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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In DMSO USD 134 In stock
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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, 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 MkjqSpVv[3Srb36gRZN{[Xl? MnnJNlUh|ryP M3;mT|EhcA>? NX7kfndW[my3boTzJJRp\SCEW3HdVE1qdmS3Y3XkJIlv[3KnYYPlJIlvKHCqb4PwbI8uS2itMTDhcoQheGixc4Doc{1GWktiZYjwdoV{e2mxbh?= MoXaNlU4PjlzOEG=
MCF-7  NWraSI5zTnWwY4Tpc44hSXO|YYm= M1TySVExKM7:TR?= NVSzTVl3OSCq MX;pcohq[mm2czDJUE0yQC2nbnjhcoNm\CClZXzsJI1q\3KjdHnvci=> NETje4EzPTd{N{CxNS=>
HepG2  MX7GeY5kfGmxbjDBd5NigQ>? NGfWbXQyOCEQvF2= M2PjU|UhcA>? MUficI9kc3NicHjvd5Bpd3K7bHH0[YQhVUGSS4OgbY5lfWOnZDDifUBmgG:pZX7veZMhXEeILd8yNS=> NVjnZ4M2OjV3NkC0PFg>
HepG2  MkDNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7Yb5QzOCEQvF2= NH70eG4zPCCq NEH6OnR{fXCycnXzd4V{KFSJRj5OtlEucW6mdXPl[EBk\WyuIIDyc4xq\mW{YYTpc44h[W6mIHnueoF{cW:w M{THTVI2PTZyNEi4
MDA-MB-231 MkLhSpVv[3Srb36gRZN{[Xl? MmmzNlUh|ryP MUGyMVMhcA>? M3HoUYRm[3KnYYPld{BxNUWUS{GvNkBidmRiU{GwNGE1KGW6cILld5Nqd25? MnXsNlU2PTV6N{W=
SW480 MV7GeY5kfGmxbjDBd5NigQ>? MYKyNOKh|ryP NFLJO5QyyqCq NFjSU3Jz\WS3Y3XzJJRp\SCneIDy[ZN{cW:wIH;mJGFVTjNicILveIVqdg>? MXWyOVQ1PzhzNh?=
HCT-15 NEn2d2pHfW6ldHnvckBCe3OjeR?= NUPkR4tZOSCq NX7kVoNy[XS2ZX71ZZRmeyCSR1WyMYlv\HWlZXSgdIhwe3Cqb4L5cIF1cW:wIH;mJGVzc8Li MlTnNlU1OzF2MkW=
HCT-15 NXfqbWxxSXCxcITvd4l{KEG|c3H5 Ml[yNUBp MV;hZo9tcXOqZYOgeIhmKHC{b4TlZ5RqfmViZX\m[YN1eyCxZjDQS2UzyqCjZ3HpcpN1KGO3cnP1cYlvNWmwZIXj[YQh[XCxcITvd4l{ M2rx[lI2PDNzNEK1
786-O Mk[0RZBweHSxc3nzJGF{e2G7 NHLnPYw2OMLizszN NYPDNnJUOjRiaB?= Mo\3dI91\W62aXH0[ZPDqHSqZTDwdo8u[XCxcITveIlkKGWoZnXjeJMhd2ZiTlO= NH;qR2czPDVyOES3Oi=>
A498 MUnBdI9xfG:|aYOgRZN{[Xl? NELGWFU2OMLizszN NXnZSotzOjRiaB?= M3rQUJBwfGWwdHnheIV{yqC2aHWgdJJwNWGyb4D0c5Rq[yCnZn\lZ5R{KG:oIF7D M4jielI1PTB6NEe2
