PD 0325901

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PD 0325901 | CAS No. 391210-10-9 | MEK Inhibitors
1 Image
Description: Potent inhibitor of MEK1/2
Alternative Names: PD325901

Chemical Name: N-[(2R)-2,3-Dihydroxypropoxy]-3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-benzamide

Purity: ≥99%

Product Details
Citations (21)

Biological Activity

PD 0325901 is a potent MEK1 and MEK2 inhibitor. PD 0325901 inhibits MEK activity in mouse colon 26 cells (IC50 = 0.33 nM). PD 0325901 inhibits the growth of melanoma cell lines in vitro and in vivo; induces G1-phase cell cycle arrest and apoptosis in a mouse xenograft model. PD 0325901 also inhibits production of proangiogenic cytokines such as VEGF. PD 0325901 enhances generation of induced pluripotent stem cells (iPSCs). PD 0325901 in combination with Vitamin C sustains mouse ES cells at an undifferentiated and hypomethylated state. PD 0325901 promotes myelin recovery in drug-induced demyelination in vivo in mice model. Orally active.

For more information about how PD 0325901 may be used, see our protocols: Culturing Transcriptomically Distinct Pluripotent mESCs, Highly Efficient Generation of CiPSCs from MEFs, Accelerated Induction of Cortical Neurons from hiPSCs.

Technical Data

Soluble to 25 mM in DMSO
Store at -20°C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold for research purposes under agreement from Pfizer Inc.

Background References

  1. 3D mouse embryonic stem cell culture for generating inner ear organoids.
    Koehler KR, Hashino E.
    Nat Protoc
  2. A chemical platform for improved induction of human iPSCs.
    Lin et al.
    Nat.Methods., 2009;6:805
  3. The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901.
    Barrett et al.
    Bioorg.Med.Chem.Lett., 2008;18:6501
  4. Growth-inhibitor and antiangiogenic activity of the MEK inhibitor PD0325901 in malignant melanoma with or without BRAF mutations.
    Ciuffreda et al.
    Neoplasia, 2009;11:720
  5. The biological profile of PD 0325901: a second generation analog of CI-1040 with improved pharmaceutical potential.
    Sebolt-Leopold et al.
    Proc.Amer.Assoc.Cancer Res., 2004;45:925

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Citations for PD 0325901

The citations listed below are publications that use Tocris products. Selected citations for PD 0325901 include:

21 Citations: Showing 1 - 10

  1. A dose-dependent response to MEK inhibition determines hypoblast fate in bovine embryos.
    Authors: Canizo Et al.
    BMC Dev Biol  2019;19:13
  2. Implantation initiation of self-assembled embryo-like structures generated using three types of mouse blastocyst-derived stem cells.
    Authors: Zhang Et al.
    Nat Commun  2019;10:496
  3. Discordant congenital Zika syndrome twins show differential in vitro viral susceptibility of neural progenitor cells.
    Authors: Caires-J?nior
    Nat Commun  2018;9(1):475
  4. Gain of toxic apolipoprotein E4 effects in human iPSC-derived neurons is ameliorated by a small-molecule structure corrector.
    Authors: Wang
    Nat Med  2018;24(5):647
  5. CRISPR-based chromatin remodeling of the endogenous Oct4 or Sox2 locus enables reprogramming to pluripotency.
    Authors: Liu Et al.
    Cell Stem Cell.  2018;22:252
  6. Distinctive features of lincRNA gene expression suggest widespread RNA-independent functions.
    Authors: Tuck Et al.
    Life Sci Alliance  2018;1:e201800124
  7. PARK2 Depletion Connects Energy and Oxidative Stress to PI3K/Akt Activation via PTEN S-Nitrosylation.
    Authors: Gupta Et al.
    Mol Cell  2017;65:999
  8. Gene Resistance to Transcriptional Reprogramming following Nuclear Transfer Is Directly Mediated by Multiple Chromatin-Repressive Pathways.
    Authors: Jullien Et al.
    Mol Cell  2017;65:873
  9. Stem Cell Differentiation as a Non-Markov Stochastic Process.
    Authors: Stumpf Et al.
    Cell Syst  2017;5:268
  10. Establishment of mouse expanded potential stem cells.
    Authors: Yang Et al.
    Nature  2017;550:393
  11. The intrinsically kinase-inactive EPHB6 receptor predisposes cancer cells to DR5-induced apoptosis by promoting mitochondrial fragmentation.
    Authors: Zawily Et al.
    Oncotarget  2016;7:77865
  12. Poly(I:C) increases the expression of mPGES-1 and COX-2 in rat primary microglia.
    Authors: Oliveira Et al.
    Stem Cells  2016;13:11
  13. Transient acquisition of pluripotency during somatic cell transdifferentiation with iPSC reprogramming factors.
    Authors: Maza Et al.
    Nat Biotechnol  2015;33:769
  14. HD iPSC-derived neural progenitors accumulate in culture and are susceptible to BDNF withdrawal due to glutamate toxicity.
    Authors: Mattis Et al.
    PLoS One  2015;24:3257
  15. Effects of AKT inhibition on HGF-mediated erlo. resistance in non-small cell lung cancer cell lines.
    Authors: Holland Et al.
    J Cancer Res Clin Oncol  2015;141:615
  16. Functional annotation of native enhancers with a Cas9-histone demethylase fusion.
    Authors: Kearns Et al.
    Nat Methods  2015;12:401
  17. The bimodally expressed microRNA miR-142 gates exit from pluripotency.
    Authors: Sladitschek and Neveu
    J Neuroinflammation  2015;11:850
  18. Manganese Superoxide Dismutase Gene Expression Is Induced by Nanog and Oct4, Essential Pluripotent Stem Cells' Transcription Factors.
    Authors: Solari Et al.
    Mol Syst Biol  2015;10:e0144336
  19. A method to identify and isolate pluripotent human stem cells and mouse epiblast stem cells using lipid body-associated retinyl ester fluorescence.
    Authors: Muthusamy Et al.
    Stem Cell Reports  2014;3:169
  20. Glycogen synthase kinase 3β and activin/nodal inhibition in human embryonic stem cells induces a pre-neuroepithelial state that is required for specification to a floor plate cell lineage.
    Authors: Denham Et al.
    Development  2012;30:2400
  21. Conversion from mouse embryonic to extra-embryonic endoderm stem cells reveals distinct differentiation capacities of pluripotent stem cell states.
    Authors: Cho Et al.
    Cancer Biol Ther  2012;139:2866


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