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 50 Publications

10 Customer Reviews

  • a-c, Inhibitors of BRAFV600E (PLX4032) and MEK1/2 (PD98059 or AZD6244) increase PGC1α and ID2 expression (a, b) and repress integrin expression and signalling (b, c). Cells were treated with indicated concentration of inhibitors for 6 h (a, b) or 24 h (c). d, e, PLX4032 increases the interaction between ID2 and TCF4 (d) and decreases the occupancy of TCF4 at the promoters of integrin genes (e). f–g, PGC1α and ID2 are partially required for PLX4032-mediated inhibition of invasion and metastasis. For in vitro assays (f), A375 cells were incubated with 1 μM PLX4032 for 10 h. Images represent one picture captured per membrane with the scale bar representing 200 μm. Values in a, b, e and f represent mean±s.d. of independent biological triplicates; *P<0.05 and **P<0.01 by Student's t-test  in a, b, e, f.

    Nature, 2016, 537(7620):422-427.. PD98059 purchased from Selleck.

     

    Melanoma cell viability and in vivo growth by cyclindependent kinase 2/4 inhibition. Western blot analysis for c-Jun, phosphorylated-ERK1/2 (Thr202/Tyr204) (p-ERK1/2), and total ERK1/2 protein levels was done for human melanoma cell lines treated with the BRAFV600E inhibitor GDC-0879 (1 μM), or MEK inhibitors CI-1040 (1 μM), U0126 (1 μM), and PD98059 (10 μM) for 18 hours.

    J Natl Cancer Inst 2012 104(21), 1673-9. PD98059 purchased from Selleck.

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    Melanoma cell viability and in vivo growth by cyclindependent kinase 2/4 inhibition. In vivo growth of LOXIMVI xenografts in athymic nude Foxn1nu mice is shown. Tumors were allowed to grow to a maximum volume of 250 mm3, and the mice were subsequently treated daily at the indicated dose levels with CDK2/4 inhibitors by intraperitoneal injection in combination with a BRAFV600E- or MEK-inhibitor. CDK2/4 inhibitor (CVT-313/indolocarbazole CDK4-I) treatment sensitizes tumors to GDC-0879 and CI1040.

    J Natl Cancer Inst 2012 104(21), 1673-9. PD98059 purchased from Selleck.

    effect of ERK1/2 inhibitor PD98059 (1, 5, and 10 μM) on SRP72 protein expression was evaluated on Jurkat cells stimulated with rhIL-1. The cells were harvested at 0,120, and 240 min, and the protein expression was verified by WB using antibodies against human SRP72, human SRP54 (nonphosphorylated SRP protein), and humanGAPDHas constitutive protein.Adecreased SRP72 expression at 10 μM and 240 min was found.

     

     

    J Biol Chem 2010 285, 32824-32833. PD98059 purchased from Selleck.

  • C, effect of ERK1/2 inhibitor PD98059 (1, 5, and 10 μM) was evaluated in SRP72-immunoprecipitated cell lysates. WB using anti-phosphoserine antibody showed a decreased SRP72 band when used as the inhibitor at concentrations of 1 μM at 240 min, 5 μM at 120 min, and 10 μM at 120 and 240 min (lanes 3, 5, 8, and 9). D, results were analyzed and RUA illustrated, finding significant results at 1 μM at 240 versus 0, 5 μM at 120 versus 0, and 10 μM at 120 versus 0 min.

     

     

    J Biol Chem 2010 285, 32824-32833. PD98059 purchased from Selleck.

    We used real time RT-PCR to investigate the effects of PD98059 on SRP72 mRNA expression. All the samples were treated under the same experimental conditions used in protein tests done by WB, and phosphorylation was measured indirectly by IP-WB. The results did not show significant changes on the mRNA expression of SRP72 after the treatment with these inhibitors.

     

     

    J Biol Chem 2010 285, 32824-32833. PD98059 purchased from Selleck.

  •  

    Activation of a TLR2eERK1/2 pathway in MDDC. (C) MDDC were either untreated or treated with C. pneumoniae alone or in the presence of the ERK1/2 inhibitor PD98059 for 48 h. IL-12p70 and IL-10 release in culture media was assessed by ELISA. (D) MDDC were treated as in panel C for 48 h and then cocultured with purified allogeneic CD3t T cells. On day 12, supernatants were collected, and secreted cytokines were measured by ELISA.

    Microbes Infect 2013 15, 105-14. PD98059 purchased from Selleck.

    HepG2 cells, “Pnt-2” primary HCC cells or THLE-2 normal liver cells were pretreated with PD-98059 (1 mM) or MEK-162 (“MEK”, 1 mM) for 1 h prior toWAY-600 (“WAY”, 100 nM) treatment, after applied period, cell viability and apoptosis were tested by MTT assay (F and H).

    Biochem Biophys Res Commun, 2016, 474(2):330-7.. PD98059 purchased from Selleck.

  • Collagen I and α-SMA are conducive for S. aureus adhesion to and invasion into BMFBs. BMFBs were treated with PD98059 2 h before the addition of 5 ng/ml TGF-β1; 24 h later, the adhesion (A) and invasion (B) assays were performed as previously described. The results are expressed as the mean cfu/ml ± SD from experiments performed in triplicate (*P < 0.05, **P < 0.01).

