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 147 Publications

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Nature, 2016, 10.1038/nature19347

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Molecules, 2019, 24(6)

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Environ Toxicol, 2019, 34(6):679-688

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Biochim Biophys Acta Mol Cell Res, 2018, 1865(1):57-66

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J Virol, 2018, 92(8)

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Inflammopharmacology, 2018, 10.1007/s10787-018-0492-y

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Biomed Pharmacother, 2018, 105:320-325

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J Cell Biochem, 2018, 119(1):300-313

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In Vivo, 2018, 32(3):549-554

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Cancer Lett, 2017, 395:31-44

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Cell Physiol Biochem, 2017, 41(5):1957-1969

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Chem Biol Interact, 2017, 270:1-8

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Am J Transl Res, 2017, 9(6):2878-2890

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Evid Based Complement Alternat Med, 2017, 2017:5985703

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Clin Cancer Res, 2016, 10.1158/1078-0432.CCR-15-2242

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Cytokine, 2015, 17:139-144

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Tissue Cell, 2015, 47(3):301-10

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Growth Factors, 2015, 33(5-6):356-65

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Genet Mol Res, 2015, 14(4):18325-33

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Cell Death Dis, 2014, 5:e1187

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FASEB J, 2014, 10.1096/fj.13-247924

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Mol Cancer Ther, 2014, 13(4):926-37

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Carcinogenesis, 2014, 35(4):795-806

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Oncol Rep, 2014, 32(6):2777-88

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J Periodontal Res, 2014, 10.1111/jre.12193

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Biochem Biophys Res Commun, 2014, 446(1):167-72

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J Cardiovasc Pharmacol, 2014, 64(2):180-90

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Evid Based Complement Alternat Med, 2014, Zhang JL

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Regul Pept, 2014, 194-195:41-8

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Hepatology, 2013, 59(4):1262-72

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Mol Cancer Ther, 2013, 13(1):37-48

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J Thromb Haemost, 2013, 12(3):395-408

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Genetic Syndromes & Gene Therapy, 2013, 4:6

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J Biomol Screen, 2012, 17(6):813-21

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Microbiol Immunol, 2012, 56(11):782-8

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Sci Signal, 2011, 4(192):ra62

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Atheroscler, 2011, 218(2):486-92

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Int J Mol Med, 2011, 28(1):115-9