NHBE MWjGeY5kfGmxbjDBd5NigQ>? M37vRVIwOjBizszN MUSyJIg> MV\heJRmdnWjdHXzJGlNNTN|IIP0bY12dGG2ZXSgR3hEVDhxSVytPEB{\WO{ZYTpc44> MlH3NlQ1Pzl3Mk[=
A375 NXrKbHlDS2WubDDJcpZie2mxbjDBd5NigQ>? MWqxNQKBmzJyINM1US=> M1fwXlI1KGh? MWTy[YR2[2W|IH3lcIFvd22jIHPlcIwhcW64YYPpc44> M4\HWVI1PDZ4MEO2
HBMEC M1XJVmZ2dmO2aX;uJGF{e2G7 M2XzWVExKM7:TR?= NEC2XG4yKGh? M{jJW4Jtd2OtczDWSWdHNWmwZIXj[YQhTXCqQUKg[ZhxemW|c3nvci=> NF73WIQzPDR3OEm4Ni=>
HPAEpiCs  M1jJS2Z2dmO2aX;uJGF{e2G7 MXizNEDPxE1? M4[0dVEhcA>? NVy2NlJucW6qaXLpeJMhXE6ILd8xJJN1cW23bHH0[YQheDR{L4C0OEBOSVCNIIDoc5NxcG:{eXzheIlwdg>? MWeyOFQ1OTh5MB?=
BeWo NEfWbHZHfW6ldHnvckBCe3OjeR?= MlP6NVDDqM7:TR?= M2nnd|IhcA>? MXTpcohq[mm2czDFVmsyNzJ? NHXwR5gzPDR|M{i0Oi=>
PC3  MXTBdI9xfG:|aYOgRZN{[Xl? NX[5SZVuPTBizszN NHzhcZExNjViaB?= MoK4bY5pcWKrdIOgUWh[NTR2OT3pcoR2[2WmIHHwc5B1d3Orc9Mg MUiyOFQzPDh6OR?=
HGC-27 MkDmRZBweHSxc3nzJGF{e2G7 NWXIWo9jOSEEtV2= NYjzS|Q3OSCq NULld3dpe3WycILld5NmeyCUQVSwNFEheGy3czDNT{0zOjB4LXnu[JVk\WRiY3XscEB3cWGkaXzpeJkhdG:|cx?= M3zrTFI1PDF4M{S5
MCF-7 Ml\pSpVv[3Srb36gRZN{[Xl? NF;ROXEyOMLizszN MX[xNE8{OCCvaX6= NXrZcmUzemWmdXPld{B1cGViVWTQMYRmeGWwZHXueEBGWkticHjvd5Bpd3K7bHH0bY9v NIO1fpMzPDN7MEixPS=>
HUVECs NWfMOXJMTnWwY4Tpc44hSXO|YYm= NYjJe2V2OTEEoN88US=> MlPhNUBp Ml3abY5pcWKrdIOgeIhmKEiGTDDy[YR2[2WmIFPPXE0zKGW6cILld5Nqd25iYX7kJHBIUS1{IILlcIVie2V? NIn6[4czPDN6NUGwPS=>
HeLa MXLGeY5kfGmxbjDBd5NigQ>? NVrpZ4tkPTBizszN MkmzNE42KGh? NIn3NmdjdG:la4OgWHJZNTFiboXjcIVieiCvaXfyZZRqd25iYX7kJHRZVkmSIHTve44uemWpdXzheIlwdg>? M2Trc|I1Ozd4OEK3
HL-60  NHTse3JHfW6ldHnvckBCe3OjeR?= M4HsXVExNzJyIN88US=> Mk\CNUBp NVzLWolMcW6qaXLpeJMhfGinwrDOMkBkcGmwZX7zbZNmgHS{YXP0xsBqdmS3Y3XkJIRq\m[ncnXueIlifGmxbjDpcpRwKGe{YX71cI9kgXSncx?= NVrUWHlmOjR|NUewNlA>
HL-60 M1XOcWZ2dmO2aX;uJGF{e2G7 MmjpNkDDvU1? NVj3T5RGOTZiaB?= M2S3S2ROW09? NWn2[nNQcW6qaXLpeJMhfGinIHHzd49kcWG2aX;uJI9nKHCVNkKxJHJi\i1zIHHu[EBPTkGWY{OsJIFv\CC2aHWgVmEucW6mdXPl[EBxcG:|cHjvdplt[XSrb36gc4YhdnWlbHXhdkBPTkGWY{O= M4r1T|I1OzNyME[4