    Microb Pathog, 2017, 106:25-29. PD98059 purchased from Selleck.

    After starved in serum-free medium for 24h,T47D cells incubated with the indicated concentrations of  PD98059 for 3h,followed by 20-minute  stimolation of 100ng/ml EGF.

     

    2010 Dr. Zhang of Tianjin Medical University. PD98059 purchased from Selleck.

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 M1;rTmZ2dmO2aX;uJGF{e2G7 NUnMeYN[OjVizszN NHLSWlcyKGh? NG\oTYdjdHWwdIOgeIhmKEKdYW3QMYlv\HWlZXSgbY5kemWjc3WgbY4heGixc4Doc{1EcGtzIHHu[EBxcG:|cHjvMWVTUyCneIDy[ZN{cW:w NI\6[okzPTd4OUG4NS=>
MCF-7  MVrGeY5kfGmxbjDBd5NigQ>? NIq0dGkyOCEQvF2= M1PvVFEhcA>? M1TGPYlvcGmkaYTzJGlNNTF6LXXubIFv[2WmIHPlcIwhdWmpcnH0bY9v NGezfmkzPTd{N{CxNS=>
HepG2  MYDGeY5kfGmxbjDBd5NigQ>? MnjMNVAh|ryP MoLQOUBp MkjmZoxw[2u|IIDoc5NxcG:{eXzheIVlKE2DUFvzJIlv\HWlZXSgZpkh\XixZ3Xuc5V{KFSJRj5OtlE> M4rZWVI2PTZyNEi4
HepG2  M3:0cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXeyNEDPxE1? MUiyOEBp MnzYd5VxeHKnc4Pld{BVT0ZvzsKxMYlv\HWlZXSgZ4VtdCCycn;sbYZmemG2aX;uJIFv\CCrbo\hd4lwdg>? NUfHNlN1OjV3NkC0PFg>
MDA-MB-231 MULGeY5kfGmxbjDBd5NigQ>? MXeyOUDPxE1? NUjucGR3Oi1|IHi= NYLCN3hv\GWlcnXhd4V{KHBvRWLLNU8zKGGwZDDTNVAxSTRiZYjwdoV{e2mxbh?= NF\jXHkzPTV3NUi3OS=>
SW480 MV\GeY5kfGmxbjDBd5NigQ>? MX[yNOKh|ryP M1TjXVHDqGh? NHP2SnVz\WS3Y3XzJJRp\SCneIDy[ZN{cW:wIH;mJGFVTjNicILveIVqdg>? MlPxNlU1PDd6MU[=
HCT-15 M1nQfmZ2dmO2aX;uJGF{e2G7 M3n1NlEhcA>? MnvOZZR1\W63YYTld{BRT0V{LXnu[JVk\WRicHjvd5Bpd3K7bHH0bY9vKG:oIFXyb:Kh MnfWNlU1OzF2MkW=
HCT-15 M1vMSmFxd3C2b4Ppd{BCe3OjeR?= NYXsToxYOSCq MknHZYJwdGm|aHXzJJRp\SCycn;0[YN1cX[nIHXm[oVkfHNib3[gVGdGOsLiYXfhbY5{fCCldYLjeY1qdi2rbnT1Z4VlKGGyb4D0c5Nqew>? NXroVYhIOjV2M{G0NlU>
786-O MWTBdI9xfG:|aYOgRZN{[Xl? MYC1NOKh|ryP NYLsR2lOOjRiaB?= NVH0W2E5eG:2ZX70bYF1\XQEoITo[UBxem9vYYDvdJRwfGmlIHXm[oVkfHNib3[gUmM> M4K1fFI1PTB6NEe2
A498 NUjUSIpzSXCxcITvd4l{KEG|c3H5 NXPNeocyPTEEoN88US=> NUGxSWFCOjRiaB?= MU\wc5RmdnSrYYTld:KhfGinIIDyc{1ieG:ydH;0bYMh\W[oZXP0d{Bw\iCQQx?= MWeyOFUxQDR5Nh?=
NHBE MmnKSpVv[3Srb36gRZN{[Xl? M1qxeVIwOjBizszN NX\p[mp7OiCq MYfheJRmdnWjdHXzJGlNNTN|IIP0bY12dGG2ZXSgR3hEVDhxSVytPEB{\WO{ZYTpc44> NYfEe4VXOjR2N{m1NlY>
A375 MoDmR4VtdCCLbo\hd4lwdiCDc4PhfS=> NFXNcmEyOOLCk{KwJOK2VQ>? Mn3BNlQhcA>? MmXZdoVlfWOnczDt[Yxidm:vYTDj[YxtKGmwdnHzbY9v MXuyOFQ3PjB|Nh?=
HBMEC MY\GeY5kfGmxbjDBd5NigQ>? NVK2PYVJOTBizszN M{PKUlEhcA>? MofyZoxw[2u|IG\FS2YucW6mdXPl[EBGeGiDMjDlfJBz\XO|aX;u NGPyenEzPDR3OEm4Ni=>