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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	NUjkd5RPTnWwY4Tpc44hSXO\|YYm=	MnO0NlUh\|ryP	Mm\WNUBp		MnvXZox2dnS\|IITo[UBDY2GfUD3pcoR2[2WmIHnuZ5Jm[XOnIHnuJJBpd3OyaH:tR4hsOSCjbnSgdIhwe3Cqbz3FVmsh\XiycnXzd4lwdg>?	NID3RmozPTd4OUG4NS=>
MCF-7	M4rC[mZ2dmO2aX;uJGF{e2G7	M1jyUFExKM7:TR?=	MYixJIg>		NGHzT41qdmirYnn0d{BKVC1zOD3lcohidmOnZDDj[YxtKG2rZ4LheIlwdg>?	NXnqPG85OjV5MkewNVE>
HepG2	MYrGeY5kfGmxbjDBd5NigQ>?	NYLie3I6OTBizszN	MXW1JIg>		MVvicI9kc3NicHjvd5Bpd3K7bHH0[YQhVUGSS4OgbY5lfWOnZDDifUBmgG:pZX7veZMhXEeILd8yNS=>	Mn3sNlU2PjB2OEi=
HepG2	MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NV\5UGw4OjBizszN	NW\ZZm1nOjRiaB?=		NXfnSYJYe3WycILld5NmeyCWR1[t{tIyNWmwZIXj[YQh[2WubDDwdo9tcW[ncnH0bY9vKGGwZDDpcpZie2mxbh?=	MXyyOVU3ODR6OB?=
MDA-MB-231	MV7GeY5kfGmxbjDBd5NigQ>?	NWXlUlN7OjVizszN	MXeyMVMhcA>?		MXrk[YNz\WG\|ZYOgdE1GWktzL{KgZY5lKFNzMEDBOEBmgHC{ZYPzbY9v	MYqyOVU2PTh5NR?=
SW480	MV7GeY5kfGmxbjDBd5NigQ>?	MV:yNOKh\|ryP	MmPJNeKhcA>?		MXLy[YR2[2W\|IITo[UBmgHC{ZYPzbY9vKG:oIFHUSlMheHKxdHXpci=>	MlLXNlU1PDd6MU[=
HCT-15	MYrGeY5kfGmxbjDBd5NigQ>?		M{OzfFEhcA>?		MlzJZZR1\W63YYTld{BRT0V{LXnu[JVk\WRicHjvd5Bpd3K7bHH0bY9vKG:oIFXyb:Kh	MXWyOVQ{OTR{NR?=
HCT-15	NHHoWlNCeG:ydH;zbZMhSXO\|YYm=		MlfRNUBp		NFqyUXVi[m:uaYPo[ZMhfGinIIDyc5Rm[3SrdnWg[YZn\WO2czDv[kBRT0V{wrDh[4FqdnO2IHP1doN2dWmwLXnu[JVk\WRiYYDvdJRwe2m\|	NWLzU3hSOjV2M{G0NlU>
786-O	NXjpVHUzSXCxcITvd4l{KEG\|c3H5	M1TIXFUxyqEQvF2=	NYjO[HZlOjRiaB?=		M13KSZBwfGWwdHnheIV{yqC2aHWgdJJwNWGyb4D0c5Rq[yCnZn\lZ5R{KG:oIF7D	M3zOXVI1PTB6NEe2
A498	NYf0eYpvSXCxcITvd4l{KEG\|c3H5	M3nW[lUxyqEQvF2=	MkPyNlQhcA>?		NYToRopkeG:2ZX70bYF1\XQEoITo[UBxem9vYYDvdJRwfGmlIHXm[oVkfHNib3[gUmM>	NGewdGEzPDVyOES3Oi=>
NHBE	M1fa[GZ2dmO2aX;uJGF{e2G7	NFPNZ4czNzJyIN88US=>	NELPR4UzKGh?		MUjheJRmdnWjdHXzJGlNNTN\|IIP0bY12dGG2ZXSgR3hEVDhxSVytPEB{\WO{ZYTpc44>	MkTCNlQ1Pzl3Mk[=
A375	MWTD[YxtKEmwdnHzbY9vKEG\|c3H5	MlHxNVDjiJN{MDFCuW0>	NHzab4IzPCCq		NHW0S2Nz\WS3Y3XzJI1mdGGwb33hJINmdGxiaX72ZZNqd25?	NUe4WnZYOjR2Nk[wN\|Y>
HBMEC	NXPPfYtITnWwY4Tpc44hSXO\|YYm=	Mlr5NVAh\|ryP	MoO0NUBp		NGfITm5jdG:la4OgWmVITi2rbnT1Z4VlKEWyaFGyJIV5eHKnc4Ppc44>	NFjuO20zPDR3OEm4Ni=>
HPAEpiCs	MV3GeY5kfGmxbjDBd5NigQ>?	NHfFXpQ{OCEQvF2=	NGrZRYcyKGh?		M13GRolvcGmkaYTzJHRPTi4QsTDzeIlufWyjdHXkJJA1Oi:yNESgUWFRUyCyaH;zdIhwenmuYYTpc44>	NVnyPHZzOjR2NEG4O\|A>
BeWo	NYXxbJZmTnWwY4Tpc44hSXO\|YYm=	Mo\uNVDDqM7:TR?=	NEHLcHYzKGh?		MXXpcohq[mm2czDFVmsyNzJ?	NX\PZVNUOjR2M{O4OFY>
PC3	MULBdI9xfG:\|aYOgRZN{[Xl?	M2niOVUxKM7:TR?=	NX3WN3B7OC53IHi=		MnnpbY5pcWKrdIOgUWh[NTR2OT3pcoR2[2WmIHHwc5B1d3Orc9Mg	NETOUJAzPDR{NEi4PS=>
