PD98059

Catalog No.S1177

PD98059 Chemical Structure

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.

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Cited by 190 Publications

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?=
TE3 MknBSpVv[3Srb36gRZN{[Xl? M2DZRVUxKM7:TR?= NWrOPJc3PDhiaB?= NGXCZldFVVOR NXTsXHBlfXC{ZXf1cIF1\XNidHjlJIV5eHKnc4Ppc44hd2ZiSFzBJINt[XO|IFm= NWnpc3gyOjR{NESwNlM>
TE4 NG\qUFZHfW6ldHnvckBCe3OjeR?= NHvK[VM2OCEQvF2= MonUOFghcA>? NX7jVGVZTE2VTx?= M1u0UZVxemWpdXzheIV{KHSqZTDlfJBz\XO|aX;uJI9nKEiOQTDjcIF{eyCL MnnBNlQzPDRyMkO=
TE5 MkPMSpVv[3Srb36gRZN{[Xl? Mlu4OVAh|ryP M3PBdlQ5KGh? NGHhXppFVVOR MXX1dJJm\3WuYYTld{B1cGViZYjwdoV{e2mxbjDv[kBJVEFiY3zhd5MhUQ>? MV[yOFI1PDB{Mx?=
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=
OE19 NVW5co45TnWwY4Tpc44hSXO|YYm= Ml\UOVAh|ryP MVW0PEBp MXLEUXNQ NV;6dFE{cW6lcnXhd4V{KGW6cILld5Nqd25ib3[gTGxCNUFyMjDvdkBJVEFvQUK0JI1wdGWldXzldy=> NWrEVItQOjR{NESwNlM>
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>
7402 NWO2[5pqSXCxcITvd4l{KEG|c3H5 M2Gx[|MxKM7:TR?= MnvYOUBl NWnBdZdO\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdg>? M{TMNlI1OjFzMkWz
7721 NGLwcXhCeG:ydH;zbZMhSXO|YYm= Mki3N|Ah|ryP MWS1JIQ> NHHQTpVl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9v MWiyOFIyOTJ3Mx?=
SGC7901  M4XDUmFxd3C2b4Ppd{BCe3OjeR?= M2r5UlUxyqEQvF2= MVuyOE81QC95MjDo MV\EUXNQ NYTtSnV3cW6mdXPld{BieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDKRWszKHOqUl7B M{LvNlI1OTd6MkSw
SMMC7721 NGjpNoxHfW6ldHnvckBCe3OjeR?= M4LNbVI2NzVyIN88US=> M1v5[FI1KGh? NVTzUZZKe3WycILld5NmeyC2aHWg[ZhxemW|c3nvckBw\iCyLVHreEBweiCyLVXST|EwOsLi MUeyOFE3QDB3Nh?=
MCF-7 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fhRlExKM7:TR?= NIfkcVg1QGh? M2CzdWROW09? MVjy[ZZmenOnczDCUmYucW6mdXPl[EBk\WyuIHP5Z4xmKGG{cnXzeC=> NHrOTIQzPDF4M{SwOC=>
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=
Ca9-22 M2K3VmZ2dmO2aX;uJGF{e2G7 NETEdXA{KM7:TR?= MV:xM|IhcA>? MUHy[YR2[2W|IFjiVk1qdmS3Y3XkJGFVTi1{IIDoc5NxcG:{eXzheIlwdg>? M1vOOFI1OTJ4NUOy
AGS MlrJSpVv[3Srb36gRZN{[Xl? MVexNEDPxE4EoB?= M{e4cVAvPSCq NIrKbHRqdmirYnn0d{B1cGVidYDy[Yd2dGG2aX;uJI9nKHSqZTDJUE05KGenbnW= MXKyOFExPjF4Nh?=
Caco-2  NV7YWIU2SXCxcITvd4l{KEG|c3H5 NVTL[IhrOTEEoN88US=> NIflRWQzPMLiaB?= M2TD[IRm[3KnYYPld{Bk\WyuIHHwc5B1d3OrczDpcoR2[2WmIHL5JFUuTlV? NUHRPWpCOjRyOUW4OlM>
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     


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     


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     


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     


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]

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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]

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  • 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]

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  • 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)

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

Molecular Weight 267.28
Formula

C16H13NO3

CAS No. 167869-21-8
Storage powder
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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

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*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).

Dilution Calculator

Dilution Calculator

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)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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

The Serial Dilution Calculator Equation

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  • Computed Result

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    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
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Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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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.

  • * Indicates a Required Field

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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID