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, 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 Mn7rSpVv[3Srb36gRZN{[Xl? NHTOcW8zPSEQvF2= NHfGO5UyKGh? M2H2NoJtfW62czD0bIUhSlujXWCtbY5lfWOnZDDpcoNz\WG|ZTDpckBxcG:|cHjvMWNpczFiYX7kJJBpd3OyaH:tSXJMKGW6cILld5Nqd25? MWeyOVc3QTF6MR?=
MCF-7  NX3vSnZITnWwY4Tpc44hSXO|YYm= M2nNPVExKM7:TR?= M2nWbVEhcA>? NFv2UXRqdmirYnn0d{BKVC1zOD3lcohidmOnZDDj[YxtKG2rZ4LheIlwdg>? M3zTelI2PzJ5MEGx
HepG2  M1\scmZ2dmO2aX;uJGF{e2G7 M2PDSVExKM7:TR?= MnXaOUBp MlfKZoxw[2u|IIDoc5NxcG:{eXzheIVlKE2DUFvzJIlv\HWlZXSgZpkh\XixZ3Xuc5V{KFSJRj5OtlE> MoXxNlU2PjB2OEi=
HepG2  NVfUPW5vT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3ZUWZmOjBizszN NFnRUJIzPCCq MWrzeZBxemW|c3XzJHRITi4QskGtbY5lfWOnZDDj[YxtKHC{b3zp[oVz[XSrb36gZY5lKGmwdnHzbY9v NYHTRlF2OjV3NkC0PFg>
MDA-MB-231 MWDGeY5kfGmxbjDBd5NigQ>? NFrXfYczPSEQvF2= NVTBblV2Oi1|IHi= MV;k[YNz\WG|ZYOgdE1GWktzL{KgZY5lKFNzMEDBOEBmgHC{ZYPzbY9v NFvMWZkzPTV3NUi3OS=>
SW480 NFzVZVZHfW6ldHnvckBCe3OjeR?= MlnsNlDDqM7:TR?= NVHtXGloOcLiaB?= NFfYSFdz\WS3Y3XzJJRp\SCneIDy[ZN{cW:wIH;mJGFVTjNicILveIVqdg>? MX:yOVQ1PzhzNh?=
HCT-15 MUfGeY5kfGmxbjDBd5NigQ>? MkLpNUBp MX7heJRmdnWjdHXzJHBITTJvaX7keYNm\CCyaH;zdIhwenmuYYTpc44hd2ZiRYLrxsA> MoTZNlU1OzF2MkW=
HCT-15 NXK2VnloSXCxcITvd4l{KEG|c3H5 NGrCeo8yKGh? Ml7DZYJwdGm|aHXzJJRp\SCycn;0[YN1cX[nIHXm[oVkfHNib3[gVGdGOsLiYXfhbY5{fCCldYLjeY1qdi2rbnT1Z4VlKGGyb4D0c5Nqew>? M2f3OlI2PDNzNEK1
786-O M2jpUmFxd3C2b4Ppd{BCe3OjeR?= Moe2OVDDqM7:TR?= NFPI[JQzPCCq MXzwc5RmdnSrYYTld:KhfGinIIDyc{1ieG:ydH;0bYMh\W[oZXP0d{Bw\iCQQx?= NESyS3ozPDVyOES3Oi=>
A498 MXjBdI9xfG:|aYOgRZN{[Xl? NHfYWHc2OMLizszN MX6yOEBp MV7wc5RmdnSrYYTld:KhfGinIIDyc{1ieG:ydH;0bYMh\W[oZXP0d{Bw\iCQQx?= NEHydHEzPDVyOES3Oi=>
NHBE NWW1bXlPTnWwY4Tpc44hSXO|YYm= MUWyM|IxKM7:TR?= M{[zO|IhcA>? MXrheJRmdnWjdHXzJGlNNTN|IIP0bY12dGG2ZXSgR3hEVDhxSVytPEB{\WO{ZYTpc44> MXWyOFQ4QTV{Nh?=
A375 NGHjPJRE\WyuIFnueoF{cW:wIFHzd4F6 MmXzNVDjiJN{MDFCuW0> MnPqNlQhcA>? M2nZSZJm\HWlZYOgcYVt[W6xbXGgZ4VtdCCrbo\hd4lwdg>? M3vPblI1PDZ4MEO2
HBMEC MVnGeY5kfGmxbjDBd5NigQ>? NWPidI85OTBizszN M{\OfVEhcA>? MXHicI9kc3NiVlXHSk1qdmS3Y3XkJGVxcEF{IHX4dJJme3Orb36= NXnlNlByOjR2NUi5PFI>