HEK 293 MU\GeY5kfGmxbjDBd5NigQ>? MVOxNEDPxE1? MlXZOUBp MYLEUXNQ NVrMOJl3cW6qaXLpeJMhX262LXnu[JVk\WRizsKtZ4F1\W6rbj;UR2Y1KGGldHn2bZR6KGGwZDDueYNt\WG{IN8yMYNifGWwaX6gZYNkfW23bHH0bY9v NH\0bmYzPDN{NEO2Oi=>
HEK 293 Ml3HSpVv[3Srb36gRZN{[Xl? NX3GVJprOTBizszN NILGW3o2KGh? MoPJSG1UVw>? MmO2d5VxeHKnc4Pld{B1cGViQ2LUJIFkfGm4aYT5 MYWyOFMzPDN4Nh?=
SW480 NIXHc3JHfW6ldHnvckBCe3OjeR?= MmDJNVAh|ryP MnPnNlAhcA>? M3SyU2ROW09? NIr5WYl{fXCycnXzd4V{KHSqZTDDVnQh[WO2aY\peJk> NYjzZnRwOjR|MkSzOlY>
HCSMCs M3nVZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUCxNEDPxE1? MVmyOEBp NUXHOo0z[myxY3vzJGZCSlB2LXnu[JVk\WRiSFPBV21EKHC{b3zp[oVz[XSrb36= NVXI[WxrOjR|MUKzPFE>
PANC-1 MnLkSpVv[3Srb36gRZN{[Xl? Mm[zNlAh|ryP NXj2W3hiPDhiaB?= MUDpcohq[mm2czD0bIUh\XiycnXzd4lwdiCxZjFOmFZFKGmwIILld5BwdnOnIITvJJRp\SCSUFHS{tTDqGGpb37pd5TDqA>? M{LLR|I1Ojl2MUOz
A549 NILkUpNHfW6ldHnvckBCe3OjeR?= NGG2XFM{OCEQvF2= NIX2NoYxNjViaB?= NFmwPIJFVVOR Ml7pbY5pcWKrdIOgeIhmKHSqcn;tZolvNWmwZIXj[YQhUUxvOD;DXGNNQC2OdXOgZYN1cX[rdIm= MnrjNlQzPzd4OU[=
A549 NUCzSGJHTnWwY4Tpc44hSXO|YYm= Mn[yN|Ah|ryP NVTCTW44OC53IHi= NX6zZmlOTE2VTx?= M3TxNIlvcGmkaYTzJJRpem:vYnnuMYlv\HWlZXSgR{9GSlEQsjDUbJIzOzYEoIDoc5NxcG:{eXzheIlwdg>? MUSyOFI4PzZ7Nh?=
MC-3 MlvjRZBweHSxc3nzJGF{e2G7 M2rpd|ExKM7:TR?= MlnsNlQhcA>? M3PxUZBwfGWwdHnheIVlKE2HU1OtbY5lfWOnZDDhdI9xfG:|aYOgbY4hKGOnbHzz NIm4T5IzPDJ5MEWyNy=>
Raji  M1\LNWZ2dmO2aX;uJGF{e2G7 MYCxNEDPxE1? MVuxJIg> MlHRZoxw[2u|IHjzRmFHTiCrbnT1Z4VlKEW{a{GvNkBxcG:|cHjvdplt[XSrb36= MYGyOFI3QTZ|MB?=
Raji  NYfxVY93T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrJNVAh|ryP M3vvclEhcA>? MoXZbY5pcWKrdIOgeIhmKGKjc3HsJI9zKGi|QlHGSk1{fGmvdXzheIVlKGOnbHygdJJwdGmoZYLheIlwdiCjbnSgeoli[mmuaYT5 NEPNeXgzPDJ4OU[zNC=>
HT29 M{CxfGZ2dmO2aX;uJGF{e2G7 Mlu5NVAh|ryP M3;H[lIhcA>? NIfuSnRqdmirYnn0d{Bw\iCMQVuyMEBGWktzL{KgZY5lKFOWQWSzJJBpd3OyaH;yfYxifGmxbh?= M1;HdVI1OjZ3Mkmz
