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 49 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.

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    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.. 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 NIi0OHhHfW6ldHnvckBCe3OjeR?= NHfRe4gzPSEQvF2= MV6xJIg> NXuxcYJm[my3boTzJJRp\SCEW3HdVE1qdmS3Y3XkJIlv[3KnYYPlJIlvKHCqb4PwbI8uS2itMTDhcoQheGixc4Doc{1GWktiZYjwdoV{e2mxbh?= MYSyOVc3QTF6MR?=
MCF-7  NGHsRWVHfW6ldHnvckBCe3OjeR?= MVWxNEDPxE1? MmiyNUBp NFf1R3RqdmirYnn0d{BKVC1zOD3lcohidmOnZDDj[YxtKG2rZ4LheIlwdg>? M3\LflI2PzJ5MEGx
HepG2  MYPGeY5kfGmxbjDBd5NigQ>? NEnjSJUyOCEQvF2= M{P0[FUhcA>? NGrifpVjdG:la4OgdIhwe3Cqb4L5cIF1\WRiTVHQT5MhcW6mdXPl[EBjgSCneH;n[Y5wfXNiVFfGMe6zOQ>? M2H3S|I2PTZyNEi4
HepG2  MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPINlAh|ryP NYDtNWFnOjRiaB?= MUHzeZBxemW|c3XzJHRITi4QskGtbY5lfWOnZDDj[YxtKHC{b3zp[oVz[XSrb36gZY5lKGmwdnHzbY9v NGDtRpIzPTV4MES4PC=>
MDA-MB-231 M3Lw[GZ2dmO2aX;uJGF{e2G7 MXeyOUDPxE1? MXGyMVMhcA>? MlrR[IVkemWjc3XzJJAuTVKNMT:yJIFv\CCVMUCwRVQh\XiycnXzd4lwdg>? MonxNlU2PTV6N{W=
SW480 NGGzSINHfW6ldHnvckBCe3OjeR?= M3nYSlIxyqEQvF2= MnX4NeKhcA>? MlvrdoVlfWOnczD0bIUh\XiycnXzd4lwdiCxZjDBWGY{KHC{b4TlbY4> MlnLNlU1PDd6MU[=
HCT-15 MkLRSpVv[3Srb36gRZN{[Xl? MXqxJIg> NIjGcY5ifHSnboXheIV{KFCJRUKtbY5lfWOnZDDwbI9{eGixconsZZRqd25ib3[gSZJsyqB? NYn5[3dsOjV2M{G0NlU>
HCT-15 NHy1TIlCeG:ydH;zbZMhSXO|YYm= M2rSPFEhcA>? NWjnUoNu[WKxbHnzbIV{KHSqZTDwdo91\WO2aY\lJIVn\mWldIOgc4YhWEeHMtMgZYdicW6|dDDjeZJkfW2rbj3pcoR2[2WmIHHwc5B1d3Orcx?= NEi0dVgzPTR|MUSyOS=>
786-O NVu0XWRRSXCxcITvd4l{KEG|c3H5 Mo\oOVDDqM7:TR?= MYiyOEBp MWHwc5RmdnSrYYTld:KhfGinIIDyc{1ieG:ydH;0bYMh\W[oZXP0d{Bw\iCQQx?= MVeyOFUxQDR5Nh?=
A498 M4XCW2Fxd3C2b4Ppd{BCe3OjeR?= NHnxNJo2OMLizszN NWHaO2ZmOjRiaB?= M1vqSJBwfGWwdHnheIV{yqC2aHWgdJJwNWGyb4D0c5Rq[yCnZn\lZ5R{KG:oIF7D MYWyOFUxQDR5Nh?=
NHBE NUTzVpBDTnWwY4Tpc44hSXO|YYm= MXuyM|IxKM7:TR?= Mn;nNkBp NFXJUZlifHSnboXheIV{KEmOLUOzJJN1cW23bHH0[YQhS1iFTEivTWwuQCC|ZXPy[ZRqd25? NXjucHBCOjR2N{m1NlY>
A375 MWfD[YxtKEmwdnHzbY9vKEG|c3H5 MWWxNQKBmzJyINM1US=> Ml;QNlQhcA>? M3;Fe5Jm\HWlZYOgcYVt[W6xbXGgZ4VtdCCrbo\hd4lwdg>? MoS4NlQ1PjZyM{[=
HBMEC MWjGeY5kfGmxbjDBd5NigQ>? NYDxSGY{OTBizszN NX\zc|RMOSCq M{fweoJtd2OtczDWSWdHNWmwZIXj[YQhTXCqQUKg[ZhxemW|c3nvci=> MWOyOFQ2QDl6Mh?=
HPAEpiCs  M2PBNWZ2dmO2aX;uJGF{e2G7 NUj3dHFvOzBizszN NWDzTpZMOSCq NV7xS5VNcW6qaXLpeJMhXE6ILd8xJJN1cW23bHH0[YQheDR{L4C0OEBOSVCNIIDoc5NxcG:{eXzheIlwdg>? NHji[5MzPDR2MUi3NC=>
BeWo MlGxSpVv[3Srb36gRZN{[Xl? NF\TdnEyOMLizszN MUKyJIg> NI\5eYpqdmirYnn0d{BGWktzL{K= NIjwepUzPDR|M{i0Oi=>
PC3  M4nOT2Fxd3C2b4Ppd{BCe3OjeR?= NEXLR|I2OCEQvF2= M4nSWlAvPSCq NWnwXZgycW6qaXLpeJMhVUi\LUS0PU1qdmS3Y3XkJIFxd3C2b4Ppd:Kh MWmyOFQzPDh6OR?=
HGC-27 NVvsU45USXCxcITvd4l{KEG|c3H5 MUixJOK2VQ>? NYnkdolLOSCq NXTXW2hSe3WycILld5NmeyCUQVSwNFEheGy3czDNT{0zOjB4LXnu[JVk\WRiY3XscEB3cWGkaXzpeJkhdG:|cx?= NWDRemd[OjR2MU[zOFk>
MCF-7 MUTGeY5kfGmxbjDBd5NigQ>? NH7RXGkyOMLizszN MmL3NVAwOzBibXnu NHHPRlNz\WS3Y3XzJJRp\SCXVGCt[IVx\W6mZX70JGVTUyCyaH;zdIhwenmuYYTpc44> NFfhV2ozPDN7MEixPS=>
HUVECs NHzCcmNHfW6ldHnvckBCe3OjeR?= Mnz3NVDDqM7:TR?= MWixJIg> MlywbY5pcWKrdIOgeIhmKEiGTDDy[YR2[2WmIFPPXE0zKGW6cILld5Nqd25iYX7kJHBIUS1{IILlcIVie2V? M{XsXFI1Ozh3MUC5
HeLa Mn3xSpVv[3Srb36gRZN{[Xl? MoPOOVAh|ryP NG\VcokxNjViaB?= NGrDVI9jdG:la4OgWHJZNTFiboXjcIVieiCvaXfyZZRqd25iYX7kJHRZVkmSIHTve44uemWpdXzheIlwdg>? NX3q[5JYOjR|N{[4Nlc>
HL-60  NF[4dohHfW6ldHnvckBCe3OjeR?= NGXtZmMyOC9{MDFOwG0> M{jDTVEhcA>? NFXxeoNqdmirYnn0d{B1cGYEoF6uJINpcW6nboPpd4V5fHKjY4VCpIlv\HWlZXSg[Iln\mW{ZX70bYF1cW:wIHnueI8h\3KjboXsc4N6fGW| NXHVeYFXOjR|NUewNlA>
HL-60 NIXHXmZHfW6ldHnvckBCe3OjeR?= MlnDNkDDvU1? MmP3NVYhcA>? M1vpSWROW09? MoL4bY5pcWKrdIOgeIhmKGG|c3;jbYF1cW:wIH;mJJBUPjJzIGLh[k0yKGGwZDDOSmFV[zNuIHHu[EB1cGViUlGtbY5lfWOnZDDwbI9{eGixconsZZRqd25ib3[gcpVkdGWjcjDOSmFV[zN? Mn23NlQ{OzByNki=
HEK 293 NXrpTFNvTnWwY4Tpc44hSXO|YYm= Mn7ZNVAh|ryP NIX4XJI2KGh? MV;EUXNQ M3vIWYlvcGmkaYTzJHdvfC2rbnT1Z4VlKM7{LXPheIVvcW5xVFPGOEBi[3Srdnn0fUBidmRiboXjcIVieiEQsj3jZZRmdmmwIHHjZ5VufWyjdHnvci=> NFnMfmwzPDN{NEO2Oi=>
HEK 293 M{HkTWZ2dmO2aX;uJGF{e2G7 M3zZcFExKM7:TR?= M4XxdVUhcA>? M2jTSGROW09? NXrHVHlme3WycILld5NmeyC2aHWgR3JVKGGldHn2bZR6 NIL2So0zPDN{NEO2Oi=>