HGC-27	M3rnZ2Fxd3C2b4Ppd{BCe3OjeR?=	NUfzcGM3OSEEtV2=	NIHsNGUyKGh?		MUjzeZBxemW\|c3XzJHJCTDByMTDwcJV{KE2NLUKyNFYucW6mdXPl[EBk\WyuII\pZYJqdGm2eTDsc5N{	MknxNlQ1OTZ\|NEm=
MCF-7	M3rhXmZ2dmO2aX;uJGF{e2G7	Moj1NVDDqM7:TR?=	MkHuNVAwOzBibXnu		M{W2NpJm\HWlZYOgeIhmKFWWUD3k[ZBmdmSnboSgSXJMKHCqb4PwbI9zgWyjdHnvci=>	M1X5VVI1OzlyOEG5
HUVECs	MV3GeY5kfGmxbjDBd5NigQ>?	M{Hxe\|ExyqEQvF2=	Ml7wNUBp		NGrqfmJqdmirYnn0d{B1cGViSFTMJJJm\HWlZXSgR29ZNTJiZYjwdoV{e2mxbjDhcoQhWEeLLUKgdoVt\WG\|ZR?=	M1fWTFI1Ozh3MUC5
HeLa	NIDYc\|FHfW6ldHnvckBCe3OjeR?=	M3P5NVUxKM7:TR?=	MWiwMlUhcA>?		MXHicI9kc3NiVGLYMVEhdnWlbHXhdkBucWe{YYTpc44h[W6mIGTYUmlRKGSxd36tdoVofWyjdHnvci=>	NXjPPWFSOjR\|N{[4Nlc>
HL-60	MljVSpVv[3Srb36gRZN{[Xl?	MWSxNE8zOCEQvF2=	NGfuc5cyKGh?		NH3rSplqdmirYnn0d{B1cGYEoF6uJINpcW6nboPpd4V5fHKjY4VCpIlv\HWlZXSg[Iln\mW{ZX70bYF1cW:wIHnueI8h\3KjboXsc4N6fGW\|	NWXzb4dFOjR\|NUewNlA>
HL-60	MkHhSpVv[3Srb36gRZN{[Xl?	MorPNkDDvU1?	MV6xOkBp	MVfEUXNQ	NUi4N493cW6qaXLpeJMhfGinIHHzd49kcWG2aX;uJI9nKHCVNkKxJHJi\i1zIHHu[EBPTkGWY{OsJIFv\CC2aHWgVmEucW6mdXPl[EBxcG:\|cHjvdplt[XSrb36gc4YhdnWlbHXhdkBPTkGWY{O=	NHTPdo4zPDN\|MEC2PC=>
HEK 293	NEXublZHfW6ldHnvckBCe3OjeR?=	MXGxNEDPxE1?	M1TwWVUhcA>?	MmfMSG1UVw>?	MmnFbY5pcWKrdIOgW451NWmwZIXj[YQh\|rJvY3H0[Y5qdi:WQ1[0JIFkfGm4aYT5JIFv\CCwdXPs[YFzKM7{LXPheIVvcW5iYXPjeY12dGG2aX;u	NX3oe4JDOjR\|MkSzOlY>
HEK 293	MkXESpVv[3Srb36gRZN{[Xl?	M3\TS\|ExKM7:TR?=	NV7N[I9JPSCq	NXfqVFdyTE2VTx?=	MYDzeZBxemW\|c3XzJJRp\SCFUmSgZYN1cX[rdIm=	NV3SUXoxOjR\|MkSzOlY>
SW480	MVvGeY5kfGmxbjDBd5NigQ>?	MmCxNVAh\|ryP	Moe5NlAhcA>?	Mk\wSG1UVw>?	MYTzeZBxemW\|c3XzJJRp\SCFUmSgZYN1cX[rdIm=	NVXEXlhvOjR\|MkSzOlY>
HCSMCs	MlHaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NV\ieIhbOTBizszN	NInSOYYzPCCq		NYm4N3RF[myxY3vzJGZCSlB2LXnu[JVk\WRiSFPBV21EKHC{b3zp[oVz[XSrb36=	MmHWNlQ{OTJ\|OEG=
PANC-1	NIfwTI9HfW6ldHnvckBCe3OjeR?=	MVyyNEDPxE1?	NV6zOnY2PDhiaB?=		M2Th[YlvcGmkaYTzJJRp\SCneIDy[ZN{cW:wIH;mJO6VPkRiaX6gdoV{eG:wc3WgeI8hfGinIGDQRXLPvMLiYXfvcol{fMLi	NGrybXUzPDJ7NEGzNy=>
A549	NFfoWphHfW6ldHnvckBCe3OjeR?=	M2PZO\|MxKM7:TR?=	MYiwMlUhcA>?	NV7UNZNDTE2VTx?=	Mnq4bY5pcWKrdIOgeIhmKHSqcn;tZolvNWmwZIXj[YQhUUxvOD;DXGNNQC2OdXOgZYN1cX[rdIm=	M4[1cFI1Ojd5Nkm2
A549	M{TqSWZ2dmO2aX;uJGF{e2G7	MX6zNEDPxE1?	M4\QTFAvPSCq	M{\UUmROW09?	NY\sRZFIcW6qaXLpeJMhfGi{b33ibY4ucW6mdXPl[EBEN0WEUN8yJHRpejJ\|NdMgdIhwe3Cqb4L5cIF1cW:w	M{mzfFI1Ojd5Nkm2
MC-3	MlXpRZBweHSxc3nzJGF{e2G7	MXWxNEDPxE1?	MlnENlQhcA>?		MYnwc5RmdnSrYYTl[EBOTVOFLXnu[JVk\WRiYYDvdJRwe2m\|IHnuJEBk\Wyucx?=	MUmyOFI4ODV{Mx?=