HPAEpiCs  M3SxeWZ2dmO2aX;uJGF{e2G7 NV7OO2w2OzBizszN NXjx[Gw5OSCq Mlj5bY5pcWKrdIOgWG5HNc7zIIP0bY12dGG2ZXSgdFQzN3B2NDDNRXBMKHCqb4PwbI9zgWyjdHnvci=> M3rvU|I1PDRzOEew
BeWo M1jtVmZ2dmO2aX;uJGF{e2G7 NXTFWXNIOTEEoN88US=> Mn:0NkBp MnjEbY5pcWKrdIOgSXJMOS9{ MVGyOFQ{Ozh2Nh?=
PC3  M{X3UmFxd3C2b4Ppd{BCe3OjeR?= MXS1NEDPxE1? NYr0VZROOC53IHi= Mom2bY5pcWKrdIOgUWh[NTR2OT3pcoR2[2WmIHHwc5B1d3Orc9Mg M3TEU|I1PDJ2OEi5
HGC-27 M132[GFxd3C2b4Ppd{BCe3OjeR?= M2LUdVEhyrWP MYexJIg> NUfGNJBke3WycILld5NmeyCUQVSwNFEheGy3czDNT{0zOjB4LXnu[JVk\WRiY3XscEB3cWGkaXzpeJkhdG:|cx?= NX\u[G1nOjR2MU[zOFk>
MCF-7 NGqwTXNHfW6ldHnvckBCe3OjeR?= MVmxNOKh|ryP M4TJNFExNzNyIH3pci=> NYi4Tpk2emWmdXPld{B1cGViVWTQMYRmeGWwZHXueEBGWkticHjvd5Bpd3K7bHH0bY9v Ml:wNlQ{QTB6MUm=
HUVECs M{SwUWZ2dmO2aX;uJGF{e2G7 MYWxNOKh|ryP NVr1XGR{OSCq Ml\ubY5pcWKrdIOgeIhmKEiGTDDy[YR2[2WmIFPPXE0zKGW6cILld5Nqd25iYX7kJHBIUS1{IILlcIVie2V? NVfFXHIxOjR|OEWxNFk>
HeLa MlLNSpVv[3Srb36gRZN{[Xl? NHmxPGE2OCEQvF2= NGnrR5IxNjViaB?= Mn\tZoxw[2u|IGTSXE0yKG63Y3zlZZIhdWmpcnH0bY9vKGGwZDDUXG5KWCCmb4fuMZJm\3WuYYTpc44> M4C4eVI1Ozd4OEK3
HL-60  NU\ZfpJ2TnWwY4Tpc44hSXO|YYm= MoLINVAwOjBizszN Ml;PNUBp NGnnWYNqdmirYnn0d{B1cGYEoF6uJINpcW6nboPpd4V5fHKjY4VCpIlv\HWlZXSg[Iln\mW{ZX70bYF1cW:wIHnueI8h\3KjboXsc4N6fGW| NXTTdVlKOjR|NUewNlA>
HL-60 NWnDdoxrTnWwY4Tpc44hSXO|YYm= NF\RdYMzKML3TR?= NEjTe4UyPiCq M1fx[mROW09? NELUXGpqdmirYnn0d{B1cGViYYPzc4Nq[XSrb36gc4YheFN4MkGgVoFnNTFiYX7kJG5HSVSlMzygZY5lKHSqZTDSRU1qdmS3Y3XkJJBpd3OyaH;yfYxifGmxbjDv[kBvfWOuZXHyJG5HSVSlMx?= NYT4WIJtOjR|M{CwOlg>
HEK 293 NVjFfmFyTnWwY4Tpc44hSXO|YYm= NH;UOmQyOCEQvF2= M{HoTVUhcA>? MnnXSG1UVw>? Mmq0bY5pcWKrdIOgW451NWmwZIXj[YQh|rJvY3H0[Y5qdi:WQ1[0JIFkfGm4aYT5JIFv\CCwdXPs[YFzKM7{LXPheIVvcW5iYXPjeY12dGG2aX;u M4LGWFI1OzJ2M{[2
HEK 293 NFnZXWlHfW6ldHnvckBCe3OjeR?= NVHOUVZIOTBizszN M4HOO|UhcA>? MoHaSG1UVw>? NXHBcHhqe3WycILld5NmeyC2aHWgR3JVKGGldHn2bZR6 NEfBSYwzPDN{NEO2Oi=>
SW480 M3nDcmZ2dmO2aX;uJGF{e2G7 M{e2T|ExKM7:TR?= NHPySXgzOCCq NHjIcJdFVVOR NYLZXHhSe3WycILld5NmeyC2aHWgR3JVKGGldHn2bZR6 NGCxb|YzPDN{NEO2Oi=>
HCSMCs M4\KdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV2xNEDPxE1? NFTie5ozPCCq M2PldoJtd2OtczDGRWJRPC2rbnT1Z4VlKEiFQWPNR{Bxem:uaX\ldoF1cW:w NECyOYUzPDNzMkO4NS=>