SW480 NVvJOYJOTnWwY4Tpc44hSXO|YYm= NIrEO2MyOCEQvF2= M2TtT|IxKGh? MmHxSG1UVw>? Mnnld5VxeHKnc4Pld{B1cGViQ2LUJIFkfGm4aYT5 MUKyOFMzPDN4Nh?=
HCSMCs M2P6bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVuxNEDPxE1? NInJU|gzPCCq NH[xdJljdG:la4OgSmFDWDRvaX7keYNm\CCKQ1HTUWMheHKxbHnm[ZJifGmxbh?= Ml3BNlQ{OTJ|OEG=
PANC-1 M3r2XmZ2dmO2aX;uJGF{e2G7 NFzDc|MzOCEQvF2= M1fyOVQ5KGh? NI\VZoRqdmirYnn0d{B1cGViZYjwdoV{e2mxbjDv[kDPnD[GIHnuJJJme3CxboPlJJRwKHSqZTDQVGFT|rUEoHHnc45qe3UEoB?= M3r0RVI1Ojl2MUOz
A549 Ml\nSpVv[3Srb36gRZN{[Xl? MmrKN|Ah|ryP MUewMlUhcA>? NXz2VHF[TE2VTx?= MWTpcohq[mm2czD0bIUhfGi{b33ibY4ucW6mdXPl[EBKVC16L1PYR2w5NUy3YzDhZ5Rqfmm2eR?= M3\ydVI1Ojd5Nkm2
A549 NHfqNnBHfW6ldHnvckBCe3OjeR?= NFftVWw{OCEQvF2= M1jLNFAvPSCq MUDEUXNQ M4SzeolvcGmkaYTzJJRpem:vYnnuMYlv\HWlZXSgR{9GSlEQsjDUbJIzOzYEoIDoc5NxcG:{eXzheIlwdg>? MYKyOFI4PzZ7Nh?=
MC-3 NYi5c25CSXCxcITvd4l{KEG|c3H5 Mk\UNVAh|ryP MmfGNlQhcA>? MUjwc5RmdnSrYYTl[EBOTVOFLXnu[JVk\WRiYYDvdJRwe2m|IHnuJEBk\Wyucx?= M2m5[lI1OjdyNUKz
Raji  NXL0PIlOTnWwY4Tpc44hSXO|YYm= NF;lZZoyOCEQvF2= NX;EPZZ5OSCq M2\6UYJtd2OtczDod2JCTkZiaX7keYNm\CCHcnuxM|IheGixc4Doc5J6dGG2aX;u M{jWWVI1OjZ7NkOw
Raji  MmnFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX6xNEDPxE1? NHfDepcyKGh? M{m5eolvcGmkaYTzJJRp\SCkYYPhcEBweiCqc1LBSmYue3SrbYXsZZRm\CClZXzsJJBzd2yrZnXyZZRqd25iYX7kJJZq[WKrbHn0fS=> NInpVGMzPDJ4OU[zNC=>
HT29 MmfjSpVv[3Srb36gRZN{[Xl? MnzDNVAh|ryP MlfFNkBp M4\hOolvcGmkaYTzJI9nKEqDS{KsJGVTUzFxMjDhcoQhW1SDVEOgdIhwe3Cqb4L5cIF1cW:w MmHNNlQzPjV{OUO=
HepG2 MXXBdI9xfG:|aYOgRZN{[Xl? M3jUPFIxKM7:TR?= NXXGSJhlOjRiaB?= NVzYNGtRcW6qaXLpeJMhTVKNMT:yJJBpd3OyaH;yfYxifGmxbjDhcoQh\W6qYX7j[ZMhXkJzLXnu[JVk\WRiYYDvdJRwe2m| NHzScGIzPDJ2N{mwPS=>
HepG2 M{PiOGZ2dmO2aX;uJGF{e2G7 M{TjOFIxKM7:TR?= NV\YVJFiOiCq NEH6SlVmdmijbnPld{BXSjFvaX7keYNm\CCIT2jPN4EhfHKjboPjdolxfGmxbnHsJIFkfGm4aYT5 NWfueW56OjR{NEe5NFk>
TE4 MXvGeY5kfGmxbjDBd5NigQ>? M3:yO|IxNzVyL{GwNEDPxE1? MlzIOFghcA>? M2nVR2ROW09? Mly5bY5pcWKrdIOgdE1GemtiYX7kJJdwenSvYX7ubY4h\G:5boLl[5Vt[XSnZDDwMWFsfCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MUeyOFI1PDB{Mx?=
