwrDMR3QtyqCOT2isxsBJUUZ\|QT\|CpHpIOTZuwrDQSGU3ScLiYX7kxsBNT0GOU{G2xsBo\W6nc9MgZ48ufHKnYYTl[EB4cXSqIFTlfC=>	MYWyOFE3OTZ7NR?=
HAECs	NHL2c5dHfW6ldHnvckBCe3OjeR?=	MUmxNEDPxE1?	NITOS4kyKGh?		NGruclnDqGG2dHXueYF1\XNiVF7GMe6yNXO2aX31cIF1\WRiSVPBUU0yKGGwZDDWR2FONTFiZYjwdoV{e2mxbh?=	NGrqNWYzPDF\|NE[1Oy=>
Ca9-22	M1fKdGZ2dmO2aX;uJGF{e2G7	M1W0SlMh\|ryP	NITiUW4yKGh?		NXPN[JI3[WKxbHnzbIV{KHSqZTDhZoltcXS7IH;mJGhjWiC2bzDpcoR2[2ViSVytPEBxem:mdXP0bY9v	Mo\qNlQyOjZ3M{K=
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AGS	MlrJSpVv[3Srb36gRZN{[Xl?	MVexNEDPxE4EoB?=	M{e4cVAvPSCq		NIrKbHRqdmirYnn0d{B1cGVidYDy[Yd2dGG2aX;uJI9nKHSqZTDJUE05KGenbnW=	MXKyOFExPjF4Nh?=
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HCT-8	NXLremJJSXCxcITvd4l{KEG\|c3H5	NInl[3gyOMLizszN	M{K4cFI1yqCq		MVzk[YNz\WG\|ZYOgZ4VtdCCjcH;weI9{cXNiaX7keYNm\CCkeTC1MWZW	MmHmNlQxQTV6NkO=
A549	NEHUWWNHfW6ldHnvckBCe3OjeR?=	M3vQVVUxyqEQvF2=	MXuyJIg>		MorPZoxw[2u\|IFXST{BxcG:\|cHjvdplt[XSrb36gcYVlcWG2ZXSgZpkhOSx{LV7R	MUmyOFA3Pzd{Nx?=
HPMC	MnTzSpVv[3Srb36gRZN{[Xl?	M1fzeVExyqEQvF2=	M2H3SVQ5KGh?		NU\PXnoyemW4ZYLz[ZMhfGinIHPoZY5o\XNiaX6gZ4VtdCCvb4LwbI9td2e7IHnu[JVk\WRiYomgTGdRTFN?	NYXyVVRpOjRyNEK4N\|g>
HPMC	M2rMdWFxd3C2b4Ppd{BCe3OjeR?=	NXvDWlVWOTEEoN88US=>	M33JflI1yqCq		MkTLdoV3\XK\|ZYOg[IVkemWjc3WgbY4h[2WubDD2bYFjcWyrdImgbY5lfWOnZDDifUBJT1CGUx?=	MmfUNlQxPDJ6M{i=
MGC803	MnPSRZBweHSxc3nzJGF{e2G7	MVGyNOKh\|ryP	NEe4eFQyKGh?		MWLpcohq[mm2czDhdI9xfG:\|aYOgbY5lfWOnZDDifUBKTk5vzsJCpIFv\CB34pEyMWRHXVJ?	MUKyOFAzPzd3MB?=
SGC7901	M2XROGFxd3C2b4Ppd{BCe3OjeR?=	MojmNlDDqM7:TR?=	NVXVXmJvOSCq		NXH1SnR6cW6qaXLpeJMh[XCxcITvd4l{KGmwZIXj[YQh[nliSV\OMe6yyqCjbnSgOgKBui2GRmXS	NXLsUmFWOjRyMke3OVA>
COLO205	Mk\wRZBweHSxc3nzJGF{e2G7	MUWxNE8zOC92MDFOwG0>	M3\jXlI1KGh?		MmjZbY5lfWOnczDEUmEhdGGmZHXyJIZwem2jdHnvci=>	M1vIOlI1ODF7MUC4
G292	MUfBdI9xfG:\|aYOgRZN{[Xl?	MYizNOKh\|ryP	MmewNkBp		M2jpZZJme3SxcnXzJINieHOjaXPpck1qdmS3Y3XkJINmdGxiZHXheIg>	NInMXmozPDBzMkmzNC=>
BxPC-3	M{j5VGZ2dmO2aX;uJGF{e2G7	MYCxNEDPxE4EoB?=	MWq2JIg>		Ml:wbY5kemWjc3WgcYlTNTF2MzDlfJBz\XO\|aX;u	MlHMNlM6PzN5MUC=
HPAF-II	NIfV[XVHfW6ldHnvckBCe3OjeR?=	NXKxcHNFOTBizszNxsA>	NHnnPHo3KGh?		MYLpcoNz\WG\|ZTDtbXIuOTR\|IHX4dJJme3Orb36=	Mn;vNlM6PzN5MUC=
HL-60	NUTHcoFrSXCxcITvd4l{KEG\|c3H5	NHXRXlA2OMLizszN	NHfh[\|QyKGh?		NGXiRYFz\XOldXXzJGJCOTR3IH3l[IlifGWmIHHwc5B1d3Orcx?=	MUCyN\|k1QDd3MR?=
HepG2	Mm\FSpVv[3Srb36gRZN{[Xl?	NYHlUItHPDBizszN	NIjxNYM3NzF{IHi=		MmrVbY5pcWKrdIOgeIhmKGmwY4LlZZNmKG:oIICtSXJMOSCjbnSgdE1kNUq3bjDwdo91\WmwIHX4dJJme3Orb36gZpkhWEx?	NETaTmkzOzl2Mki1NS=>
HUVECs	MonXSpVv[3Srb36gRZN{[Xl?	MlL3NlUh\|ryP	NV3DOpQ4OSCq		MmL2bY5kemWjc3WgUmYu\|rqEIIC2OUBvfWOuZXHyJJRz[W6\|bH;jZZRqd25?	NEj6emgzOzlyMUCwPC=>
LNCaP	NEi0WGdHfW6ldHnvckBCe3OjeR?=	M3zHeVExKM7:TdMg	NV7nSmsyOSCq		MVHk[YNz\WG\|ZYOgeIhmKEWJRjD1dJJm\3WuYYTl[EBxNVmELUG=	NVrBXI1mOjN6M{izNVg>
HL60	NEnvfmdHfW6ldHnvckBCe3OjeR?=	MWqyNOKh\|ryP	NGXHZZY4OiCq	MWjEUXNQ	MUnpcohq[mm2czDkZZNifGmwaXKtbY5lfWOnZDDDSFEy[iCneIDy[ZN{cW:w	M3HQSlI{QDJ3NUi1