Raji	MV\GeY5kfGmxbjDBd5NigQ>?	MoHRNVAh\|ryP	NUDQRYRVOSCq		NUHT[XlG[myxY3vzJIh{SkGIRjDpcoR2[2WmIFXyb\|EwOiCyaH;zdIhwenmuYYTpc44>	NGG2OYwzPDJ4OU[zNC=>
Raji	NHiyUlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	Mlj4NVAh\|ryP	NUWybpdyOSCq		M2e4XIlvcGmkaYTzJJRp\SCkYYPhcEBweiCqc1LBSmYue3SrbYXsZZRm\CClZXzsJJBzd2yrZnXyZZRqd25iYX7kJJZq[WKrbHn0fS=>	MoDnNlQzPjl4M{C=
HT29	NYPNO4JITnWwY4Tpc44hSXO\|YYm=	MmDSNVAh\|ryP	M37vNFIhcA>?		MWPpcohq[mm2czDv[kBLSUt{LDDFVmsyNzJiYX7kJHNVSVR\|IIDoc5NxcG:{eXzheIlwdg>?	NVG0dpd{OjR{NkWyPVM>
HepG2	M17kXmFxd3C2b4Ppd{BCe3OjeR?=	MlnXNlAh\|ryP	M3r0blI1KGh?		Ml7tbY5pcWKrdIOgSXJMOS9{IIDoc5NxcG:{eXzheIlwdiCjbnSg[Y5p[W6lZYOgWmIyNWmwZIXj[YQh[XCxcITvd4l{	NUfK[GRDOjR{NEe5NFk>
HepG2	NVv6XmtQTnWwY4Tpc44hSXO\|YYm=	NV7wPVVbOjBizszN	NIPSXY8zKGh?		M1rqNIVvcGGwY3XzJHZDOS2rbnT1Z4VlKE[RWF:zZUB1emGwc3PybZB1cW:wYXygZYN1cX[rdIm=	MXWyOFI1PzlyOR?=
TE4	M1;kOmZ2dmO2aX;uJGF{e2G7	NHPYd2gzOC93MD:xNFAh\|ryP	M4PKbFQ5KGh?	NVXUSlQ3TE2VTx?=	M1zZVolvcGmkaYTzJJAuTXKtIHHu[EB4d3K2bXHucolvKGSxd37y[Yd2dGG2ZXSgdE1Cc3RiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ?	M17VNlI1OjR2MEKz
TE1	NF65[ZZHfW6ldHnvckBCe3OjeR?=	NYfNR2lwOjBxNUCvNVAxKM7:TR?=	MlLXOFghcA>?	NImwWYpFVVOR	M4XWT4lvcGmkaYTzJJAuTXKtIHHu[EB4d3K2bXHucolvKGSxd37y[Yd2dGG2ZXSgdE1Cc3RiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ?	M{i5T\|I1OjR2MEKz
KYSE30	MVTGeY5kfGmxbjDBd5NigQ>?	M2fHPFIxNzVyL{GwNEDPxE1?	Ml[wOFghcA>?	MoniSG1UVw>?	NGXKO5JqdmirYnn0d{BxNUW{azDhcoQhf2:{dH3hco5qdiCmb4fudoVofWyjdHXkJJAuSWu2IHnuJIEh\G:\|ZT3k[ZBmdmSnboSgcYFvdmW{	MYeyOFI1PDB{Mx?=
TE1	NGq3SIdHfW6ldHnvckBCe3OjeR?=	NEjSVlY2OCEQvF2=	MmrrOFghcA>?	M2G4UGROW09?	M4rQ[JVxemWpdXzheIV{KHSqZTDlfJBz\XO\|aX;uJI9nKEiOQTDjcIF{eyCL	MX:yOFI1PDB{Mx?=
TE3	NWPhZmk4TnWwY4Tpc44hSXO\|YYm=	NETSRnE2OCEQvF2=	MYq0PEBp	MkG5SG1UVw>?	MkHseZBz\We3bHH0[ZMhfGinIHX4dJJme3Orb36gc4YhUEyDIHPsZZN{KEl?	MkHhNlQzPDRyMkO=
TE4	MofrSpVv[3Srb36gRZN{[Xl?	MYS1NEDPxE1?	MnHJOFghcA>?	NHe4UGxFVVOR	MnHleZBz\We3bHH0[ZMhfGinIHX4dJJme3Orb36gc4YhUEyDIHPsZZN{KEl?	M2S2XFI1OjR2MEKz
TE5	NFXOS2ZHfW6ldHnvckBCe3OjeR?=	NIHFdY02OCEQvF2=	NUXFNnhuPDhiaB?=	NFSybGpFVVOR	NUC2ellxfXC{ZXf1cIF1\XNidHjlJIV5eHKnc4Ppc44hd2ZiSFzBJINt[XO\|IFm=	NYXSZYVvOjR{NESwNlM>
KYSE30	MX\GeY5kfGmxbjDBd5NigQ>?	M1LHTVUxKM7:TR?=	MYe0PEBp	MXLEUXNQ	MoLDeZBz\We3bHH0[ZMhfGinIHX4dJJme3Orb36gc4YhUEyDIHPsZZN{KEl?	MUSyOFI1PDB{Mx?=
MKN7	MVrGeY5kfGmxbjDBd5NigQ>?	MmroOVAh\|ryP	MojOOFghcA>?	MUjEUXNQ	MV\pcoNz\WG\|ZYOg[ZhxemW\|c3nvckBw\iCKTFGtRVAzKG:{IFjMRU1COjRibX;s[YN2dGW\|	M1P5cVI1OjR2MEKz