TE1 NGnrbmlHfW6ldHnvckBCe3OjeR?= MnnmNlAwPTBxMUCwJO69VQ>? NILjZ5M1QCCq Mn;oSG1UVw>? M2L4WolvcGmkaYTzJJAuTXKtIHHu[EB4d3K2bXHucolvKGSxd37y[Yd2dGG2ZXSgdE1Cc3RiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MlXJNlQzPDRyMkO=
KYSE30 MVLGeY5kfGmxbjDBd5NigQ>? Mlz3NlAwPTBxMUCwJO69VQ>? Ml\vOFghcA>? MVjEUXNQ NHLFenpqdmirYnn0d{BxNUW{azDhcoQhf2:{dH3hco5qdiCmb4fudoVofWyjdHXkJJAuSWu2IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NGjEWGwzPDJ2NECyNy=>
TE1 MnL4SpVv[3Srb36gRZN{[Xl? NWeweVk{PTBizszN MVW0PEBp NX2xS2VuTE2VTx?= Mk\ReZBz\We3bHH0[ZMhfGinIHX4dJJme3Orb36gc4YhUEyDIHPsZZN{KEl? MonzNlQzPDRyMkO=
TE3 NFvSeJlHfW6ldHnvckBCe3OjeR?= NUS0RW5EPTBizszN NGr5Xos1QCCq MWrEUXNQ NHTLVoF2eHKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCKTFGgZ4xie3NiSR?= NVXrWmFqOjR{NESwNlM>
TE4 MXvGeY5kfGmxbjDBd5NigQ>? NU[zPHRWPTBizszN MmjrOFghcA>? M{TL[GROW09? MoXneZBz\We3bHH0[ZMhfGinIHX4dJJme3Orb36gc4YhUEyDIHPsZZN{KEl? M1LVWVI1OjR2MEKz
TE5 MmnWSpVv[3Srb36gRZN{[Xl? NWrpeJhFPTBizszN NXj2T5lTPDhiaB?= MXvEUXNQ MUL1dJJm\3WuYYTld{B1cGViZYjwdoV{e2mxbjDv[kBJVEFiY3zhd5MhUQ>? MmXSNlQzPDRyMkO=
KYSE30 Mn;DSpVv[3Srb36gRZN{[Xl? NYDtW|cxPTBizszN NHKzOGo1QCCq M4LseWROW09? NIDtPHV2eHKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCKTFGgZ4xie3NiSR?= Mn60NlQzPDRyMkO=
MKN7 MVLGeY5kfGmxbjDBd5NigQ>? MV61NEDPxE1? MW[0PEBp MWXEUXNQ MVvpcoNz\WG|ZYOg[ZhxemW|c3nvckBw\iCKTFGtRVAzKG:{IFjMRU1COjRibX;s[YN2dGW| M{DuV|I1OjR2MEKz
OE19 NX:5V5pwTnWwY4Tpc44hSXO|YYm= MYC1NEDPxE1? NX\HXHJHPDhiaB?= NVLQWJZITE2VTx?= MVXpcoNz\WG|ZYOg[ZhxemW|c3nvckBw\iCKTFGtRVAzKG:{IFjMRU1COjRibX;s[YN2dGW| MlPLNlQzPDRyMkO=
KATOIII  NFfwcZZHfW6ldHnvckBCe3OjeR?= M{foNlUxKM7:TR?= NHq5V2c1QCCq MnX4SG1UVw>? MmfzbY5kemWjc3XzJIV5eHKnc4Ppc44hd2ZiSFzBMWExOiCxcjDIUGEuSTJ2IH3vcIVkfWyncx?= NWfWeZhXOjR{NESwNlM>
NCI-N87  NXTYXJE{TnWwY4Tpc44hSXO|YYm= NH\qb242OCEQvF2= NX7sdVBuPDhiaB?= M3TNVWROW09? M2XveYlv[3KnYYPld{BmgHC{ZYPzbY9vKG:oIFjMRU1CODJib4KgTGxCNUF{NDDtc4xm[3WuZYO= MUmyOFI1PDB{Mx?=
NUGC3 MXfGeY5kfGmxbjDBd5NigQ>? M3;STVUxKM7:TR?= NXHSR5JWPDhiaB?= M4nNNGROW09? NXLqPZZIcW6lcnXhd4V{KGW6cILld5Nqd25ib3[gTGxCNUFyMjDvdkBJVEFvQUK0JI1wdGWldXzldy=> MUCyOFI1PDB{Mx?=