HepG2 M1vxW2Fxd3C2b4Ppd{BCe3OjeR?= MmjHNlAh|ryP NILJNnkzPCCq M1yyeYlvcGmkaYTzJGVTUzFxMjDwbI9{eGixconsZZRqd25iYX7kJIVvcGGwY3XzJHZDOS2rbnT1Z4VlKGGyb4D0c5Nqew>? MWWyOFI1PzlyOR?=
HepG2 NFK2R|ZHfW6ldHnvckBCe3OjeR?= MVqyNEDPxE1? NYHKdm1VOiCq NFK0c|ZmdmijbnPld{BXSjFvaX7keYNm\CCIT2jPN4EhfHKjboPjdolxfGmxbnHsJIFkfGm4aYT5 MkfWNlQzPDd7MEm=
TE4 MmLGSpVv[3Srb36gRZN{[Xl? NVrBVI9wOjBxNUCvNVAxKM7:TR?= M4Gz[FQ5KGh? MVTEUXNQ MWTpcohq[mm2czDwMWVzcyCjbnSge49zfG2jbn7pckBld3ewcnXneYxifGWmIICtRYt1KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NGm5dlAzPDJ2NECyNy=>
TE1 MVvGeY5kfGmxbjDBd5NigQ>? MWSyNE82OC9zMECg{txO NUT1SnBPPDhiaB?= MmW0SG1UVw>? NIjuXGJqdmirYnn0d{BxNUW{azDhcoQhf2:{dH3hco5qdiCmb4fudoVofWyjdHXkJJAuSWu2IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MljJNlQzPDRyMkO=
KYSE30 MkT0SpVv[3Srb36gRZN{[Xl? NHHhUnYzOC93MD:xNFAh|ryP Ml;5OFghcA>? NX7N[XpWTE2VTx?= M3:wcolvcGmkaYTzJJAuTXKtIHHu[EB4d3K2bXHucolvKGSxd37y[Yd2dGG2ZXSgdE1Cc3RiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NXL3WmpwOjR{NESwNlM>
TE1 M3m0VmZ2dmO2aX;uJGF{e2G7 MWC1NEDPxE1? NIGwVmE1QCCq M{npcmROW09? MYj1dJJm\3WuYYTld{B1cGViZYjwdoV{e2mxbjDv[kBJVEFiY3zhd5MhUQ>? M3\UUFI1OjR2MEKz
TE3 M1nMSmZ2dmO2aX;uJGF{e2G7 NEP5UYQ2OCEQvF2= NXnle|Z3PDhiaB?= NX:zZXQyTE2VTx?= M{LLO5VxemWpdXzheIV{KHSqZTDlfJBz\XO|aX;uJI9nKEiOQTDjcIF{eyCL MXGyOFI1PDB{Mx?=
TE4 M1T2VWZ2dmO2aX;uJGF{e2G7 NIXiPYw2OCEQvF2= MWe0PEBp MoTVSG1UVw>? Mlz2eZBz\We3bHH0[ZMhfGinIHX4dJJme3Orb36gc4YhUEyDIHPsZZN{KEl? NWTYUmU2OjR{NESwNlM>
TE5 MUXGeY5kfGmxbjDBd5NigQ>? MVK1NEDPxE1? M2m1elQ5KGh? M1z5V2ROW09? MWf1dJJm\3WuYYTld{B1cGViZYjwdoV{e2mxbjDv[kBJVEFiY3zhd5MhUQ>? NGHn[4EzPDJ2NECyNy=>
KYSE30 NYfxS2hFTnWwY4Tpc44hSXO|YYm= MkPSOVAh|ryP NXfWT3dFPDhiaB?= NYLlWW8yTE2VTx?= M2TzO5VxemWpdXzheIV{KHSqZTDlfJBz\XO|aX;uJI9nKEiOQTDjcIF{eyCL M1n6T|I1OjR2MEKz
MKN7 NHPhfVFHfW6ldHnvckBCe3OjeR?= M2TxTVUxKM7:TR?= MkDsOFghcA>? NWrRW2JmTE2VTx?= NVv2PZZZcW6lcnXhd4V{KGW6cILld5Nqd25ib3[gTGxCNUFyMjDvdkBJVEFvQUK0JI1wdGWldXzldy=> NGrYUHkzPDJ2NECyNy=>