PANC-1 NUCycHNUTnWwY4Tpc44hSXO|YYm= MXKyNEDPxE1? NFe4TGw1QCCq NYLiNWZYcW6qaXLpeJMhfGinIHX4dJJme3Orb36gc4Yh|pR4RDDpckBz\XOyb37z[UB1dyC2aHWgVHBCWs72wrDh[49vcXO2wrC= M1rlOVI1Ojl2MUOz
A549 NXjLXYZXTnWwY4Tpc44hSXO|YYm= Mn\tN|Ah|ryP MoDwNE42KGh? NHP1VWtFVVOR MXTpcohq[mm2czD0bIUhfGi{b33ibY4ucW6mdXPl[EBKVC16L1PYR2w5NUy3YzDhZ5Rqfmm2eR?= M2DkTlI1Ojd5Nkm2
A549 MXzGeY5kfGmxbjDBd5NigQ>? M2e4T|MxKM7:TR?= MYCwMlUhcA>? NGrxWVNFVVOR MUfpcohq[mm2czD0bJJwdWKrbj3pcoR2[2WmIFOvSWJR|rJiVHjyNlM2yqCyaH;zdIhwenmuYYTpc44> MWWyOFI4PzZ7Nh?=
MC-3 Ml7pRZBweHSxc3nzJGF{e2G7 MlnyNVAh|ryP MYeyOEBp M1zwbJBwfGWwdHnheIVlKE2HU1OtbY5lfWOnZDDhdI9xfG:|aYOgbY4hKGOnbHzz NEHsc4gzPDJ5MEWyNy=>
Raji  NX;ycWNXTnWwY4Tpc44hSXO|YYm= M33mN|ExKM7:TR?= NGfTfY4yKGh? M{W2WYJtd2OtczDod2JCTkZiaX7keYNm\CCHcnuxM|IheGixc4Doc5J6dGG2aX;u NH3VR|kzPDJ4OU[zNC=>
Raji  MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWCxNEDPxE1? NFrFe|IyKGh? NEjqbGpqdmirYnn0d{B1cGViYnHzZYwhd3JiaIPCRWZHNXO2aX31cIF1\WRiY3XscEBxem:uaX\ldoF1cW:wIHHu[EB3cWGkaXzpeJk> MnnINlQzPjl4M{C=
HT29 NFqzeplHfW6ldHnvckBCe3OjeR?= M4TzPVExKM7:TR?= M1nNcFIhcA>? M3PuVYlvcGmkaYTzJI9nKEqDS{KsJGVTUzFxMjDhcoQhW1SDVEOgdIhwe3Cqb4L5cIF1cW:w M1nVU|I1OjZ3Mkmz
HepG2 MoDuRZBweHSxc3nzJGF{e2G7 M3T1elIxKM7:TR?= NIW3dWgzPCCq NGfIRpZqdmirYnn0d{BGWktzL{KgdIhwe3Cqb4L5cIF1cW:wIHHu[EBmdmijbnPld{BXSjFvaX7keYNm\CCjcH;weI9{cXN? NGP6OmczPDJ2N{mwPS=>
HepG2 NVTPOVJlTnWwY4Tpc44hSXO|YYm= NGTVSYYzOCEQvF2= Mo\HNkBp NES4UGpmdmijbnPld{BXSjFvaX7keYNm\CCIT2jPN4EhfHKjboPjdolxfGmxbnHsJIFkfGm4aYT5 M3PRV|I1OjR5OUC5
TE4 NGS1d3ZHfW6ldHnvckBCe3OjeR?= NYjyRoE6OjBxNUCvNVAxKM7:TR?= MnHHOFghcA>? Ml\pSG1UVw>? MkSybY5pcWKrdIOgdE1GemtiYX7kJJdwenSvYX7ubY4h\G:5boLl[5Vt[XSnZDDwMWFsfCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NIHMNXAzPDJ2NECyNy=>
TE1 MnLySpVv[3Srb36gRZN{[Xl? MlzENlAwPTBxMUCwJO69VQ>? MVe0PEBp Mke4SG1UVw>? MXPpcohq[mm2czDwMWVzcyCjbnSge49zfG2jbn7pckBld3ewcnXneYxifGWmIICtRYt1KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NHTq[lgzPDJ2NECyNy=>
KYSE30 M{DoTmZ2dmO2aX;uJGF{e2G7 M33pflIxNzVyL{GwNEDPxE1? MkLnOFghcA>? NEHi[ZlFVVOR NITydYpqdmirYnn0d{BxNUW{azDhcoQhf2:{dH3hco5qdiCmb4fudoVofWyjdHXkJJAuSWu2IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MoXqNlQzPDRyMkO=