HPAEpiCs  NGCwT25HfW6ldHnvckBCe3OjeR?= MVizNEDPxE1? M4HXelEhcA>? NEjQfXRqdmirYnn0d{BVVkZvzsGgd5RqdXWuYYTl[EBxPDJxcES0JG1CWEticHjvd5Bpd3K7bHH0bY9v MWiyOFQ1OTh5MB?=
BeWo NWTpZmloTnWwY4Tpc44hSXO|YYm= NGDPV40yOMLizszN NWHTfmVtOiCq MYDpcohq[mm2czDFVmsyNzJ? Mn71NlQ1OzN6NE[=
PC3  NI\2WoJCeG:ydH;zbZMhSXO|YYm= NUnlOWtyPTBizszN Ml;sNE42KGh? MX;pcohq[mm2czDNTHkuPDR7LXnu[JVk\WRiYYDvdJRwe2m|wrC= MWqyOFQzPDh6OR?=
HGC-27 MYHBdI9xfG:|aYOgRZN{[Xl? NEi0VnoyKML3TR?= M1PFUFEhcA>? NXe2c|hGe3WycILld5NmeyCUQVSwNFEheGy3czDNT{0zOjB4LXnu[JVk\WRiY3XscEB3cWGkaXzpeJkhdG:|cx?= Mo\kNlQ1OTZ|NEm=
MCF-7 MVzGeY5kfGmxbjDBd5NigQ>? Mnv1NVDDqM7:TR?= MUOxNE8{OCCvaX6= NWHtU|NbemWmdXPld{B1cGViVWTQMYRmeGWwZHXueEBGWkticHjvd5Bpd3K7bHH0bY9v MonINlQ{QTB6MUm=
HUVECs NGTkV3FHfW6ldHnvckBCe3OjeR?= M1XpZlExyqEQvF2= MoLLNUBp M{LSbYlvcGmkaYTzJJRp\SCKRFygdoVlfWOnZDDDU3guOiCneIDy[ZN{cW:wIHHu[EBRT0lvMjDy[Yxm[XOn M1:xR|I1Ozh3MUC5
HeLa MXHGeY5kfGmxbjDBd5NigQ>? NF:z[Iw2OCEQvF2= NITBWlIxNjViaB?= Mn35Zoxw[2u|IGTSXE0yKG63Y3zlZZIhdWmpcnH0bY9vKGGwZDDUXG5KWCCmb4fuMZJm\3WuYYTpc44> NUHyUFlCOjR|N{[4Nlc>
HL-60  M330[WZ2dmO2aX;uJGF{e2G7 M4iydlExNzJyIN88US=> NILEXWEyKGh? NUHOVopXcW6qaXLpeJMhfGinwrDOMkBkcGmwZX7zbZNmgHS{YXP0xsBqdmS3Y3XkJIRq\m[ncnXueIlifGmxbjDpcpRwKGe{YX71cI9kgXSncx?= NFTXNogzPDN3N{CyNC=>
HL-60 Ml34SpVv[3Srb36gRZN{[Xl? M1ryOVIhyrWP MVmxOkBp NYTyWnVuTE2VTx?= M1\4ZolvcGmkaYTzJJRp\SCjc4PvZ4lifGmxbjDv[kBxWzZ{MTDSZYYuOSCjbnSgUmZCXGN|LDDhcoQhfGinIGLBMYlv\HWlZXSgdIhwe3Cqb4L5cIF1cW:wIH;mJI52[2ynYYKgUmZCXGN| Mn3yNlQ{OzByNki=
HEK 293 Mni0SpVv[3Srb36gRZN{[Xl? NWr6OpdjOTBizszN MYq1JIg> MWrEUXNQ MVXpcohq[mm2czDXcpQucW6mdXPl[EDPui2lYYTlcolvN1SFRkSgZYN1cX[rdImgZY5lKG63Y3zlZZIh|rJvY3H0[Y5qdiCjY3P1cZVt[XSrb36= MU[yOFMzPDN4Nh?=
HEK 293 Ml;ESpVv[3Srb36gRZN{[Xl? NEDmUG8yOCEQvF2= NGrhOmk2KGh? MV;EUXNQ NU[4PHNFe3WycILld5NmeyC2aHWgR3JVKGGldHn2bZR6 M{fsRVI1OzJ2M{[2
SW480 NWC3SYlYTnWwY4Tpc44hSXO|YYm= NHXMVXgyOCEQvF2= MVqyNEBp NX3lUnZWTE2VTx?= NYK4TpFve3WycILld5NmeyC2aHWgR3JVKGGldHn2bZR6 MlzhNlQ{OjR|Nk[=
HCSMCs MlHXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF:1b4YyOCEQvF2= NEnCUHAzPCCq MYficI9kc3NiRlHCVFQucW6mdXPl[EBJS0GVTVOgdJJwdGmoZYLheIlwdg>? NITIZZAzPDNzMkO4NS=>
PANC-1 M3rUSWZ2dmO2aX;uJGF{e2G7 NXzBVmpJOjBizszN NVvYNHZCPDhiaB?= MWDpcohq[mm2czD0bIUh\XiycnXzd4lwdiCxZjFOmFZFKGmwIILld5BwdnOnIITvJJRp\SCSUFHS{tTDqGGpb37pd5TDqA>? M1XES|I1Ojl2MUOz
A549 MVTGeY5kfGmxbjDBd5NigQ>? MlL5N|Ah|ryP MlLnNE42KGh? NFTmUZNFVVOR NXfGNVVtcW6qaXLpeJMhfGinIITodo9u[mmwLXnu[JVk\WRiSVytPE9EYEOOOD3MeYMh[WO2aY\peJk> MmDUNlQzPzd4OU[=