NB4	NX\h[4szTnWwY4Tpc44hSXO\|YYm=	MWWxNEDPxE4EoB?=	M1;OcFczKGh?	MnjsSG1UVw>?	MVPpcohq[mm2czDkZZNifGmwaXKtbY5lfWOnZDDDSFEy[iCneIDy[ZN{cW:w	NHjXcGozOzh{NUW4OS=>
EPOR/CR3	M3fhSmZ2dmO2aX;uJGF{e2G7	MX:1NOKh\|ryP	NHS2WYo{KGh?		MmCzdoVlfWOnczDFVG8h[W6mL3;yJGlNNTNvaX7keYNm\CC2aHWgeJlzd3OrbnWgdIhwe3Cqb4L5cIF1cW:wwrC=	MoPVNlM5OjB5M{G=
HUASMCs	NH21S2JHfW6ldHnvckBCe3OjeR?=	MkHQNVAh\|ryPwrC=	MkLmNlQhcA>?		M4rJRoRqdWmwaYPo[ZMhSW6pIFnJMYNifXOnZDDTU2NUOyCvUl7BJIFv\CCycn;0[YlvKGW6cILld5Nqd28EoB?=	NFXHNnQzOzhzNkS2PC=>
HUASMCs	M3e2RWZ2dmO2aX;uJGF{e2G7	MWWxNEDPxE4EoB?=	M2nLRVI1KGh?		MlTwbY5pcWKrdIOgRY5oKEmLLXnu[JVk\WRiRWLLNU8zKHCqb4PwbI9zgWyjdHnvckBt\X[nbB?=	M1HqNFI{QDF4NE[4
SGC7901	Mni0SpVv[3Srb36gRZN{[Xl?	NXnsR3JvOTBizszNxsA>	NHr6WWczPCCq		NULV[pFycW6qaXLpeJMhfGinIHX4dJJme3Orb36gc4YheGixc4Doc5J6dGG2ZXSgSXJMOS9{	NYGwXFBqOjN5OUK1PFg>
MKN45	NVntOGI2TnWwY4Tpc44hSXO\|YYm=	NV7XTnh2OTBizszNxsA>	NY\pXVFzOjRiaB?=		NVu1S2pVcW6qaXLpeJMhfGinIHX4dJJme3Orb36gc4YheGixc4Doc5J6dGG2ZXSgSXJMOS9{	NUHtU2NOOjN5OUK1PFg>
SGC7901	MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	Mlu5NVAh\|ryPwrC=	NIXSNVYzPC92OD:3NkBp		MUPpcohq[mm2czDj[YxtKGe{b4f0bEBkdy22cnXheIVlKHerdHigSGFRXA>?	NGnHVWczOzd7MkW4PC=>
MKN45	MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NUizc3VwOTBizszNxsA>	NInsdpMzPC92OD:3NkBp		NWG0U3NLcW6qaXLpeJMh[2WubDDndo94fGhiY3:teJJm[XSnZDD3bZRpKESDUGS=	NX\sOVc6OjN5OUK1PFg>
SGC7901	NYnBdnVjSXCxcITvd4l{KEG\|c3H5	NFzpTpMyOCEQvF5CpC=>	MVKyOEBp		Mn\abY5kemWjc3XzJJRp\SCGQWDUMYlv\HWlZXSgZ4VtdCCjcH;weI9{cXN?	M2HJTFI{Pzl{NUi4
MKN45	NYjPWJpQSXCxcITvd4l{KEG\|c3H5	M2HhTVExKM7:TdMg	M4PJPFI1KGh?		NWfLfJd[cW6lcnXhd4V{KHSqZTDERXBVNWmwZIXj[YQh[2WubDDhdI9xfG:\|aYO=	MYCyN\|c6OjV6OB?=
BxPC-3 cells	NGfKcpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M13yTFIxyqEQvF2=	NV;vVY5DOC53IHi=		NGO2e5hqdmirYnn0d{BXTUeILVGtdoVofWyjdHXkJGhWXkWFIHfyc5d1cCCjbnSgeJVj\SCob4LtZZRqd25iaX7keYNm\CCkeTDQRXIuOiCDUB?=	NUKxfHA3OjN5NkSwOFY>
NB4	NVvjclJ7SXCxcITvd4l{KEG\|c3H5	MXuxNE8zOC94MDFOwG0>	MWKxMlUhcA>?	NHTJdWJFVVOR	NH;BSnVl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgZ48ufHKnYYTl[EB4cXSqIGDhZ4xqfGG6ZXy=	M1q1dVI{PzN3NUSx
HepG2	NH\ISVVHfW6ldHnvckBCe3OjeR?=	Ml;ENlDDqM7:TR?=	M4\DTFI1KGh?		MnfwbY5pcWKrdIOgeIhmKEiRLUGgdJJwfGWrbjDlfJBz\XO\|aX;uJINwNXS{ZXH0[YQhf2m2aDDt[ZRnd3KvaX6=	NVew[\|Y1OjN5MEe2NFk>
HUVECs	M3zKS2Fxd3C2b4Ppd{BCe3OjeR?=	NGXr[XYzNzRizszN	M1y2PFI1NzR6IHi=		M4n4Z4lv\HWlZYOgZ4VtdCCmZXH0bC=>	NWnWPWhrOjN5MEe1NlA>
KG-1	MkjWRZBweHSxc3nzJGF{e2G7	MXWyNOKh\|ryP	NXXOenQ2OTJiaB?=		MYPlcohidmOnczDj[YxtKGGyb4D0c5NqeyCrbnT1Z4VlKGK7IGOx	NF;pWYwzOzdyNk[5NS=>
AML 1#	NGXYNnZCeG:ydH;zbZMhSXO\|YYm=	M4nhSVIxyqEQvF2=	MkP3NVIhcA>?		M2m0[YVvcGGwY3XzJINmdGxiYYDvdJRwe2m\|IHnu[JVk\WRiYomgV\|E>	MV6yN\|cxPjZ7MR?=
A2780	MWrGeY5kfGmxbjDBd5NigQ>?	NF;wcJYzOMLizszN	MonhNUBp		MVXicI9kc3NiRGTDSE1qdmS3Y3XkJGRTPSCneIDy[ZN{cW:w	M3\wUVI{Pjl4OE[y