OE19	NHHp[HZHfW6ldHnvckBCe3OjeR?=	MlvWOVAh\|ryP	M3XqW\|Q5KGh?	M2GzSmROW09?	NUTJdo41cW6lcnXhd4V{KGW6cILld5Nqd25ib3[gTGxCNUFyMjDvdkBJVEFvQUK0JI1wdGWldXzldy=>	MWCyOFI1PDB{Mx?=
KATOIII	NVSwUVFITnWwY4Tpc44hSXO\|YYm=	NFPKWpE2OCEQvF2=	MV60PEBp	MlTiSG1UVw>?	M3zkbIlv[3KnYYPld{BmgHC{ZYPzbY9vKG:oIFjMRU1CODJib4KgTGxCNUF{NDDtc4xm[3WuZYO=	M3[1cVI1OjR2MEKz
NCI-N87	M2HNXmZ2dmO2aX;uJGF{e2G7	MU[1NEDPxE1?	NWO0SnJ1PDhiaB?=	NXfLV49VTE2VTx?=	NVPHS285cW6lcnXhd4V{KGW6cILld5Nqd25ib3[gTGxCNUFyMjDvdkBJVEFvQUK0JI1wdGWldXzldy=>	NFzIZoszPDJ2NECyNy=>
NUGC3	MoPVSpVv[3Srb36gRZN{[Xl?	MVO1NEDPxE1?	Mlv4OFghcA>?	M1XpNGROW09?	MWXpcoNz\WG\|ZYOg[ZhxemW\|c3nvckBw\iCKTFGtRVAzKG:{IFjMRU1COjRibX;s[YN2dGW\|	MmXNNlQzPDRyMkO=
NUGC2	NULSR2RiTnWwY4Tpc44hSXO\|YYm=	MmPrOVAh\|ryP	NH72ems1QCCq	MojxSG1UVw>?	MoXtbY5kemWjc3XzJIV5eHKnc4Ppc44hd2ZiSFzBMWExOiCxcjDIUGEuSTJ2IH3vcIVkfWyncx?=	MWGyOFI1PDB{Mx?=
SGC-7901	MmGzRZBweHSxc3nzJGF{e2G7	MXqyNEDPxE1?	Ml\UNlQhcA>?		M2LJSYlvcGmkaYTzJGNRNW2nZHnheIVlKGGyb4D0c5Nqew>?	NHHtXnUzPDJ2MUO1NS=>
MG-63	NGS1Z3ZHfW6ldHnvckBCe3OjeR?=	MVmyNEDPxE1?	NEjVO4UxNjViaB?=		MULicI9kc3NidHjlJGNJNWmwZIXj[YQheGixc4Doc5J6dGG2ZXSgSWxMOSCycn;0[YlvKGW6cILld5Nqd25?	NFTleVMzPDJ\|OU[0NC=>
ARPE-19	NXjhW4d2TnWwY4Tpc44hSXO\|YYm=	MYqyNEDPxE1?	NVvk[nA5OC53IHi=		M{TRdolvcGmkaYTzJGFx\Wyrbj3pcoR2[2WmIIDoc5NxcG:{eXzheIlwdiCxZjDFdosh[W6mIFHreC=>	MlW2NlQzOjd7MUi=
CRL-2302	NXrVd20zTnWwY4Tpc44hSXO\|YYm=	MlrpNlAh\|ryP	MY[wMlUhcA>?		NEn1Z2NqdmirYnn0d{BCeGWuaX6tbY5lfWOnZDDwbI9{eGixconsZZRqd25ib3[gSZJsKGGwZDDBb5Q>	NUnY[ZRwOjR{Mke5NVg>
MCF-7	M4LnNWZ2dmO2aX;uJGF{e2G7	MmjnNlAh\|ryP	NXjqbJRpOSCq		M2DRT4Fjd2yrc3jld{BmgHC{ZYPzbY9vKG:oIIDoc5NxcG:{eXzheIVlKEWUSzDjc{11emWjdH3lcpQhf2m2aDDjc45rfWejdHW=	M3fZclI1OjF4Mki5
MCF-7	MkfERZBweHSxc3nzJGF{e2G7	M1;iPVIxKM7:TR?=	M2f1UlEhcA>?		NH3hNoVqdmO{ZXHz[ZMh[2G\|cHHz[U06KGWweont[UBi[3Srdnn0fS=>	MkTENlQzOTZ{OEm=
DLD-1	M2L3dmZ2dmO2aX;uJGF{e2G7	NVfHZlNROjEEoN88US=>	NFHiZZI1QCCq		NHLpUJRz\WS3Y3XzJJRp\SCETlnQN{BmgHC{ZYPzbY9vKHC{ZT30doVifGWmIIfpeIghPS2jenGt[GM>	Mn62NlQzOTF3OEG=
HT-29	NXrEb5J6TnWwY4Tpc44hSXO\|YYm=	MmHSNlDDqM7:TR?=	MX:0PEBp		NWTQOVN2emWmdXPld{B1cGViQl7JVFMh\XiycnXzd4lwdiCycnWteJJm[XSnZDD3bZRpKDVvYYrhMYRE	M{\ifFI1OjFzNUix
7402	MVHBdI9xfG:\|aYOgRZN{[Xl?	M4LTS\|MxKM7:TR?=	MoXzOUBl		NYf6RVBx\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdg>?	NXvtb\|I3OjR{MUGyOVM>
7721	NX;FPJo6SXCxcITvd4l{KEG\|c3H5	M2XJN\|MxKM7:TR?=	MmrNOUBl		M4PVOYRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44>	NH\PclEzPDJzMUK1Ny=>