NUGC2 M2XlemZ2dmO2aX;uJGF{e2G7 MX61NEDPxE1? Moj5OFghcA>? MkC0SG1UVw>? NYrsVJF7cW6lcnXhd4V{KGW6cILld5Nqd25ib3[gTGxCNUFyMjDvdkBJVEFvQUK0JI1wdGWldXzldy=> M4\GclI1OjR2MEKz
SGC-7901  NYXrPXZCSXCxcITvd4l{KEG|c3H5 MUmyNEDPxE1? MUeyOEBp Mmj0bY5pcWKrdIOgR3AudWWmaXH0[YQh[XCxcITvd4l{ NHnlOGIzPDJ2MUO1NS=>
MG-63 M3XNSmZ2dmO2aX;uJGF{e2G7 MUOyNEDPxE1? NF\qWWwxNjViaB?= MUDicI9kc3NidHjlJGNJNWmwZIXj[YQheGixc4Doc5J6dGG2ZXSgSWxMOSCycn;0[YlvKGW6cILld5Nqd25? NVPuU2VoOjR{M{m2OFA>
ARPE-19 NE[1NXJHfW6ldHnvckBCe3OjeR?= NGDHbmEzOCEQvF2= NHjReYYxNjViaB?= MWnpcohq[mm2czDBdIVtcW5vaX7keYNm\CCyaH;zdIhwenmuYYTpc44hd2ZiRYLrJIFv\CCDa4S= M4Pse|I1OjJ5OUG4
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MCF-7 NX:wUZdKTnWwY4Tpc44hSXO|YYm= MYKyNEDPxE1? M4XC[VEhcA>? Mn;DZYJwdGm|aHXzJIV5eHKnc4Ppc44hd2ZicHjvd5Bpd3K7bHH0[YQhTVKNIHPvMZRz\WG2bXXueEB4cXSqIHPvcop2\2G2ZR?= MV[yOFIyPjJ6OR?=
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HT-29 MoXkSpVv[3Srb36gRZN{[Xl? MVWyNOKh|ryP NHTs[2k1QCCq MUjy[YR2[2W|IITo[UBDVkmSMzDlfJBz\XO|aX;uJJBz\S22cnXheIVlKHerdHigOU1igmFvZFO= M3LCZ|I1OjFzNUix
7402 NGfoOolCeG:ydH;zbZMhSXO|YYm= MnG3N|Ah|ryP NGDhWHQ2KGR? M{PyXYRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44> MnX5NlQzOTF{NUO=
7721 M{ftZmFxd3C2b4Ppd{BCe3OjeR?= M4W1blMxKM7:TR?= MojBOUBl NEX6ZpZl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9v Mn\BNlQzOTF{NUO=
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SMMC7721 MlrQSpVv[3Srb36gRZN{[Xl? NV;TVoZoOjVxNUCg{txO NFTyWlczPCCq M1XJU5N2eHC{ZYPz[ZMhfGinIHX4dJJme3Orb36gc4YheC2Da4Sgc5IheC2HUluxM|LDqA>? M3Pqd|I1OTZ6MEW2
MCF-7 MkLYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mkj5NVAh|ryP M{PtVFQ5cA>? NEjGZmJFVVOR M17ibJJmfmW{c3XzJGJPTi2rbnT1Z4VlKGOnbHygZ5lkdGViYYLy[ZN1 MWiyOFE3OzRyNB?=
Caco-2 MX3GeY5kfGmxbjDBd5NigQ>? NVL3XZlyPTEEoN88US=> NFS3To01QGh? M2HETWROW09? MYrlcohidmOnczD0bIUhdVKQQTDs[ZZmdHNib3dCpHNEVk5zQTzGXHlFOy{EoFzDWEzDqEyRWD|CpGhKTjODLNMgXmcyPi{EoGDESVZCyqCjbnVCpGxISUyVMUdCpIdmdmW|wrDjc{11emWjdHXkJJdqfGhiRHX4 MkHKNlQyPjF4OUW=
HAECs MV7GeY5kfGmxbjDBd5NigQ>? MmH1NVAh|ryP NVrleJhNOSCq MnPTxsBifHSnboXheIV{KFSQRj5OtU1{fGmvdXzheIVlKEmFQV2tNUBidmRiVlPBUU0yKGW6cILld5Nqd25? M1LSe|I1OTN2NkW3