OE19 MUnGeY5kfGmxbjDBd5NigQ>? Moj3OVAh|ryP MVO0PEBp MX\EUXNQ NXXFZXE4cW6lcnXhd4V{KGW6cILld5Nqd25ib3[gTGxCNUFyMjDvdkBJVEFvQUK0JI1wdGWldXzldy=> M4C0S|I1OjR2MEKz
KATOIII  NFPMSoZHfW6ldHnvckBCe3OjeR?= MVy1NEDPxE1? MX20PEBp NF;6U3hFVVOR MYDpcoNz\WG|ZYOg[ZhxemW|c3nvckBw\iCKTFGtRVAzKG:{IFjMRU1COjRibX;s[YN2dGW| M2nZUlI1OjR2MEKz
NCI-N87  NIXyUWxHfW6ldHnvckBCe3OjeR?= MX:1NEDPxE1? NYS3TIZ3PDhiaB?= M1foVGROW09? MWDpcoNz\WG|ZYOg[ZhxemW|c3nvckBw\iCKTFGtRVAzKG:{IFjMRU1COjRibX;s[YN2dGW| Mn2zNlQzPDRyMkO=
NUGC3 MlewSpVv[3Srb36gRZN{[Xl? MXu1NEDPxE1? MWi0PEBp MofiSG1UVw>? M2i1SIlv[3KnYYPld{BmgHC{ZYPzbY9vKG:oIFjMRU1CODJib4KgTGxCNUF{NDDtc4xm[3WuZYO= MViyOFI1PDB{Mx?=
NUGC2 M1zPcmZ2dmO2aX;uJGF{e2G7 M2r5bVUxKM7:TR?= MlnlOFghcA>? MnvGSG1UVw>? MljHbY5kemWjc3XzJIV5eHKnc4Ppc44hd2ZiSFzBMWExOiCxcjDIUGEuSTJ2IH3vcIVkfWyncx?= NETQb2szPDJ2NECyNy=>
SGC-7901  MXfBdI9xfG:|aYOgRZN{[Xl? NUnEPIZ7OjBizszN MWWyOEBp M1j3PYlvcGmkaYTzJGNRNW2nZHnheIVlKGGyb4D0c5Nqew>? NF;hO|gzPDJ2MUO1NS=>
MG-63 MkXQSpVv[3Srb36gRZN{[Xl? MVqyNEDPxE1? MoTZNE42KGh? MX7icI9kc3NidHjlJGNJNWmwZIXj[YQheGixc4Doc5J6dGG2ZXSgSWxMOSCycn;0[YlvKGW6cILld5Nqd25? MkXFNlQzOzl4NEC=
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Caco-2 M4TSO2Z2dmO2aX;uJGF{e2G7 NU\ONngxPTEEoN88US=> MWi0PIg> MnL5SG1UVw>? NI\rTFhmdmijbnPld{B1cGVibWLORUBt\X[nbIOgc4bDqFOFTl6xRUxHYFmGMz|CpGxEXC{EoFzPXEzDqEiLRkPBMOKhYkdzNj|CpHBFTT[DwrDhcoTDqEyJQVzTNVbDqGenbnXzxsBkdy22cnXheIVlKHerdHigSIV5 M4\lN|I1OTZzNkm1
HAECs MWXGeY5kfGmxbjDBd5NigQ>? Ml\jNVAh|ryP NInESXYyKGh? NH\FcHPDqGG2dHXueYF1\XNiVF7GMe6yNXO2aX31cIF1\WRiSVPBUU0yKGGwZDDWR2FONTFiZYjwdoV{e2mxbh?= MUCyOFE{PDZ3Nx?=
Ca9-22 Mn;6SpVv[3Srb36gRZN{[Xl? NIfrT3I{KM7:TR?= MYKxJIg> M2XGNIFjd2yrc3jld{B1cGViYXLpcIl1gSCxZjDIZnIhfG9iaX7keYNmKEmOLUigdJJw\HWldHnvci=> NH25cXIzPDF{NkWzNi=>
Ca9-22 NIDKOXVHfW6ldHnvckBCe3OjeR?= MmDnN{DPxE1? NUH5fZpsOS9{IHi= M3XaZ5Jm\HWlZYOgTIJTNWmwZIXj[YQhSVSILUKgdIhwe3Cqb4L5cIF1cW:w MV2yOFEzPjV|Mh?=