SGC7901	NWHmNoJISXCxcITvd4l{KEG\|c3H5	M{D6XFUxyqEQvF2=	NXewRWJSOjRxNEivO\|IhcA>?	NEL4OVVFVVOR	NGLWOnFqdmS3Y3XzJIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIFrBT\|Ihe2iUTlG=	MWiyOFE4QDJ2MB?=
SMMC7721	MXXGeY5kfGmxbjDBd5NigQ>?	NIT1foYzPS93MDFOwG0>	MXSyOEBp		M1HkRZN2eHC{ZYPz[ZMhfGinIHX4dJJme3Orb36gc4YheC2Da4Sgc5IheC2HUluxM\|LDqA>?	MW[yOFE3QDB3Nh?=
MCF-7	NYPIXIl4T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NV;IZVNyOTBizszN	MmjzOFhp	NED6UoJFVVOR	Mn32doV3\XK\|ZYOgRm5HNWmwZIXj[YQh[2WubDDjfYNt\SCjcoLld5Q>	MXKyOFE3OzRyNB?=
Caco-2	MnfKSpVv[3Srb36gRZN{[Xl?	MlrrOVDDqM7:TR?=	M{HMclQ5cA>?	MWTEUXNQ	NHiwbFhmdmijbnPld{B1cGVibWLORUBt\X[nbIOgc4bDqFOFTl6xRUxHYFmGMz\|CpGxEXC{EoFzPXEzDqEiLRkPBMOKhYkdzNj\|CpHBFTT[DwrDhcoTDqEyJQVzTNVbDqGenbnXzxsBkdy22cnXheIVlKHerdHigSIV5	NXz1N4NYOjRzNkG2PVU>
HAECs	NUX2WHRTTnWwY4Tpc44hSXO\|YYm=	M1vFUVExKM7:TR?=	M1rv[FEhcA>?		MYdCpIF1fGWwdXH0[ZMhXE6ILd8xMZN1cW23bHH0[YQhUUODTT2xJIFv\CCYQ1HNMVEh\XiycnXzd4lwdg>?	NFrIbYQzPDF\|NE[1Oy=>
Ca9-22	NWnCfW12TnWwY4Tpc44hSXO\|YYm=	NEP2O4s{KM7:TR?=	NWPjU4FmOSCq		MknqZYJwdGm\|aHXzJJRp\SCjYnnsbZR6KG:oIFjiVkB1dyCrbnT1Z4UhUUxvODDwdo9lfWO2aX;u	MXuyOFEzPjV\|Mh?=
Ca9-22	NHrIOJFHfW6ldHnvckBCe3OjeR?=	NVHVOZdSOyEQvF2=	MWmxM\|IhcA>?		Mkj5doVlfWOnczDIZnIucW6mdXPl[EBCXEZvMjDwbI9{eGixconsZZRqd25?	NGi1VJAzPDF{NkWzNi=>
AGS	Ml3QSpVv[3Srb36gRZN{[Xl?	MonENVAh\|ryPwrC=	MljQNE42KGh?		NUPCXIZmcW6qaXLpeJMhfGinIIXwdoVofWyjdHnvckBw\iC2aHWgTWwuQCCpZX7l	MW[yOFExPjF4Nh?=
Caco-2	MX7BdI9xfG:\|aYOgRZN{[Xl?	MY[xNOKh\|ryP	MX2yOOKhcA>?		Mniy[IVkemWjc3XzJINmdGxiYYDvdJRwe2m\|IHnu[JVk\WRiYomgOU1HXQ>?	MkjDNlQxQTV6NkO=
HCT-8	M1z5cmFxd3C2b4Ppd{BCe3OjeR?=	NF[yWHAyOMLizszN	MUSyOOKhcA>?		MXPk[YNz\WG\|ZYOgZ4VtdCCjcH;weI9{cXNiaX7keYNm\CCkeTC1MWZW	MV[yOFA6PTh4Mx?=
A549	Moq1SpVv[3Srb36gRZN{[Xl?	MXe1NOKh\|ryP	MYqyJIg>		M3PT[YJtd2OtczDFVmsheGixc4Doc5J6dGG2aX;uJI1m\GmjdHXkJIJ6KDFuMj3OVS=>	Mnz6NlQxPjd5Mke=
HPMC	MlvCSpVv[3Srb36gRZN{[Xl?	M3\JOFExyqEQvF2=	MoGwOFghcA>?		NFHPdZlz\X[ncoPld{B1cGViY3jhcodmeyCrbjDj[YxtKG2xcoDoc4xw\3liaX7keYNm\CCkeTDIS3BFWw>?	MkXMNlQxPDJ6M{i=
HPMC	NIm5NI1CeG:ydH;zbZMhSXO\|YYm=	NYewUVFPOTEEoN88US=>	M1XMXlI1yqCq		MVfy[ZZmenOnczDk[YNz\WG\|ZTDpckBk\WyuII\pZYJqdGm2eTDpcoR2[2WmIHL5JGhIWESV	NIm1VWEzPDB2MkizPC=>
MGC803	M3[5W2Fxd3C2b4Ppd{BCe3OjeR?=	MXyyNOKh\|ryP	NGjMeFIyKGh?		MVjpcohq[mm2czDhdI9xfG:\|aYOgbY5lfWOnZDDifUBKTk5vzsJCpIFv\CB34pEyMWRHXVJ?	NEnoSZIzPDB{N{e1NC=>
SGC7901	NIfi[ZZCeG:ydH;zbZMhSXO\|YYm=	NGr3Z4ozOMLizszN	NGTMTJEyKGh?		M2TnZolvcGmkaYTzJIFxd3C2b4Ppd{BqdmS3Y3XkJIJ6KEmITj5OteKh[W6mIEZihNIuTE[XUh?=	M3fhTFI1ODJ5N{Ww
COLO205	MYHBdI9xfG:\|aYOgRZN{[Xl?	MVixNE8zOC92MDFOwG0>	M2PHbVI1KGh?		NXzFdo0{cW6mdXPld{BFVkFibHHk[IVzKG[xcn3heIlwdg>?	M3qwbVI1ODF7MUC4