Ca9-22 NF;DXFBHfW6ldHnvckBCe3OjeR?= MUezJO69VQ>? MlfONUBp M2nrT4Fjd2yrc3jld{B1cGViYXLpcIl1gSCxZjDIZnIhfG9iaX7keYNmKEmOLUigdJJw\HWldHnvci=> M3TaTVI1OTJ4NUOy
Ca9-22 NWXlS4FLTnWwY4Tpc44hSXO|YYm= MlnkN{DPxE1? NHzZXVIyNzJiaB?= MnT1doVlfWOnczDIZnIucW6mdXPl[EBCXEZvMjDwbI9{eGixconsZZRqd25? MlvhNlQyOjZ3M{K=
AGS M1vpTGZ2dmO2aX;uJGF{e2G7 MWKxNEDPxE4EoB?= NFXwWmMxNjViaB?= M2r3O4lvcGmkaYTzJJRp\SC3cILl[5Vt[XSrb36gc4YhfGinIFnMMVgh\2WwZR?= M37NXFI1OTB4MU[2
Caco-2  MYPBdI9xfG:|aYOgRZN{[Xl? NFXPUYkyOMLizszN MmG1NlTDqGh? MU\k[YNz\WG|ZYOgZ4VtdCCjcH;weI9{cXNiaX7keYNm\CCkeTC1MWZW NEnUfnkzPDB7NUi2Ny=>
HCT-8 NUHveIxTSXCxcITvd4l{KEG|c3H5 MoXlNVDDqM7:TR?= MVKyOOKhcA>? MlvJ[IVkemWjc3XzJINmdGxiYYDvdJRwe2m|IHnu[JVk\WRiYomgOU1HXQ>? MUSyOFA6PTh4Mx?=
A549 MmraSpVv[3Srb36gRZN{[Xl? MlryOVDDqM7:TR?= M4qxdVIhcA>? M{HFW4Jtd2OtczDFVmsheGixc4Doc5J6dGG2aX;uJI1m\GmjdHXkJIJ6KDFuMj3OVS=> MontNlQxPjd5Mke=
HPMC NIn5eGNHfW6ldHnvckBCe3OjeR?= NIexO3YyOMLizszN MYO0PEBp Mor6doV3\XK|ZYOgeIhmKGOqYX7n[ZMhcW5iY3XscEBud3KyaH;sc4d6KGmwZIXj[YQh[nliSFfQSHM> NHXTRYkzPDB2MkizPC=>
HPMC Mni3RZBweHSxc3nzJGF{e2G7 Mk\ENVDDqM7:TR?= NEjTPZgzPMLiaB?= MmfLdoV3\XK|ZYOg[IVkemWjc3WgbY4h[2WubDD2bYFjcWyrdImgbY5lfWOnZDDifUBJT1CGUx?= NGXVXW8zPDB2MkizPC=>
MGC803  MUHBdI9xfG:|aYOgRZN{[Xl? NIT5PWszOMLizszN NX7xTnNxOSCq NWnzNIJVcW6qaXLpeJMh[XCxcITvd4l{KGmwZIXj[YQh[nliSV\OMe6yyqCjbnSgOgKBui2GRmXS NH7FfXkzPDB{N{e1NC=>
SGC7901 MX7BdI9xfG:|aYOgRZN{[Xl? MonsNlDDqM7:TR?= NF\wcnUyKGh? M1voVYlvcGmkaYTzJIFxd3C2b4Ppd{BqdmS3Y3XkJIJ6KEmITj5OteKh[W6mIEZihNIuTE[XUh?= M3TVW|I1ODJ5N{Ww
COLO205 NV;hO3hMSXCxcITvd4l{KEG|c3H5 MkTuNVAwOjBxNECg{txO M3PYUlI1KGh? MkXrbY5lfWOnczDEUmEhdGGmZHXyJIZwem2jdHnvci=> MUmyOFAyQTFyOB?=
G292  NYr6S3g{SXCxcITvd4l{KEG|c3H5 Mn;TN|DDqM7:TR?= MW[yJIg> NWmxOWQyemW|dH;y[ZMh[2Gyc3HpZ4lvNWmwZIXj[YQh[2WubDDk[YF1cA>? M{DwU|I1ODF{OUOw
BxPC-3 MlnuSpVv[3Srb36gRZN{[Xl? MnTYNVAh|ryPwrC= NHv0bWU3KGh? M1y5dIlv[3KnYYPlJI1qWi1zNEOg[ZhxemW|c3nvci=> M2XlSVI{QTd|N{Gw
HPAF-II NIDTNnZHfW6ldHnvckBCe3OjeR?= MnL2NVAh|ryPwrC= NGLVR5g3KGh? NWjhc4dIcW6lcnXhd4UhdWmULUG0N{BmgHC{ZYPzbY9v MX[yN|k4OzdzMB?=