A549 NV\ob29wTnWwY4Tpc44hSXO|YYm= MmTrN|Ah|ryP M2frWFAvPSCq MVLEUXNQ M2PyNIlvcGmkaYTzJJRpem:vYnnuMYlv\HWlZXSgR{9GSlEQsjDUbJIzOzYEoIDoc5NxcG:{eXzheIlwdg>? NIHVbnQzPDJ5N{[5Oi=>
MC-3 M1XMNmFxd3C2b4Ppd{BCe3OjeR?= M2[5XVExKM7:TR?= MXeyOEBp MVTwc5RmdnSrYYTl[EBOTVOFLXnu[JVk\WRiYYDvdJRwe2m|IHnuJEBk\Wyucx?= NH3sOVczPDJ5MEWyNy=>
Raji  NFexUWFHfW6ldHnvckBCe3OjeR?= MYWxNEDPxE1? MofXNUBp MUPicI9kc3NiaIPCRWZHKGmwZIXj[YQhTXKtMT:yJJBpd3OyaH;yfYxifGmxbh?= NVTpcINuOjR{Nkm2N|A>
Raji  MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fQRlExKM7:TR?= NHjUN2syKGh? MXXpcohq[mm2czD0bIUh[mG|YXygc5IhcHOEQV\GMZN1cW23bHH0[YQh[2WubDDwdo9tcW[ncnH0bY9vKGGwZDD2bYFjcWyrdIm= NWrkXY5QOjR{Nkm2N|A>
HT29 NEDRbGhHfW6ldHnvckBCe3OjeR?= NVHIXJJMOTBizszN NVvkNmc{OiCq NXfkeHVucW6qaXLpeJMhd2ZiSlHLNkwhTVKNMT:yJIFv\CCVVFHUN{BxcG:|cHjvdplt[XSrb36= NEnRU2wzPDJ4NUK5Ny=>
HepG2 NUPKN2ZlSXCxcITvd4l{KEG|c3H5 MVSyNEDPxE1? M{n3flI1KGh? MmjObY5pcWKrdIOgSXJMOS9{IIDoc5NxcG:{eXzheIlwdiCjbnSg[Y5p[W6lZYOgWmIyNWmwZIXj[YQh[XCxcITvd4l{ NUDveFJEOjR{NEe5NFk>
HepG2 NEHsdXhHfW6ldHnvckBCe3OjeR?= NW\IN446OjBizszN M1r3VlIhcA>? MXrlcohidmOnczDWRlEucW6mdXPl[EBHV1iRM3GgeJJidnOlcnnweIlwdmGuIHHjeIl3cXS7 NHm2TIYzPDJ2N{mwPS=>
TE4 NUfkU5BYTnWwY4Tpc44hSXO|YYm= M4e0W|IxNzVyL{GwNEDPxE1? NHP2WHk1QCCq NU\uR5NRTE2VTx?= M3LhOolvcGmkaYTzJJAuTXKtIHHu[EB4d3K2bXHucolvKGSxd37y[Yd2dGG2ZXSgdE1Cc3RiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NFvaOmIzPDJ2NECyNy=>
TE1 NFvPXIVHfW6ldHnvckBCe3OjeR?= NV\ReG16OjBxNUCvNVAxKM7:TR?= MUi0PEBp NIfjdVZFVVOR NIeybW1qdmirYnn0d{BxNUW{azDhcoQhf2:{dH3hco5qdiCmb4fudoVofWyjdHXkJJAuSWu2IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ M321XFI1OjR2MEKz
KYSE30 Mmf5SpVv[3Srb36gRZN{[Xl? NF72TnEzOC93MD:xNFAh|ryP M3HBTFQ5KGh? NXXu[4xUTE2VTx?= M2jaWIlvcGmkaYTzJJAuTXKtIHHu[EB4d3K2bXHucolvKGSxd37y[Yd2dGG2ZXSgdE1Cc3RiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M3PFPFI1OjR2MEKz
TE1 MU\GeY5kfGmxbjDBd5NigQ>? NWjYcY4xPTBizszN NULlbmJ2PDhiaB?= MnfMSG1UVw>? NHfue4h2eHKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCKTFGgZ4xie3NiSR?= MoDQNlQzPDRyMkO=
TE3 Mke1SpVv[3Srb36gRZN{[Xl? Mn;KOVAh|ryP MnTQOFghcA>? M3Pwd2ROW09? MUX1dJJm\3WuYYTld{B1cGViZYjwdoV{e2mxbjDv[kBJVEFiY3zhd5MhUQ>? M1n4dFI1OjR2MEKz
TE4 NYDEVphvTnWwY4Tpc44hSXO|YYm= NUftXGtRPTBizszN MWW0PEBp MlvnSG1UVw>? MmXxeZBz\We3bHH0[ZMhfGinIHX4dJJme3Orb36gc4YhUEyDIHPsZZN{KEl? NELkRmEzPDJ2NECyNy=>
TE5 MWPGeY5kfGmxbjDBd5NigQ>? NY\RbIo4PTBizszN NVL1fZU{PDhiaB?= NEiwNphFVVOR MoLweZBz\We3bHH0[ZMhfGinIHX4dJJme3Orb36gc4YhUEyDIHPsZZN{KEl? MXiyOFI1PDB{Mx?=