AGS NH7DbYpHfW6ldHnvckBCe3OjeR?= MkT1NVAh|ryPwrC= MnjXNE42KGh? MWPpcohq[mm2czD0bIUhfXC{ZXf1cIF1cW:wIH;mJJRp\SCLTD24JIdmdmV? M4rpRVI1OTB4MU[2
Caco-2  MVfBdI9xfG:|aYOgRZN{[Xl? M13YdFExyqEQvF2= M4fkflI1yqCq M{XiNYRm[3KnYYPld{Bk\WyuIHHwc5B1d3OrczDpcoR2[2WmIHL5JFUuTlV? NYnqWGJpOjRyOUW4OlM>
HCT-8 NWXSV2p6SXCxcITvd4l{KEG|c3H5 MWmxNOKh|ryP NUfJPGJFOjUEoHi= MlW4[IVkemWjc3XzJINmdGxiYYDvdJRwe2m|IHnu[JVk\WRiYomgOU1HXQ>? M2HXVFI1ODl3OE[z
A549 MkC1SpVv[3Srb36gRZN{[Xl? NIHMbZE2OMLizszN NHTofJkzKGh? NYjvdnJN[myxY3vzJGVTUyCyaH;zdIhwenmuYYTpc44hdWWmaXH0[YQh[nliMTyyMW5S NIi1NJEzPDB4N{eyOy=>
HPMC NHLT[3RHfW6ldHnvckBCe3OjeR?= NHLYfFAyOMLizszN NFzLfXU1QCCq NEK0U5dz\X[ncoPld{B1cGViY3jhcodmeyCrbjDj[YxtKG2xcoDoc4xw\3liaX7keYNm\CCkeTDIS3BFWw>? MXuyOFA1Ojh|OB?=
HPMC NYDrXIh{SXCxcITvd4l{KEG|c3H5 M4r2cVExyqEQvF2= NE\oUHUzPMLiaB?= NF7aeFBz\X[ncoPld{Bl\WO{ZXHz[UBqdiClZXzsJJZq[WKrbHn0fUBqdmS3Y3XkJIJ6KEiJUFTT MoDSNlQxPDJ6M{i=
MGC803  NHrRboRCeG:ydH;zbZMhSXO|YYm= NYDuOJZ4OjEEoN88US=> MkTPNUBp NF\MXZhqdmirYnn0d{BieG:ydH;zbZMhcW6mdXPl[EBjgSCLRl6t{tHDqGGwZDC15qCzNUSIVWK= M{\FTlI1ODJ5N{Ww
SGC7901 MlT3RZBweHSxc3nzJGF{e2G7 MXyyNOKh|ryP M4jWeVEhcA>? NFT4PJBqdmirYnn0d{BieG:ydH;zbZMhcW6mdXPl[EBjgSCLRl6t{tHDqGGwZDC15qCzNUSIVWK= Mn7qNlQxOjd5NUC=
COLO205 MXHBdI9xfG:|aYOgRZN{[Xl? M{G4SVExNzJyL{SwJO69VQ>? NHvETJAzPCCq NFnKO5pqdmS3Y3XzJGRPSSCuYXTk[ZIh\m:{bXH0bY9v NHP0eIIzPDBzOUGwPC=>
G292  NU\mZVcxSXCxcITvd4l{KEG|c3H5 Mn7sN|DDqM7:TR?= MoDWNkBp M1nHOpJme3SxcnXzJINieHOjaXPpck1qdmS3Y3XkJINmdGxiZHXheIg> NYi2O2VIOjRyMUK5N|A>
BxPC-3 MlzCSpVv[3Srb36gRZN{[Xl? NWe2cYdCOTBizszNxsA> NFHjVVY3KGh? NXvJfXptcW6lcnXhd4UhdWmULUG0N{BmgHC{ZYPzbY9v M{i5T|I{QTd|N{Gw
HPAF-II NHX1SpdHfW6ldHnvckBCe3OjeR?= NVfMWoJGOTBizszNxsA> NIfrRW03KGh? MojjbY5kemWjc3WgcYlTNTF2MzDlfJBz\XO|aX;u M2XJPVI{QTd|N{Gw
HL-60 NEjXRlJCeG:ydH;zbZMhSXO|YYm= MnzGOVDDqM7:TR?= NXTMbpU{OSCq NIPkbGJz\XOldXXzJGJCOTR3IH3l[IlifGWmIHHwc5B1d3Orcx?= M3O3TlI{QTR6N{Wx