HL-60 Mn;vRZBweHSxc3nzJGF{e2G7 M4LuRlUxyqEQvF2= NHfPR4IyKGh? MknkdoV{[3WnczDCRVE1PSCvZXTpZZRm\CCjcH;weI9{cXN? MVWyN|k1QDd3MR?=
HepG2 MWHGeY5kfGmxbjDBd5NigQ>? NX;QTVZvPDBizszN NE[1S|Q3NzF{IHi= NI\0XIZqdmirYnn0d{B1cGViaX7jdoVie2Vib3[gdE1GWktzIHHu[EBxNWNvSoXuJJBzd3SnaX6g[ZhxemW|c3nvckBjgSCSTB?= NXnQfm52OjN7NEK4OVE>
HUVECs M2jQ[2Z2dmO2aX;uJGF{e2G7 NHrNNHIzPSEQvF2= MVWxJIg> NIjUUm1qdmO{ZXHz[UBPTi4QulKgdFY2KG63Y3zlZZIhfHKjboPsc4NifGmxbh?= M3T5WVI{QTBzMEC4
LNCaP  MYTGeY5kfGmxbjDBd5NigQ>? MYSxNEDPxE4EoB?= NFrnTpgyKGh? NUfzWpVP\GWlcnXhd4V{KHSqZTDFS2YhfXC{ZXf1cIF1\WRicD3ZRk0y MYWyN|g{QDNzOB?=
HL60  MX3GeY5kfGmxbjDBd5NigQ>? NUflfHJIOjEEoN88US=> MXm3NkBp M3T1SmROW09? NGTVVVNqdmirYnn0d{Bl[XOjdHnubYIucW6mdXPl[EBETDFzYjDlfJBz\XO|aX;u NGjMXFUzOzh{NUW4OS=>
NB4  NF3xRnlHfW6ldHnvckBCe3OjeR?= MVqxNEDPxE4EoB?= MnvyO|IhcA>? MYXEUXNQ Ml31bY5pcWKrdIOg[IF{[XSrbnniMYlv\HWlZXSgR2QyOWJiZYjwdoV{e2mxbh?= MVqyN|gzPTV6NR?=
EPOR/CR3 NXHpUIRQTnWwY4Tpc44hSXO|YYm= NHXBN4g2OMLizszN NF3Hb2Q{KGh? M2ftVpJm\HWlZYOgSXBQKGGwZD;vdkBKVC1|LXnu[JVk\WRidHjlJJR6em:|aX7lJJBpd3OyaH;yfYxifGmxbtMg MVuyN|gzODd|MR?=
HUASMCs MoPOSpVv[3Srb36gRZN{[Xl? MVKxNEDPxE4EoB?= NYDobXBnOjRiaB?= NWD6S4ts\GmvaX7pd4hmeyCDbnegTWku[2G3c3XkJHNQS1N|IH3SUmEh[W6mIIDyc5RmcW5iZYjwdoV{e2mxbtMg M3XQZ|I{QDF4NE[4
HUASMCs NUflZVR6TnWwY4Tpc44hSXO|YYm= NFHQR|gyOCEQvF5CpC=> MXSyOEBp NIi4RXdqdmirYnn0d{BCdmdiSVmtbY5lfWOnZDDFVmsyNzJicHjvd5Bpd3K7bHH0bY9vKGyndnXs M1[zXFI{QDF4NE[4
SGC7901 NHm0cJlHfW6ldHnvckBCe3OjeR?= M2noS|ExKM7:TdMg MWeyOEBp MonjbY5pcWKrdIOgeIhmKGW6cILld5Nqd25ib3[gdIhwe3Cqb4L5cIF1\WRiRWLLNU8z MVWyN|c6OjV6OB?=
MKN45 MXzGeY5kfGmxbjDBd5NigQ>? NWXifGlkOTBizszNxsA> Mme3NlQhcA>? NGTWNZRqdmirYnn0d{B1cGViZYjwdoV{e2mxbjDv[kBxcG:|cHjvdplt[XSnZDDFVmsyNzJ? MYiyN|c6OjV6OB?=
SGC7901 M3\5Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXrRnJpOTBizszNxsA> M2G5SFI1NzR6L{eyJIg> NV7McnFycW6qaXLpeJMh[2WubDDndo94fGhiY3:teJJm[XSnZDD3bZRpKESDUGS= MYqyN|c6OjV6OB?=
MKN45 NWPCdoxTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX[xNEDPxE4EoB?= MofWNlQwPDhxN{KgbC=> MXvpcohq[mm2czDj[YxtKGe{b4f0bEBkdy22cnXheIVlKHerdHigSGFRXA>? NWO2WItvOjN5OUK1PFg>