KYSE30 Mnn3SpVv[3Srb36gRZN{[Xl? MWe1NEDPxE1? M2LmVlQ5KGh? NYfpO5BSTE2VTx?= NVLYTYlDfXC{ZXf1cIF1\XNidHjlJIV5eHKnc4Ppc44hd2ZiSFzBJINt[XO|IFm= NH:y[oYzPDJ2NECyNy=>
MKN7 MmLJSpVv[3Srb36gRZN{[Xl? MnTFOVAh|ryP MVO0PEBp NYXSR|lXTE2VTx?= Mne5bY5kemWjc3XzJIV5eHKnc4Ppc44hd2ZiSFzBMWExOiCxcjDIUGEuSTJ2IH3vcIVkfWyncx?= NGmyd|kzPDJ2NECyNy=>
OE19 M3zlXmZ2dmO2aX;uJGF{e2G7 M2\NVFUxKM7:TR?= M1vpXVQ5KGh? MVfEUXNQ NFTKbVRqdmO{ZXHz[ZMh\XiycnXzd4lwdiCxZjDIUGEuSTB{IH;yJGhNSS2DMkSgcY9t\WO3bHXz NELhfFUzPDJ2NECyNy=>
KATOIII  M{HaRWZ2dmO2aX;uJGF{e2G7 M1P2TlUxKM7:TR?= MofBOFghcA>? NHrZPJFFVVOR NHf3XXhqdmO{ZXHz[ZMh\XiycnXzd4lwdiCxZjDIUGEuSTB{IH;yJGhNSS2DMkSgcY9t\WO3bHXz NXjnb|kxOjR{NESwNlM>
NCI-N87  MXTGeY5kfGmxbjDBd5NigQ>? MlrnOVAh|ryP NIDUZlU1QCCq MWjEUXNQ NHHFfoxqdmO{ZXHz[ZMh\XiycnXzd4lwdiCxZjDIUGEuSTB{IH;yJGhNSS2DMkSgcY9t\WO3bHXz NV64b29POjR{NESwNlM>
NUGC3 M17zfmZ2dmO2aX;uJGF{e2G7 NE\GOZE2OCEQvF2= NFzJNHk1QCCq Ml[5SG1UVw>? MoPDbY5kemWjc3XzJIV5eHKnc4Ppc44hd2ZiSFzBMWExOiCxcjDIUGEuSTJ2IH3vcIVkfWyncx?= NI\qd2gzPDJ2NECyNy=>
NUGC2 MknxSpVv[3Srb36gRZN{[Xl? MUC1NEDPxE1? NXntWodXPDhiaB?= M1HLb2ROW09? NXnUW|Y{cW6lcnXhd4V{KGW6cILld5Nqd25ib3[gTGxCNUFyMjDvdkBJVEFvQUK0JI1wdGWldXzldy=> NUjPOYtGOjR{NESwNlM>
SGC-7901  MYjBdI9xfG:|aYOgRZN{[Xl? M3rMclIxKM7:TR?= NFPSVI0zPCCq MV\pcohq[mm2czDDVE1u\WSrYYTl[EBieG:ydH;zbZM> M13CdVI1OjRzM{Wx
MG-63 NGrRVGtHfW6ldHnvckBCe3OjeR?= NW[yNJJROjBizszN MkfuNE42KGh? MUXicI9kc3NidHjlJGNJNWmwZIXj[YQheGixc4Doc5J6dGG2ZXSgSWxMOSCycn;0[YlvKGW6cILld5Nqd25? M3PtZVI1OjN7NkSw
ARPE-19 MmHtSpVv[3Srb36gRZN{[Xl? NYL4TXJIOjBizszN NVX6SphMOC53IHi= NGjSWmVqdmirYnn0d{BCeGWuaX6tbY5lfWOnZDDwbI9{eGixconsZZRqd25ib3[gSZJsKGGwZDDBb5Q> M3;FbFI1OjJ5OUG4
CRL-2302 M1j5VmZ2dmO2aX;uJGF{e2G7 NFmwdZYzOCEQvF2= NEH6VHkxNjViaB?= NHrDW5pqdmirYnn0d{BCeGWuaX6tbY5lfWOnZDDwbI9{eGixconsZZRqd25ib3[gSZJsKGGwZDDBb5Q> NFfUNoEzPDJ{N{mxPC=>
MCF-7 M161cWZ2dmO2aX;uJGF{e2G7 NGja[oEzOCEQvF2= MmXuNUBp NXn0NFBZ[WKxbHnzbIV{KGW6cILld5Nqd25ib3[gdIhwe3Cqb4L5cIF1\WRiRWLLJINwNXS{ZXH0cYVvfCC5aYToJINwdmq3Z3H0[S=> NI\GNY8zPDJzNkK4PS=>
MCF-7 M2rDfWFxd3C2b4Ppd{BCe3OjeR?= M2j4ZVIxKM7:TR?= MoS2NUBp MUDpcoNz\WG|ZYOgZ4F{eGG|ZT25JIVvgnmvZTDhZ5Rqfmm2eR?= MnnpNlQzOTZ{OEm=
DLD-1  M{PRdGZ2dmO2aX;uJGF{e2G7 NGjT[mQzOMLizszN MXu0PEBp MlvzdoVlfWOnczD0bIUhSk6LUEOg[ZhxemW|c3nvckBxemVvdILlZZRm\CC5aYToJFUu[XqjLXTD M1zJZVI1OjFzNUix
HT-29 MnL1SpVv[3Srb36gRZN{[Xl? NIDHXnIzOMLizszN MYO0PEBp MV3y[YR2[2W|IITo[UBDVkmSMzDlfJBz\XO|aX;uJJBz\S22cnXheIVlKHerdHigOU1igmFvZFO= NGLKRZczPDJzMUW4NS=>