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	c-Jun / α-tubulin / p-ERK / ERK / p-AKT / AKT; PubMed: 17482134 Cancer cell ERK regulates c-Jun levels in melanoma. The indicated melanoma cell lines were treated with 50μM PD98059 (PD) or 10μM LY294002 (LY) for 12h in the absence of serum. Protein samples were analyzed by Western blots using the indicated antibodies. α-Tubulin reveals equal loading. p-JNK / JNK / Cyclin D1 ; PubMed: 17482134 Cancer cell Inhibition of the MEK/ERK pathway affects c-Jun, P-JNK and cyclin D1 levels. The indicated melanoma cell lines were treated with 50μM PD98059 for 16h. Protein samples were analyzed by Western blots using the indicated antibodies. α-Tubulin reveals equal loading. p-HER2 / HER2 ; PubMed: 24244023 J Immunol TE1cells were treated with wortmannin (Akt signal inhibitor), PD98059 (MAPK signal inhibitor), or lapatinib (EGFR and HER2 dual inhibitor) at the indicated doses or with DMSO as a negative control for 48 h. HER2-related signaling molecules were assessed by Western blot. MMP9 / XIAP / VEGF ; PubMed: 29695559 In Vivo SK-Hep1 cells were treated 10 μM PD98059 for 48 h. Protein levels of MMP-9, XIAP, VEGF, cyclin-D1, and pERK were evaluated with western blotting assay.	17482134 24244023 29695559