G292	M1KzSmFxd3C2b4Ppd{BCe3OjeR?=	MlnXN\|DDqM7:TR?=	NGjsS4kzKGh?		Ml;JdoV{fG:{ZYOgZ4Fxe2GrY3nuMYlv\HWlZXSgZ4VtdCCmZXH0bC=>	NYOz[Y1YOjRyMUK5N\|A>
BxPC-3	NFTxPHVHfW6ldHnvckBCe3OjeR?=	M1PFb\|ExKM7:TdMg	MV:2JIg>		NGjMXFhqdmO{ZXHz[UBucVJvMUSzJIV5eHKnc4Ppc44>	MUSyN\|k4OzdzMB?=
HPAF-II	M33ST2Z2dmO2aX;uJGF{e2G7	NWnORmFQOTBizszNxsA>	MnPGOkBp		NX2yfI1bcW6lcnXhd4UhdWmULUG0N{BmgHC{ZYPzbY9v	NX\sZnZ2OjN7N{O3NVA>
HL-60	NEfoR2JCeG:ydH;zbZMhSXO\|YYm=	NX\rblJ6PTEEoN88US=>	MnX0NUBp		MUjy[ZNkfWW\|IFLBNVQ2KG2nZHnheIVlKGGyb4D0c5Nqew>?	MmC4NlM6PDh5NUG=
HepG2	MVXGeY5kfGmxbjDBd5NigQ>?	M{XWN\|QxKM7:TR?=	M1ziZ\|YwOTJiaB?=		NHjpWGJqdmirYnn0d{B1cGViaX7jdoVie2Vib3[gdE1GWktzIHHu[EBxNWNvSoXuJJBzd3SnaX6g[ZhxemW\|c3nvckBjgSCSTB?=	M{\vU\|I{QTR{OEWx
HUVECs	NVzkflRNTnWwY4Tpc44hSXO\|YYm=	NX:5U3hxOjVizszN	NVnIWVBrOSCq		NVXUWIs1cW6lcnXhd4UhVkZvzsrCJJA3PSCwdXPs[YFzKHS{YX7zcI9k[XSrb36=	NFjYfHQzOzlyMUCwPC=>
LNCaP	NGPzeVRHfW6ldHnvckBCe3OjeR?=	MYexNEDPxE4EoB?=	MUGxJIg>		NHjjXIZl\WO{ZXHz[ZMhfGinIFXHSkB2eHKnZ4XsZZRm\CCyLWnCMVE>	MoL5NlM5Ozh\|MUi=
HL60	NVfETWh7TnWwY4Tpc44hSXO\|YYm=	NWryWoF4OjEEoN88US=>	M4fEbFczKGh?	MU\EUXNQ	NVP1[ndZcW6qaXLpeJMh\GG\|YYTpcoljNWmwZIXj[YQhS0RzMXKg[ZhxemW\|c3nvci=>	MYKyN\|gzPTV6NR?=
NB4	NGjobJJHfW6ldHnvckBCe3OjeR?=	Mnn2NVAh\|ryPwrC=	NYPteFhtPzJiaB?=	Ml7jSG1UVw>?	M1ztcolvcGmkaYTzJIRie2G2aX7pZk1qdmS3Y3XkJGNFOTGkIHX4dJJme3Orb36=	NXP5[WNXOjN6MkW1PFU>
EPOR/CR3	MmDxSpVv[3Srb36gRZN{[Xl?	MlLkOVDDqM7:TR?=	M3jkeVMhcA>?		MljJdoVlfWOnczDFVG8h[W6mL3;yJGlNNTNvaX7keYNm\CC2aHWgeJlzd3OrbnWgdIhwe3Cqb4L5cIF1cW:wwrC=	MV6yN\|gzODd\|MR?=
HUASMCs	M4nKbmZ2dmO2aX;uJGF{e2G7	MUSxNEDPxE4EoB?=	MWCyOEBp		NEWyfXhlcW2rbnnzbIV{KEGwZzDJTU1k[XW\|ZXSgV29EWzNibWLORUBidmRicILveIVqdiCneIDy[ZN{cW:wwrC=	MlPlNlM5OTZ2Nki=
HUASMCs	M4DLPGZ2dmO2aX;uJGF{e2G7	M4TMdVExKM7:TdMg	MVmyOEBp		M1TFfIlvcGmkaYTzJGFv\yCLST3pcoR2[2WmIFXST\|EwOiCyaH;zdIhwenmuYYTpc44hdGW4ZXy=	MknXNlM5OTZ2Nki=
SGC7901	MmfFSpVv[3Srb36gRZN{[Xl?	MmPqNVAh\|ryPwrC=	NFLZcXczPCCq		MVLpcohq[mm2czD0bIUh\XiycnXzd4lwdiCxZjDwbI9{eGixconsZZRm\CCHUluxM\|I>	NVroTGRLOjN5OUK1PFg>
MKN45	Ml7TSpVv[3Srb36gRZN{[Xl?	NHzXUHEyOCEQvF5CpC=>	NEn5UVEzPCCq		NXvXNJFRcW6qaXLpeJMhfGinIHX4dJJme3Orb36gc4YheGixc4Doc5J6dGG2ZXSgSXJMOS9{	M3TIWFI{Pzl{NUi4
SGC7901	NGnWfJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MVOxNEDPxE4EoB?=	M4nabVI1NzR6L{eyJIg>		MV\pcohq[mm2czDj[YxtKGe{b4f0bEBkdy22cnXheIVlKHerdHigSGFRXA>?	NGn3fnEzOzd7MkW4PC=>