7402 M1TBPGFxd3C2b4Ppd{BCe3OjeR?= MX[zNEDPxE1? NVy4OVNWPSCm NYDGSGh1\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdg>? NFXMd20zPDJzMUK1Ny=>
7721 M{Dnd2Fxd3C2b4Ppd{BCe3OjeR?= Mln1N|Ah|ryP NITUW3c2KGR? M2P4UoRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44> M2i3cFI1OjFzMkWz
SGC7901  M17Ec2Fxd3C2b4Ppd{BCe3OjeR?= NYCxeGdOPTEEoN88US=> NEXMeo8zPC92OD:3NkBp NGPK[YlFVVOR M{jScIlv\HWlZYOgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiSlHLNkB{cFKQQR?= NUHUSlRmOjRzN{iyOFA>
SMMC7721 MnmzSpVv[3Srb36gRZN{[Xl? M4rOVVI2NzVyIN88US=> NViyNo5nOjRiaB?= M4LhUpN2eHC{ZYPz[ZMhfGinIHX4dJJme3Orb36gc4YheC2Da4Sgc5IheC2HUluxM|LDqA>? Mnm1NlQyPjhyNU[=
MCF-7 NUe4dmtrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnztNVAh|ryP NF;HOoM1QGh? MoX2SG1UVw>? M{HkeJJmfmW{c3XzJGJPTi2rbnT1Z4VlKGOnbHygZ5lkdGViYYLy[ZN1 M1T6VlI1OTZ|NEC0
Caco-2 MVLGeY5kfGmxbjDBd5NigQ>? NUOxXY1zPTEEoN88US=> NYnFR|hrPDiq MYDEUXNQ M1q2TYVvcGGwY3XzJJRp\SCvUl7BJIxmfmWuczDv[uKhW0OQTkHBMGZZYUR|LNMgUGNVNMLiTF;YMOKhUEmIM1GsxsBbTzF4LNMgVGRGPkIEoHHu[OKhVEeDTGOxOuKh\2WwZYRCpINwNXS{ZXH0[YQhf2m2aDDE[Zg> M2fPZ|I1OTZzNkm1
HAECs NH3RPFdHfW6ldHnvckBCe3OjeR?= MWSxNEDPxE1? Ml3qNUBp M2nJXOKh[XS2ZX71ZZRmeyCWTl[t{tEue3SrbYXsZZRm\CCLQ1HNMVEh[W6mIG\DRW0uOSCneIDy[ZN{cW:w NFfDWpkzPDF|NE[1Oy=>
Ca9-22 MVTGeY5kfGmxbjDBd5NigQ>? MYKzJO69VQ>? NI[yNZEyKGh? M3nHR4Fjd2yrc3jld{B1cGViYXLpcIl1gSCxZjDIZnIhfG9iaX7keYNmKEmOLUigdJJw\HWldHnvci=> Mo[1NlQyOjZ3M{K=
Ca9-22 NUfNZoVRTnWwY4Tpc44hSXO|YYm= Ml3hN{DPxE1? M2rvc|EwOiCq Mmi4doVlfWOnczDIZnIucW6mdXPl[EBCXEZvMjDwbI9{eGixconsZZRqd25? NUf5dpBxOjRzMk[1N|I>
AGS NFn4cFJHfW6ldHnvckBCe3OjeR?= MVSxNEDPxE4EoB?= Mk\BNE42KGh? MmjTbY5pcWKrdIOgeIhmKHWycnXneYxifGmxbjDv[kB1cGViSVytPEBo\W6n M3voNVI1OTB4MU[2
Caco-2  NFfVU5VCeG:ydH;zbZMhSXO|YYm= NG[1eY0yOMLizszN NUHMd2xlOjUEoHi= M1HidIRm[3KnYYPld{Bk\WyuIHHwc5B1d3OrczDpcoR2[2WmIHL5JFUuTlV? MViyOFA6PTh4Mx?=
HCT-8 Mlm0RZBweHSxc3nzJGF{e2G7 MUexNOKh|ryP MoXENlTDqGh? NEXlUIdl\WO{ZXHz[ZMh[2WubDDhdI9xfG:|aYOgbY5lfWOnZDDifUA2NU[X M2PaXVI1ODl3OE[z
A549 MlT5SpVv[3Srb36gRZN{[Xl? NEnPNow2OMLizszN M1TlV|IhcA>? NVjye5E1[myxY3vzJGVTUyCyaH;zdIhwenmuYYTpc44hdWWmaXH0[YQh[nliMTyyMW5S NIL5XG4zPDB4N{eyOy=>
HPMC M4jXVGZ2dmO2aX;uJGF{e2G7 Mn7HNVDDqM7:TR?= MVe0PEBp NFPrcI1z\X[ncoPld{B1cGViY3jhcodmeyCrbjDj[YxtKG2xcoDoc4xw\3liaX7keYNm\CCkeTDIS3BFWw>? NFrkdZMzPDB2MkizPC=>