TE1 MUnGeY5kfGmxbjDBd5NigQ>? M3WxNlUxKM7:TR?= NGPXW4U1QCCq M{\pPGROW09? NH3LU3B2eHKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCKTFGgZ4xie3NiSR?= NUnvTFB{OjR{NESwNlM>
TE3 NXfye2Y3TnWwY4Tpc44hSXO|YYm= MYS1NEDPxE1? MXy0PEBp NYHKc3o2TE2VTx?= MnHDeZBz\We3bHH0[ZMhfGinIHX4dJJme3Orb36gc4YhUEyDIHPsZZN{KEl? MoP2NlQzPDRyMkO=
TE4 NInTenNHfW6ldHnvckBCe3OjeR?= M{L2OlUxKM7:TR?= MorZOFghcA>? MXzEUXNQ NGTPdpV2eHKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCKTFGgZ4xie3NiSR?= NF;oZmszPDJ2NECyNy=>
TE5 M{nDbWZ2dmO2aX;uJGF{e2G7 MWm1NEDPxE1? M{jCdlQ5KGh? M1\WfWROW09? NG\RRm12eHKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCKTFGgZ4xie3NiSR?= Mke2NlQzPDRyMkO=
KYSE30 NGjDWGRHfW6ldHnvckBCe3OjeR?= M{i2PVUxKM7:TR?= M{\LZ|Q5KGh? M3zneGROW09? M3XuRpVxemWpdXzheIV{KHSqZTDlfJBz\XO|aX;uJI9nKEiOQTDjcIF{eyCL NFfT[VAzPDJ2NECyNy=>
MKN7 MUHGeY5kfGmxbjDBd5NigQ>? M3XmelUxKM7:TR?= NYjBN3pjPDhiaB?= MW\EUXNQ MlvobY5kemWjc3XzJIV5eHKnc4Ppc44hd2ZiSFzBMWExOiCxcjDIUGEuSTJ2IH3vcIVkfWyncx?= M{nyfVI1OjR2MEKz
OE19 MY\GeY5kfGmxbjDBd5NigQ>? NH3TZ3g2OCEQvF2= MnLIOFghcA>? NHvn[INFVVOR M1jPdIlv[3KnYYPld{BmgHC{ZYPzbY9vKG:oIFjMRU1CODJib4KgTGxCNUF{NDDtc4xm[3WuZYO= NYfZbIE4OjR{NESwNlM>
KATOIII  NW\3SnpyTnWwY4Tpc44hSXO|YYm= M{\HUFUxKM7:TR?= MnS2OFghcA>? NEPKcHRFVVOR MnrtbY5kemWjc3XzJIV5eHKnc4Ppc44hd2ZiSFzBMWExOiCxcjDIUGEuSTJ2IH3vcIVkfWyncx?= Mk\jNlQzPDRyMkO=
NCI-N87  NGTDfo9HfW6ldHnvckBCe3OjeR?= M33zVFUxKM7:TR?= M3fyTlQ5KGh? MUTEUXNQ NFztZ4lqdmO{ZXHz[ZMh\XiycnXzd4lwdiCxZjDIUGEuSTB{IH;yJGhNSS2DMkSgcY9t\WO3bHXz MW[yOFI1PDB{Mx?=
NUGC3 NGPXfWRHfW6ldHnvckBCe3OjeR?= M4TYOVUxKM7:TR?= NGnoNHU1QCCq NX;ldG1oTE2VTx?= NGm3bGtqdmO{ZXHz[ZMh\XiycnXzd4lwdiCxZjDIUGEuSTB{IH;yJGhNSS2DMkSgcY9t\WO3bHXz MojSNlQzPDRyMkO=
NUGC2 MV3GeY5kfGmxbjDBd5NigQ>? M3WwS|UxKM7:TR?= MmXsOFghcA>? MnTxSG1UVw>? MVLpcoNz\WG|ZYOg[ZhxemW|c3nvckBw\iCKTFGtRVAzKG:{IFjMRU1COjRibX;s[YN2dGW| MkT6NlQzPDRyMkO=
SGC-7901  NHnQPJNCeG:ydH;zbZMhSXO|YYm= M1PJbVIxKM7:TR?= NXLa[pg2OjRiaB?= NIq2cJFqdmirYnn0d{BEWC2vZXTpZZRm\CCjcH;weI9{cXN? NYm4dXR[OjR{NEGzOVE>
MG-63 M4rITWZ2dmO2aX;uJGF{e2G7 MX:yNEDPxE1? NYHNOYd6OC53IHi= NG\He25jdG:la4OgeIhmKEOKLXnu[JVk\WRicHjvd5Bpd3K7bHH0[YQhTUyNMTDwdo91\WmwIHX4dJJme3Orb36= NYPuNppuOjR{M{m2OFA>