MKN45	NHvJb4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M1\uN\|ExKM7:TdMg	NHvuU\|kzPC92OD:3NkBp		MVnpcohq[mm2czDj[YxtKGe{b4f0bEBkdy22cnXheIVlKHerdHigSGFRXA>?	NF;qNpMzOzd7MkW4PC=>
SGC7901	MVTBdI9xfG:\|aYOgRZN{[Xl?	MmHsNVAh\|ryPwrC=	M{nnNVI1KGh?		M1K2O4lv[3KnYYPld{B1cGViRFHQWE1qdmS3Y3XkJINmdGxiYYDvdJRwe2m\|	M{XHeFI{Pzl{NUi4
MKN45	MUTBdI9xfG:\|aYOgRZN{[Xl?	NEHyd3cyOCEQvF5CpC=>	NXTVbGRxOjRiaB?=		MlrkbY5kemWjc3XzJJRp\SCGQWDUMYlv\HWlZXSgZ4VtdCCjcH;weI9{cXN?	NXzBVmlbOjN5OUK1PFg>
BxPC-3 cells	Ml30S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NGDGXXczOMLizszN	NX7QdpZGOC53IHi=		NXjDSZVZcW6qaXLpeJMhXkWJRj3BMZJm\3WuYYTl[EBJXV[HQzDndo94fGhiYX7kJJR2[mViZn;ycYF1cW:wIHnu[JVk\WRiYomgVGFTNTJiQWC=	MWeyN\|c3PDB2Nh?=
NB4	Mn7TRZBweHSxc3nzJGF{e2G7	NXSwRVZsOTBxMkCvOlAh\|ryP	NXjO[2ZWOS53IHi=	MVPEUXNQ	NYfEWGJM\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JINwNXS{ZXH0[YQhf2m2aDDQZYNtcXSjeHXs	M4PVXlI{PzN3NUSx
HepG2	MmjISpVv[3Srb36gRZN{[Xl?	MnHhNlDDqM7:TR?=	NIrV[\|UzPCCq		M2j2U4lvcGmkaYTzJJRp\SCKTz2xJJBzd3SnaX6g[ZhxemW\|c3nvckBkdy22cnXheIVlKHerdHigcYV1\m:{bXnu	MUSyN\|cxPzZyOR?=
HUVECs	MYLBdI9xfG:\|aYOgRZN{[Xl?	MYSyM\|Qh\|ryP	NYTLeGhPOjRxNEigbC=>		M1PHWolv\HWlZYOgZ4VtdCCmZXH0bC=>	NW\UboNzOjN5MEe1NlA>
KG-1	M2jmcmFxd3C2b4Ppd{BCe3OjeR?=	MW[yNOKh\|ryP	NVLGdmRROTJiaB?=		NG\Gc4dmdmijbnPld{Bk\WyuIHHwc5B1d3OrczDpcoR2[2WmIHL5JHMy	MYKyN\|cxPjZ7MR?=
AML 1#	NH7JbohCeG:ydH;zbZMhSXO\|YYm=	M4\MNlIxyqEQvF2=	NILs[4wyOiCq		NHW0VWxmdmijbnPld{Bk\WyuIHHwc5B1d3OrczDpcoR2[2WmIHL5JHMy	NH61OnAzOzdyNk[5NS=>
A2780	NEDmVGZHfW6ldHnvckBCe3OjeR?=	MnLZNlDDqM7:TR?=	M1HWXlEhcA>?		NIP5eXFjdG:la4OgSHRETC2rbnT1Z4VlKESUNTDlfJBz\XO\|aX;u	Ml;5NlM3QTZ6NkK=

... 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]	+ Expand 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]	+ Expand 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]	+ Expand 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

+ Expand

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).

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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The Serial Dilution Calculator Equation

Serial Dilutions
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Computed Result

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):

Molecular Weight Calculator

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Molarity Calculator

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

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 147 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 147 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)