SGC7901 MmrWRZBweHSxc3nzJGF{e2G7 NVr6d4E2OTBizszNxsA> MYSyOEBp MVTpcoNz\WG|ZYOgeIhmKESDUGStbY5lfWOnZDDj[YxtKGGyb4D0c5Nqew>? MonaNlM4QTJ3OEi=
MKN45 NYLxNJNOSXCxcITvd4l{KEG|c3H5 M{HX[VExKM7:TdMg MknVNlQhcA>? NVza[JplcW6lcnXhd4V{KHSqZTDERXBVNWmwZIXj[YQh[2WubDDhdI9xfG:|aYO= MkDqNlM4QTJ3OEi=
BxPC-3 cells MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX2yNOKh|ryP MonPNE42KGh? NH3JbmNqdmirYnn0d{BXTUeILVGtdoVofWyjdHXkJGhWXkWFIHfyc5d1cCCjbnSgeJVj\SCob4LtZZRqd25iaX7keYNm\CCkeTDQRXIuOiCDUB?= NVPwW21VOjN5NkSwOFY>
NB4  NXrKNJpOSXCxcITvd4l{KEG|c3H5 NHK3d3YyOC9{MD:2NEDPxE1? NFq0O5kyNjViaB?= MWTEUXNQ MlPi[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHPvMZRz\WG2ZXSge4l1cCCSYXPsbZRigGWu NGT3NGgzOzd|NUW0NS=>
HepG2  MXnGeY5kfGmxbjDBd5NigQ>? M2L3eVIxyqEQvF2= M1HHWVI1KGh? MYTpcohq[mm2czD0bIUhUE9vMTDwdo91\WmwIHX4dJJme3Orb36gZ48ufHKnYYTl[EB4cXSqIH3leIZwem2rbh?= M2fWOVI{PzB5NkC5
HUVECs NWK5OmhISXCxcITvd4l{KEG|c3H5 NEW4cZYzNzRizszN MlzPNlQwPDhiaB?= NVW3dWxycW6mdXPld{Bk\WyuIHTlZZRp NVjETIx5OjN5MEe1NlA>
KG-1  NX\tRWR[SXCxcITvd4l{KEG|c3H5 NHficpczOMLizszN MVmxNkBp NVnLfIxS\W6qYX7j[ZMh[2WubDDhdI9xfG:|aYOgbY5lfWOnZDDifUBUOQ>? MUOyN|cxPjZ7MR?=
AML 1# NF3JOXJCeG:ydH;zbZMhSXO|YYm= MUmyNOKh|ryP M3PYSlEzKGh? NHvDUFNmdmijbnPld{Bk\WyuIHHwc5B1d3OrczDpcoR2[2WmIHL5JHMy MUGyN|cxPjZ7MR?=
A2780  MlHMSpVv[3Srb36gRZN{[Xl? NIDwem0zOMLizszN M3LablEhcA>? NYjYO4R2[myxY3vzJGRVS0RvaX7keYNm\CCGUkWg[ZhxemW|c3nvci=> MWWyN|Y6Pjh4Mh?=

... 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 individually and in order:
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
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
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:

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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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Dilution Calculator

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

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Molecular Weight Calculator

Molecular Weight Calculator

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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