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]

Protocol

Kinase Assay: ^[1]	- Collapse In vitro MEK-inhibitory activity: 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.
Cell Research: ^[1]	- Collapse Cell lines: K-Balb, KNRK, v-raf-3Y1, SRA/3Y1, EGFR/3T3, and K562 Concentrations: Dissolved in DMSO, final concentrations ~100 μM Incubation Time: 3 dyas, or 7-10 days Method: 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. (Only for Reference)
Animal Research: ^[7]	- Collapse Animal Models: Male Sprague–Dawley rats with acute pancreatitis Formulation: Dissolved in DMSO, and diluted in saline Dosages: 10 mg/kg Administration: Injection i.v. (Only for Reference)

References

- Collapse

Solubility (25°C)

In vitro	DMSO	14 mg/mL warmed (52.37 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 4% DMSO+30% PEG 300+5% Tween 80+ddH2O For best results, use promptly after mixing.	1mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download PD98059 SDF

Molecular Weight	267.28
Formula	C₁₆H₁₃NO₃
CAS No.	167869-21-8
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	N/A

Bio Calculators

Molarity Calculator

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Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

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The Serial Dilution Calculator Equation

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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):

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Frequently Asked Questions

Question 1:
How to formulate this inhibitor for i.p. injection?
Answer:
You can prepare the stock by the vehicle 30% PEG400/0.5% Tween80/5% Propylene glycol, 0.5% CMC.

MEK Signaling Pathway Map

MEK Inhibitors with Unique Features

Pan MEK Inhibitor

U0126-EtOH : MEK1, IC50=0.07 μM; MEK2, IC50=0.06 μM.
Most Potent MEK Inhibitor

PD0325901 : MEK, IC50=0.33 nM.
FDA-approved MEK Inhibitor

Trametinib (GSK1120212) : Approved by FDA for BRAF V600E mutated metastatic melanoma.
Newest MEK Inhibitor

Binimetinib (MEK162, ARRY-162, ARRY-438162) : Potent inhibitor of MEK1/2 with IC50 of 12 nM.