ARPE-19 MmrSSpVv[3Srb36gRZN{[Xl? MVSyNEDPxE1? M2q4N|AvPSCq MUDpcohq[mm2czDBdIVtcW5vaX7keYNm\CCyaH;zdIhwenmuYYTpc44hd2ZiRYLrJIFv\CCDa4S= M2\RT|I1OjJ5OUG4
CRL-2302 NVLtNWNmTnWwY4Tpc44hSXO|YYm= MUCyNEDPxE1? MYGwMlUhcA>? M3;GbIlvcGmkaYTzJGFx\Wyrbj3pcoR2[2WmIIDoc5NxcG:{eXzheIlwdiCxZjDFdosh[W6mIFHreC=> NX7GOmpWOjR{Mke5NVg>
MCF-7 NFTVfVVHfW6ldHnvckBCe3OjeR?= Ml\qNlAh|ryP MofqNUBp NVTv[3hY[WKxbHnzbIV{KGW6cILld5Nqd25ib3[gdIhwe3Cqb4L5cIF1\WRiRWLLJINwNXS{ZXH0cYVvfCC5aYToJINwdmq3Z3H0[S=> MXiyOFIyPjJ6OR?=
MCF-7 MkXSRZBweHSxc3nzJGF{e2G7 NIPJOZQzOCEQvF2= NXH0[2tOOSCq NHfSephqdmO{ZXHz[ZMh[2G|cHHz[U06KGWweont[UBi[3Srdnn0fS=> M2DlWFI1OjF4Mki5
DLD-1  MUXGeY5kfGmxbjDBd5NigQ>? M2nGZVIxyqEQvF2= NUPaTo9IPDhiaB?= MkLTdoVlfWOnczD0bIUhSk6LUEOg[ZhxemW|c3nvckBxemVvdILlZZRm\CC5aYToJFUu[XqjLXTD MX:yOFIyOTV6MR?=
HT-29 MkLMSpVv[3Srb36gRZN{[Xl? NG[5dYUzOMLizszN NX7Oe29uPDhiaB?= NYjzemRkemWmdXPld{B1cGViQl7JVFMh\XiycnXzd4lwdiCycnWteJJm[XSnZDD3bZRpKDVvYYrhMYRE MlvaNlQzOTF3OEG=
7402 NVHMbYZCSXCxcITvd4l{KEG|c3H5 MVezNEDPxE1? NFnRXW02KGR? NYLmfnd{\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdg>? M13lSlI1OjFzMkWz
7721 NIm0NWNCeG:ydH;zbZMhSXO|YYm= NXnzVoxvOzBizszN NGP1cYk2KGR? MVfk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;u M3\BTVI1OjFzMkWz
SGC7901  NGT3eW9CeG:ydH;zbZMhSXO|YYm= Mki2OVDDqM7:TR?= M1PYUFI1NzR6L{eyJIg> Mlz4SG1UVw>? NWmxbVJ7cW6mdXPld{BieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDKRWszKHOqUl7B M13pe|I1OTd6MkSw
SMMC7721 NF\wfZRHfW6ldHnvckBCe3OjeR?= NG\zd2IzPS93MDFOwG0> NVXjOY1{OjRiaB?= MYrzeZBxemW|c3XzJJRp\SCneIDy[ZN{cW:wIH;mJJAuSWu2IH;yJJAuTVKNMT:yxsA> MUeyOFE3QDB3Nh?=
MCF-7 M4TNR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPvNVAh|ryP NF[wZWU1QGh? NV3rWm9VTE2VTx?= NEDOPFdz\X[ncoPld{BDVkZvaX7keYNm\CClZXzsJIN6[2ynIHHydoV{fA>? MUWyOFE3OzRyNB?=
Caco-2 MYHGeY5kfGmxbjDBd5NigQ>? M3PwPVUxyqEQvF2= MmKwOFhp NX6xfIl6TE2VTx?= MVrlcohidmOnczD0bIUhdVKQQTDs[ZZmdHNib3dCpHNEVk5zQTzGXHlFOy{EoFzDWEzDqEyRWD|CpGhKTjODLNMgXmcyPi{EoGDESVZCyqCjbnVCpGxISUyVMUdCpIdmdmW|wrDjc{11emWjdHXkJJdqfGhiRHX4 MUWyOFE3OTZ7NR?=
HAECs MknUSpVv[3Srb36gRZN{[Xl? MV6xNEDPxE1? M17WbVEhcA>? NXzm[mpoyqCjdITlcpVifGW|IGTOSk3PuS2|dHnteYxifGWmIFnDRW0uOSCjbnSgWmNCVS1zIHX4dJJme3Orb36= Mo\QNlQyOzR4NUe=