HepG2 MUHGeY5kfGmxbjDBd5NigQ>? M{LLRlQxKM7:TR?= M4DyNlYwOTJiaB?= Mn\lbY5pcWKrdIOgeIhmKGmwY4LlZZNmKG:oIICtSXJMOSCjbnSgdE1kNUq3bjDwdo91\WmwIHX4dJJme3Orb36gZpkhWEx? NYjBTFl[OjN7NEK4OVE>
HUVECs MXfGeY5kfGmxbjDBd5NigQ>? MX2yOUDPxE1? NWfIVm5WOSCq NUj6XYlicW6lcnXhd4UhVkZvzsrCJJA3PSCwdXPs[YFzKHS{YX7zcI9k[XSrb36= MYqyN|kxOTByOB?=
LNCaP  M4HndmZ2dmO2aX;uJGF{e2G7 NH73dWkyOCEQvF5CpC=> Mmm1NUBp NH71NGhl\WO{ZXHz[ZMhfGinIFXHSkB2eHKnZ4XsZZRm\CCyLWnCMVE> MWWyN|g{QDNzOB?=
HL60  M4rxdmZ2dmO2aX;uJGF{e2G7 NYHQZ4p2OjEEoN88US=> M{fGVVczKGh? NE[5VGRFVVOR NVn6R5FncW6qaXLpeJMh\GG|YYTpcoljNWmwZIXj[YQhS0RzMXKg[ZhxemW|c3nvci=> MnrZNlM5OjV3OEW=
NB4  M{LJWWZ2dmO2aX;uJGF{e2G7 M3nkdFExKM7:TdMg M2i2UVczKGh? NWXOfmVyTE2VTx?= NVXyWZg4cW6qaXLpeJMh\GG|YYTpcoljNWmwZIXj[YQhS0RzMXKg[ZhxemW|c3nvci=> M4fPTlI{QDJ3NUi1
EPOR/CR3 NFjTW2RHfW6ldHnvckBCe3OjeR?= M2P6NFUxyqEQvF2= Ml\mN{Bp MoT6doVlfWOnczDFVG8h[W6mL3;yJGlNNTNvaX7keYNm\CC2aHWgeJlzd3OrbnWgdIhwe3Cqb4L5cIF1cW:wwrC= MV[yN|gzODd|MR?=
HUASMCs M1\XZWZ2dmO2aX;uJGF{e2G7 MXGxNEDPxE4EoB?= NFnVNXYzPCCq NF7ifmFlcW2rbnnzbIV{KEGwZzDJTU1k[XW|ZXSgV29EWzNibWLORUBidmRicILveIVqdiCneIDy[ZN{cW:wwrC= MUGyN|gyPjR4OB?=
HUASMCs NYjw[YRkTnWwY4Tpc44hSXO|YYm= NHK3OZIyOCEQvF5CpC=> M4G0flI1KGh? NGjlfIRqdmirYnn0d{BCdmdiSVmtbY5lfWOnZDDFVmsyNzJicHjvd5Bpd3K7bHH0bY9vKGyndnXs NXzMc5NqOjN6MU[0Olg>
SGC7901 MYrGeY5kfGmxbjDBd5NigQ>? NVr3NVVNOTBizszNxsA> NU\FOItuOjRiaB?= MoTPbY5pcWKrdIOgeIhmKGW6cILld5Nqd25ib3[gdIhwe3Cqb4L5cIF1\WRiRWLLNU8z NYDhdFlFOjN5OUK1PFg>
MKN45 MoTPSpVv[3Srb36gRZN{[Xl? NXjMZpRNOTBizszNxsA> MkTPNlQhcA>? M{XqXIlvcGmkaYTzJJRp\SCneIDy[ZN{cW:wIH;mJJBpd3OyaH;yfYxifGWmIFXST|EwOg>? NF3KTG8zOzd7MkW4PC=>
SGC7901 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jJVVExKM7:TdMg NVTKbnl4OjRxNEivO|IhcA>? MYLpcohq[mm2czDj[YxtKGe{b4f0bEBkdy22cnXheIVlKHerdHigSGFRXA>? M1X5U|I{Pzl{NUi4