HPMC M{n1TmFxd3C2b4Ppd{BCe3OjeR?= NG\aSoMyOMLizszN M{\hNFI1yqCq M{PmW5JmfmW{c3XzJIRm[3KnYYPlJIlvKGOnbHygeoli[mmuaYT5JIlv\HWlZXSgZpkhUEeSRGO= NUTGOWlSOjRyNEK4N|g>
MGC803  NWfuPJI6SXCxcITvd4l{KEG|c3H5 M4fseVIxyqEQvF2= MmLQNUBp NGjaU3pqdmirYnn0d{BieG:ydH;zbZMhcW6mdXPl[EBjgSCLRl6t{tHDqGGwZDC15qCzNUSIVWK= MmjsNlQxOjd5NUC=
SGC7901 M{\vZmFxd3C2b4Ppd{BCe3OjeR?= M{Phe|IxyqEQvF2= NYX2WYx1OSCq MmPEbY5pcWKrdIOgZZBweHSxc3nzJIlv\HWlZXSgZpkhUU[QLd8xxsBidmRiNfMAtk1FTlWU MXSyOFAzPzd3MB?=
COLO205 MVHBdI9xfG:|aYOgRZN{[Xl? NGXwSW0yOC9{MD:0NEDPxE1? M321SVI1KGh? NIH3dI9qdmS3Y3XzJGRPSSCuYXTk[ZIh\m:{bXH0bY9v MWmyOFAyQTFyOB?=
G292  NEXCXW9CeG:ydH;zbZMhSXO|YYm= MUizNOKh|ryP NF6x[nIzKGh? M2jlRZJme3SxcnXzJINieHOjaXPpck1qdmS3Y3XkJINmdGxiZHXheIg> M3;Ib|I1ODF{OUOw
BxPC-3 NYrSUXprTnWwY4Tpc44hSXO|YYm= Mm\uNVAh|ryPwrC= NYfJeoI{PiCq M4rwSYlv[3KnYYPlJI1qWi1zNEOg[ZhxemW|c3nvci=> NIj6VowzOzl5M{exNC=>
HPAF-II Mk\jSpVv[3Srb36gRZN{[Xl? NWXDT21KOTBizszNxsA> NWO5W2dTPiCq NH\lVHRqdmO{ZXHz[UBucVJvMUSzJIV5eHKnc4Ppc44> NUDZXYJSOjN7N{O3NVA>
HL-60 MoH1RZBweHSxc3nzJGF{e2G7 M1u4eFUxyqEQvF2= NHjOdnYyKGh? MkjHdoV{[3WnczDCRVE1PSCvZXTpZZRm\CCjcH;weI9{cXN? NEXM[lQzOzl2OEe1NS=>
HepG2 MYXGeY5kfGmxbjDBd5NigQ>? MknuOFAh|ryP NEG5fJQ3NzF{IHi= MVjpcohq[mm2czD0bIUhcW6lcnXhd4Uhd2ZicD3FVmsyKGGwZDDwMYMuUnWwIIDyc5RmcW5iZYjwdoV{e2mxbjDifUBRVA>? NVjMc3d1OjN7NEK4OVE>
HUVECs MnnVSpVv[3Srb36gRZN{[Xl? NWi3S5pJOjVizszN MoWyNUBp MnfWbY5kemWjc3WgUmYu|rqEIIC2OUBvfWOuZXHyJJRz[W6|bH;jZZRqd25? NX;HcoFoOjN7MEGwNFg>
LNCaP  NIewUmZHfW6ldHnvckBCe3OjeR?= NFLQPZUyOCEQvF5CpC=> NXqwTnFpOSCq MV\k[YNz\WG|ZYOgeIhmKEWJRjD1dJJm\3WuYYTl[EBxNVmELUG= MVOyN|g{QDNzOB?=
HL60  MVTGeY5kfGmxbjDBd5NigQ>? Mn\MNlDDqM7:TR?= M{HjWFczKGh? MoDnSG1UVw>? NFX5TJZqdmirYnn0d{Bl[XOjdHnubYIucW6mdXPl[EBETDFzYjDlfJBz\XO|aX;u MV6yN|gzPTV6NR?=
NB4  M4TnUmZ2dmO2aX;uJGF{e2G7 NUTTXVRmOTBizszNxsA> MXS3NkBp M{Sw[2ROW09? MUfpcohq[mm2czDkZZNifGmwaXKtbY5lfWOnZDDDSFEy[iCneIDy[ZN{cW:w NIniV28zOzh{NUW4OS=>
EPOR/CR3 MknYSpVv[3Srb36gRZN{[Xl? Mnz1OVDDqM7:TR?= MmPRN{Bp MlXadoVlfWOnczDFVG8h[W6mL3;yJGlNNTNvaX7keYNm\CC2aHWgeJlzd3OrbnWgdIhwe3Cqb4L5cIF1cW:wwrC= MVKyN|gzODd|MR?=
HUASMCs NYrXSo15TnWwY4Tpc44hSXO|YYm= NIDyclMyOCEQvF5CpC=> NIX5e|EzPCCq Mlr1[IlucW6rc3jld{BCdmdiSVmtZ4F2e2WmIGPPR3M{KG2UTlGgZY5lKHC{b4TlbY4h\XiycnXzd4lwdsLi NUntbmM{OjN6MU[0Olg>
HUASMCs MVrGeY5kfGmxbjDBd5NigQ>? M4ezRlExKM7:TdMg MVyyOEBp MmnubY5pcWKrdIOgRY5oKEmLLXnu[JVk\WRiRWLLNU8zKHCqb4PwbI9zgWyjdHnvckBt\X[nbB?= NHnqTWQzOzhzNkS2PC=>
SGC7901 MlfOSpVv[3Srb36gRZN{[Xl? M2L6N|ExKM7:TdMg MkPiNlQhcA>? M13xXYlvcGmkaYTzJJRp\SCneIDy[ZN{cW:wIH;mJJBpd3OyaH;yfYxifGWmIFXST|EwOg>? MY[yN|c6OjV6OB?=