Ca9-22 MkXqSpVv[3Srb36gRZN{[Xl? NI\H[Ys{KM7:TR?= MUexJIg> NETpXmxi[m:uaYPo[ZMhfGinIHHibYxqfHlib3[gTIJTKHSxIHnu[JVk\SCLTD24JJBzd2S3Y4Tpc44> MmDxNlQyOjZ3M{K=
Ca9-22 MXLGeY5kfGmxbjDBd5NigQ>? Mn[3N{DPxE1? NE\yeWQyNzJiaB?= NUm5N|hDemWmdXPld{BJ[lJvaX7keYNm\CCDVF[tNkBxcG:|cHjvdplt[XSrb36= M2\2cVI1OTJ4NUOy
AGS MnjzSpVv[3Srb36gRZN{[Xl? Mmj0NVAh|ryPwrC= M3zYZVAvPSCq MW\pcohq[mm2czD0bIUhfXC{ZXf1cIF1cW:wIH;mJJRp\SCLTD24JIdmdmV? MmOyNlQyODZzNk[=
Caco-2  NYDCXWJZSXCxcITvd4l{KEG|c3H5 NHL6N20yOMLizszN M3;UOlI1yqCq Mofo[IVkemWjc3XzJINmdGxiYYDvdJRwe2m|IHnu[JVk\WRiYomgOU1HXQ>? NHHqUYozPDB7NUi2Ny=>
HCT-8 MoOwRZBweHSxc3nzJGF{e2G7 MoXrNVDDqM7:TR?= MYqyOOKhcA>? M2PpOoRm[3KnYYPld{Bk\WyuIHHwc5B1d3OrczDpcoR2[2WmIHL5JFUuTlV? NFu2NIEzPDB7NUi2Ny=>
A549 NUPDb|VSTnWwY4Tpc44hSXO|YYm= MoHmOVDDqM7:TR?= MXqyJIg> MYjicI9kc3NiRWLLJJBpd3OyaH;yfYxifGmxbjDt[YRq[XSnZDDifUAyNDJvTmG= M3TURlI1ODZ5N{K3
HPMC MUTGeY5kfGmxbjDBd5NigQ>? MlO1NVDDqM7:TR?= M4XZRlQ5KGh? MmPkdoV3\XK|ZYOgeIhmKGOqYX7n[ZMhcW5iY3XscEBud3KyaH;sc4d6KGmwZIXj[YQh[nliSFfQSHM> M{XMblI1ODR{OEO4
HPMC MnGyRZBweHSxc3nzJGF{e2G7 NXfqXoxXOTEEoN88US=> M4TDe|I1yqCq NHr4[ZFz\X[ncoPld{Bl\WO{ZXHz[UBqdiClZXzsJJZq[WKrbHn0fUBqdmS3Y3XkJIJ6KEiJUFTT NWS5N3lkOjRyNEK4N|g>
MGC803  NF\lempCeG:ydH;zbZMhSXO|YYm= NIKw[JEzOMLizszN NGTie4gyKGh? NYf0O3UxcW6qaXLpeJMh[XCxcITvd4l{KGmwZIXj[YQh[nliSV\OMe6yyqCjbnSgOgKBui2GRmXS MlfaNlQxOjd5NUC=
SGC7901 M3rXU2Fxd3C2b4Ppd{BCe3OjeR?= M2LVUlIxyqEQvF2= NE\Gb3EyKGh? M2TEeolvcGmkaYTzJIFxd3C2b4Ppd{BqdmS3Y3XkJIJ6KEmITj5OteKh[W6mIEZihNIuTE[XUh?= MmfnNlQxOjd5NUC=
COLO205 NED5OnVCeG:ydH;zbZMhSXO|YYm= M2XKcVExNzJyL{SwJO69VQ>? Mk\0NlQhcA>? M37oTYlv\HWlZYOgSG5CKGyjZHTldkBnd3KvYYTpc44> NXjYOYw4OjRyMUmxNFg>
G292  NIHRZVJCeG:ydH;zbZMhSXO|YYm= M3fuWVMxyqEQvF2= NHLqXW0zKGh? M1q1dJJme3SxcnXzJINieHOjaXPpck1qdmS3Y3XkJINmdGxiZHXheIg> NU\PbXlQOjRyMUK5N|A>
BxPC-3 Ml\XSpVv[3Srb36gRZN{[Xl? NFLud4YyOCEQvF5CpC=> NXfPPVNqPiCq MlTkbY5kemWjc3WgcYlTNTF2MzDlfJBz\XO|aX;u MnT6NlM6PzN5MUC=
HPAF-II MoC0SpVv[3Srb36gRZN{[Xl? NV;wS3d[OTBizszNxsA> M4\WXFYhcA>? MXPpcoNz\WG|ZTDtbXIuOTR|IHX4dJJme3Orb36= NInVT3AzOzl5M{exNC=>