MKN45 NEHS[HRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LHSVExKM7:TdMg NX3ySlV7OjRxNEivO|IhcA>? M{XXN4lvcGmkaYTzJINmdGxiZ4Lve5RpKGOxLYTy[YF1\WRid3n0bEBFSVCW MYiyN|c6OjV6OB?=
SGC7901 NEL3RmxCeG:ydH;zbZMhSXO|YYm= NUjNdmV2OTBizszNxsA> M3m1blI1KGh? MmD0bY5kemWjc3XzJJRp\SCGQWDUMYlv\HWlZXSgZ4VtdCCjcH;weI9{cXN? MlTUNlM4QTJ3OEi=
MKN45 NUnFVIhVSXCxcITvd4l{KEG|c3H5 NWiwfVFyOTBizszNxsA> MnjwNlQhcA>? NYjnWVRVcW6lcnXhd4V{KHSqZTDERXBVNWmwZIXj[YQh[2WubDDhdI9xfG:|aYO= Mk[xNlM4QTJ3OEi=
BxPC-3 cells M3fUfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUXu[GV7OjEEoN88US=> NHfCTlkxNjViaB?= NGTBZm9qdmirYnn0d{BXTUeILVGtdoVofWyjdHXkJGhWXkWFIHfyc5d1cCCjbnSgeJVj\SCob4LtZZRqd25iaX7keYNm\CCkeTDQRXIuOiCDUB?= MnTiNlM4PjRyNE[=
NB4  NW\scGRySXCxcITvd4l{KEG|c3H5 MnXiNVAwOjBxNkCg{txO MX:xMlUhcA>? MkTzSG1UVw>? Mn36[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHPvMZRz\WG2ZXSge4l1cCCSYXPsbZRigGWu MWOyN|c{PTV2MR?=
HepG2  NW\oUVd7TnWwY4Tpc44hSXO|YYm= NE[3ZXYzOMLizszN MU[yOEBp MkmzbY5pcWKrdIOgeIhmKEiRLUGgdJJwfGWrbjDlfJBz\XO|aX;uJINwNXS{ZXH0[YQhf2m2aDDt[ZRnd3KvaX6= NFjVcZUzOzdyN{[wPS=>
HUVECs MVPBdI9xfG:|aYOgRZN{[Xl? NUnVRXh7Oi92IN88US=> M4\PNVI1NzR6IHi= M1PZb4lv\HWlZYOgZ4VtdCCmZXH0bC=> M3OwRlI{PzB5NUKw
KG-1  MmSxRZBweHSxc3nzJGF{e2G7 NH;uRYkzOMLizszN M17FW|EzKGh? MoLw[Y5p[W6lZYOgZ4VtdCCjcH;weI9{cXNiaX7keYNm\CCkeTDTNS=> NIK3e40zOzdyNk[5NS=>
AML 1# NIjIV3FCeG:ydH;zbZMhSXO|YYm= MXSyNOKh|ryP M1XqSVEzKGh? NFr3TlRmdmijbnPld{Bk\WyuIHHwc5B1d3OrczDpcoR2[2WmIHL5JHMy MWWyN|cxPjZ7MR?=
A2780  M2DhRWZ2dmO2aX;uJGF{e2G7 NEDjRXYzOMLizszN M4HJblEhcA>? M2T1WIJtd2OtczDEWGNFNWmwZIXj[YQhTFJ3IHX4dJJme3Orb36= MWKyN|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 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:

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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

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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