Related MEK Products

Cobimetinib (GDC-0973, RG7420) ^New

Cobimetinib (GDC-0973, RG7420) is a potent and highly selective MEK1 inhibitor with IC50 of 4.2 nM, showing more than 100-fold selectively for MEK1 over MEK2 and showed no significant inhibition when tested against a panel of more than 100 of serine-threonine and tyrosine kinases. Phase 3.
BI-847325 ^New

BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively. Phase 1.
GDC-0623 ^New

GDC-0623 is a potent and ATP-uncompetitive MEK1 inhibitor with K_i of 0.13 nM. Phase 1.
Trametinib (GSK1120212)

Trametinib (GSK1120212) is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM in cell-free assays, no inhibition of the kinase activities of c-Raf, B-Raf, ERK1/2.

Features:More potent than PD0325901 or AZD6244.
PD0325901(Mirdametinib)

PD0325901 is a selective and non ATP-competitive MEK inhibitor with IC50 of 0.33 nM in cell-free assays, roughly 500-fold more potent than CI-1040 on phosphorylation of ERK1 and ERK2. Phase 2.
Selumetinib (AZD6244)

Selumetinib (AZD6244) is a potent, highly selective MEK inhibitor with IC50 of 14 nM for MEK1 and Kd value of 530 nM for MEK2. It also inhibits ERK1/2 phosphorylation with IC50 of 10 nM, no inhibition to p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf, etc. Phase 3.

Features:First MEK inhibitor being tested in Phase II clinical trials.
U0126-EtOH

U0126-EtOH is a highly selective inhibitor of MEK1/2 with IC50 of 0.07 μM/0.06 μM in cell-free assays, 100-fold higher affinity for ΔN3-S218E/S222D MEK than PD98059.

Features:A chemically synthesized and highly selective inhibitor of both MEK1 and MEK2.
PD184352 (CI-1040)

PD184352 (CI-1040) is an ATP non-competitive MEK1/2 inhibitor with IC50 of 17 nM in cell-based assays, 100-fold more selective for MEK1/2 than MEK5. Phase 2.

Features:First MEK inhibitor to begin clinical development.
Binimetinib (MEK162, ARRY-162, ARRY-438162)

Binimetinib (MEK162, ARRY-162, ARRY-438162) is a potent inhibitor of MEK1/2 with IC50 of 12 nM in a cell-free assay. Phase 3.
Refametinib (RDEA119, Bay 86-9766)

Refametinib (RDEA119, Bay 86-9766) is a potent, ATP non-competitive and highly selective inhibitor of MEK1 and MEK2 with IC50 of 19 nM and 47 nM, respectively.

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PD98059

Cited by 190 Publications

Purity & Quality Control

Choose Selective MEK Inhibitors

Biological Activity

Protocol

References

Solubility (25°C)

Chemical Information Download PD98059 SDF

Bio Calculators

Molarity Calculator

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

Dilution Calculator

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

The Serial Dilution Calculator Equation

Serial Dilutions

Computed Result

Molecular Weight Calculator

Total Molecular Weight: g/mol

Instructions to calculate molar mass (molecular weight) of a chemical compound:

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molarity Calculator

Tech Support

Frequently Asked Questions

MEK Signaling Pathway Map

MEK Inhibitors with Unique Features

Related MEK Products

Choose Your Country or Region

By Signaling Pathways

By product type

PD98059

Cited by 190 Publications

Purity & Quality Control

Choose Selective MEK Inhibitors

Biological Activity

Protocol

References

Solubility (25°C)

Chemical Information Download PD98059 SDF

Bio Calculators

Molarity Calculator

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

Dilution Calculator

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

The Serial Dilution Calculator Equation

Serial Dilutions

Computed Result

Molecular Weight Calculator

Total Molecular Weight: g/mol

Instructions to calculate molar mass (molecular weight) of a chemical compound:

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molarity Calculator

Tech Support

Frequently Asked Questions

MEK Signaling Pathway Map

MEK Inhibitors with Unique Features

Related MEK Products

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)