HL-60 NH7WT4NCeG:ydH;zbZMhSXO|YYm= M{PRO|UxyqEQvF2= MkTBNUBp MlmwdoV{[3WnczDCRVE1PSCvZXTpZZRm\CCjcH;weI9{cXN? MmTpNlM6PDh5NUG=
HepG2 MX;GeY5kfGmxbjDBd5NigQ>? NIi5bm81OCEQvF2= NVLoN|J4Pi9zMjDo MV;pcohq[mm2czD0bIUhcW6lcnXhd4Uhd2ZicD3FVmsyKGGwZDDwMYMuUnWwIIDyc5RmcW5iZYjwdoV{e2mxbjDifUBRVA>? NYP5Ro11OjN7NEK4OVE>
HUVECs NFHidHVHfW6ldHnvckBCe3OjeR?= M2HLZlI2KM7:TR?= MmC4NUBp MYnpcoNz\WG|ZTDOSk3PwkJicE[1JI52[2ynYYKgeJJidnOub3PheIlwdg>? MnruNlM6ODFyMEi=
LNCaP  MX7GeY5kfGmxbjDBd5NigQ>? MmqzNVAh|ryPwrC= MVixJIg> MVLk[YNz\WG|ZYOgeIhmKEWJRjD1dJJm\3WuYYTl[EBxNVmELUG= M3fJ[|I{QDN6M{G4
HL60  MX\GeY5kfGmxbjDBd5NigQ>? Ml3XNlDDqM7:TR?= MVq3NkBp MnPjSG1UVw>? M4DIdYlvcGmkaYTzJIRie2G2aX7pZk1qdmS3Y3XkJGNFOTGkIHX4dJJme3Orb36= MnT6NlM5OjV3OEW=
NB4  NYXRSmc3TnWwY4Tpc44hSXO|YYm= NUDDN202OTBizszNxsA> MoDJO|IhcA>? M3u3UWROW09? NHvEVJlqdmirYnn0d{Bl[XOjdHnubYIucW6mdXPl[EBETDFzYjDlfJBz\XO|aX;u NH;xZ3YzOzh{NUW4OS=>
EPOR/CR3 NHXPS|JHfW6ldHnvckBCe3OjeR?= M2XubVUxyqEQvF2= NXTTNJVJOyCq NHHQO2Nz\WS3Y3XzJGVRVyCjbnSvc5IhUUxvMz3pcoR2[2WmIITo[UB1gXKxc3nu[UBxcG:|cHjvdplt[XSrb39CpC=> NVO2XYxPOjN6MkC3N|E>
HUASMCs NFPB[YdHfW6ldHnvckBCe3OjeR?= MkftNVAh|ryPwrC= NUTv[mFYOjRiaB?= M1PicIRqdWmwaYPo[ZMhSW6pIFnJMYNifXOnZDDTU2NUOyCvUl7BJIFv\CCycn;0[YlvKGW6cILld5Nqd28EoB?= NX7TRpJNOjN6MU[0Olg>
HUASMCs NITQVpdHfW6ldHnvckBCe3OjeR?= M2Lv[FExKM7:TdMg Ml\NNlQhcA>? M2e5SYlvcGmkaYTzJGFv\yCLST3pcoR2[2WmIFXST|EwOiCyaH;zdIhwenmuYYTpc44hdGW4ZXy= NHrC[FMzOzhzNkS2PC=>
SGC7901 MlnpSpVv[3Srb36gRZN{[Xl? MWixNEDPxE4EoB?= MlmyNlQhcA>? MlTDbY5pcWKrdIOgeIhmKGW6cILld5Nqd25ib3[gdIhwe3Cqb4L5cIF1\WRiRWLLNU8z NFjJOowzOzd7MkW4PC=>
MKN45 Ml7LSpVv[3Srb36gRZN{[Xl? MXGxNEDPxE4EoB?= MmLBNlQhcA>? M1naNIlvcGmkaYTzJJRp\SCneIDy[ZN{cW:wIH;mJJBpd3OyaH;yfYxifGWmIFXST|EwOg>? MoDtNlM4QTJ3OEi=
SGC7901 MnLQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7pSYJkOTBizszNxsA> NFPSd44zPC92OD:3NkBp NYfYV2pucW6qaXLpeJMh[2WubDDndo94fGhiY3:teJJm[XSnZDD3bZRpKESDUGS= MVOyN|c6OjV6OB?=
MKN45 NUXnRok1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3XoXlExKM7:TdMg NFjwZ44zPC92OD:3NkBp MVzpcohq[mm2czDj[YxtKGe{b4f0bEBkdy22cnXheIVlKHerdHigSGFRXA>? MnzBNlM4QTJ3OEi=
SGC7901 NWjobGRwSXCxcITvd4l{KEG|c3H5 M1\nblExKM7:TdMg MUeyOEBp MkXsbY5kemWjc3XzJJRp\SCGQWDUMYlv\HWlZXSgZ4VtdCCjcH;weI9{cXN? NUTWb5pOOjN5OUK1PFg>