MKN45 M2TC[WZ2dmO2aX;uJGF{e2G7 NGnRUGIyOCEQvF5CpC=> NILjfIozPCCq NXzuWXRXcW6qaXLpeJMhfGinIHX4dJJme3Orb36gc4YheGixc4Doc5J6dGG2ZXSgSXJMOS9{ NWrISYdqOjN5OUK1PFg>
SGC7901 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkP6NVAh|ryPwrC= M3LZfVI1NzR6L{eyJIg> NXnBPXpUcW6qaXLpeJMh[2WubDDndo94fGhiY3:teJJm[XSnZDD3bZRpKESDUGS= MlzvNlM4QTJ3OEi=
MKN45 NU\JU|lYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jqc|ExKM7:TdMg NETWUnAzPC92OD:3NkBp NUnBdYZUcW6qaXLpeJMh[2WubDDndo94fGhiY3:teJJm[XSnZDD3bZRpKESDUGS= MUOyN|c6OjV6OB?=
SGC7901 MmHMRZBweHSxc3nzJGF{e2G7 MoTaNVAh|ryPwrC= Ml\WNlQhcA>? MXPpcoNz\WG|ZYOgeIhmKESDUGStbY5lfWOnZDDj[YxtKGGyb4D0c5Nqew>? MWGyN|c6OjV6OB?=
MKN45 NUHSd25vSXCxcITvd4l{KEG|c3H5 M{\se|ExKM7:TdMg MXGyOEBp NYT0U3d5cW6lcnXhd4V{KHSqZTDERXBVNWmwZIXj[YQh[2WubDDhdI9xfG:|aYO= NUC5WmNzOjN5OUK1PFg>
BxPC-3 cells MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUCyNOKh|ryP MY[wMlUhcA>? M3fXeYlvcGmkaYTzJHZGT0ZvQT3y[Yd2dGG2ZXSgTHVXTUNiZ4Lve5RpKGGwZDD0eYJmKG[xcn3heIlwdiCrbnT1Z4VlKGK7IGDBVk0zKEGS MlvCNlM4PjRyNE[=
NB4  NYHQOoM4SXCxcITvd4l{KEG|c3H5 M1npO|ExNzJyL{[wJO69VQ>? NWq0UHRIOS53IHi= MX\EUXNQ NUTafWdL\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JINwNXS{ZXH0[YQhf2m2aDDQZYNtcXSjeHXs M3:1OFI{PzN3NUSx
HepG2  M1TwW2Z2dmO2aX;uJGF{e2G7 MV2yNOKh|ryP MlLkNlQhcA>? MmTDbY5pcWKrdIOgeIhmKEiRLUGgdJJwfGWrbjDlfJBz\XO|aX;uJINwNXS{ZXH0[YQhf2m2aDDt[ZRnd3KvaX6= M2HjUFI{PzB5NkC5
HUVECs NGXFOXhCeG:ydH;zbZMhSXO|YYm= NFy4ZoEzNzRizszN NF3ydVAzPC92ODDo NV;ISIdWcW6mdXPld{Bk\WyuIHTlZZRp Ml\xNlM4ODd3MkC=
KG-1  NUnnZlc3SXCxcITvd4l{KEG|c3H5 M1zM[FIxyqEQvF2= NUWyOo1rOTJiaB?= Mlf1[Y5p[W6lZYOgZ4VtdCCjcH;weI9{cXNiaX7keYNm\CCkeTDTNS=> MorTNlM4ODZ4OUG=
AML 1# MVzBdI9xfG:|aYOgRZN{[Xl? NEi0NHYzOMLizszN NEmxV48yOiCq MmDo[Y5p[W6lZYOgZ4VtdCCjcH;weI9{cXNiaX7keYNm\CCkeTDTNS=> NETzXVgzOzdyNk[5NS=>
A2780  NXXTXpVvTnWwY4Tpc44hSXO|YYm= NUXXd2VuOjEEoN88US=> M4X0NVEhcA>? NH3ZZZNjdG:la4OgSHRETC2rbnT1Z4VlKESUNTDlfJBz\XO|aX;u M{HEVFI{Pjl4OE[y

... Click to View More Cell Line Experimental Data

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)

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

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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).

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

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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