MKN45 NVjlUmRsSXCxcITvd4l{KEG|c3H5 MVmxNEDPxE4EoB?= NXrSWm1oOjRiaB?= NWPnS5RTcW6lcnXhd4V{KHSqZTDERXBVNWmwZIXj[YQh[2WubDDhdI9xfG:|aYO= Mn7QNlM4QTJ3OEi=
BxPC-3 cells MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2C1b|IxyqEQvF2= MV2wMlUhcA>? M2TNOYlvcGmkaYTzJHZGT0ZvQT3y[Yd2dGG2ZXSgTHVXTUNiZ4Lve5RpKGGwZDD0eYJmKG[xcn3heIlwdiCrbnT1Z4VlKGK7IGDBVk0zKEGS NEjYRWgzOzd4NEC0Oi=>
NB4  MYnBdI9xfG:|aYOgRZN{[Xl? M{Pa[VExNzJyL{[wJO69VQ>? NIP6fZYyNjViaB?= MU\EUXNQ MVzk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliY3:teJJm[XSnZDD3bZRpKFCjY3zpeIF5\Wx? MVSyN|c{PTV2MR?=
HepG2  MmHSSpVv[3Srb36gRZN{[Xl? MkmxNlDDqM7:TR?= M2joSVI1KGh? MnrTbY5pcWKrdIOgeIhmKEiRLUGgdJJwfGWrbjDlfJBz\XO|aX;uJINwNXS{ZXH0[YQhf2m2aDDt[ZRnd3KvaX6= M1TtbVI{PzB5NkC5
HUVECs M1nD[GFxd3C2b4Ppd{BCe3OjeR?= M320blIwPCEQvF2= NIHFengzPC92ODDo Mli5bY5lfWOnczDj[YxtKGSnYYTo NVTGZppNOjN5MEe1NlA>
KG-1  NH;wR4NCeG:ydH;zbZMhSXO|YYm= M3PPdlIxyqEQvF2= NIGwcYgyOiCq MmjD[Y5p[W6lZYOgZ4VtdCCjcH;weI9{cXNiaX7keYNm\CCkeTDTNS=> NHXYXFYzOzdyNk[5NS=>
AML 1# MV7BdI9xfG:|aYOgRZN{[Xl? M1nKOFIxyqEQvF2= NVzmXoJNOTJiaB?= NH;rOlVmdmijbnPld{Bk\WyuIHHwc5B1d3OrczDpcoR2[2WmIHL5JHMy NIjydZgzOzdyNk[5NS=>
A2780  MX7GeY5kfGmxbjDBd5NigQ>? NHnSUG0zOMLizszN MWCxJIg> M{LkeIJtd2OtczDEWGNFNWmwZIXj[YQhTFJ3IHX4dJJme3Orb36= M2noPFI{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:
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
1mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 267.28
Formula

C16H13NO3

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

Bio Calculators

Molarity Calculator

Molarity Calculator

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

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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

Dilution Calculator

Dilution Calculator

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

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

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

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Molecular Weight Calculator

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