Potent MEK1 and MEK2 inhibitor. Inhibits MEK activity in mouse colon 26 cells (IC50 = 0.33 nM). 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. Also inhibits production of proangiogenic cytokines such as VEGF. Enhances generation of induced pluripotent stem cells (iPSCs). Orally active.
Sold for research purposes under agreement from Pfizer Inc.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 482.19. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.07 mL||10.37 mL||20.74 mL|
|5 mM||0.41 mL||2.07 mL||4.15 mL|
|10 mM||0.21 mL||1.04 mL||2.07 mL|
|50 mM||0.04 mL||0.21 mL||0.41 mL|
The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.
References are publications that support the products' biological activity.
Barrett et al (2008) The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901. Bioorg.Med.Chem.Lett. 18 6501 PMID: 18952427
Ciuffreda et al (2009) Growth-inhibitor and antiangiogenic activity of the MEK inhibitor PD0325901 in malignant melanoma with or without BRAF mutations. Neoplasia 11 720 PMID: 19649202
Lin et al (2009) A chemical platform for improved induction of human iPSCs. Nat.Methods. 6 805 PMID: 19838168
If you know of a relevant reference for PD 0325901, please let us know.
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9 Citations for PD 0325901
Citations are publications that use Tocris products. Selected citations for PD 0325901 include:
Denham et al (2012) 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. Development 30 2400 PMID: 22911885
Cho et al (2012) Conversion from mouse embryonic to extra-embryonic endoderm stem cells reveals distinct differentiation capacities of pluripotent stem cell states. Cancer Biol Ther 139 2866 PMID: 22791892
Oliveira et al (2016) Poly(I:C) increases the expression of mPGES-1 and COX-2 in rat primary microglia. Stem Cells 13 11 PMID: 26780827
Kearns et al (2015) Functional annotation of native enhancers with a Cas9-histone demethylase fusion. Nat Methods 12 401 PMID: 25775043
Maza et al (2015) Transient acquisition of pluripotency during somatic cell transdifferentiation with iPSC reprogramming factors. Nat Biotechnol 33 769 PMID: 26098448
Mattis et al (2015) HD iPSC-derived neural progenitors accumulate in culture and are susceptible to BDNF withdrawal due to glutamate toxicity. PLoS One 24 3257 PMID: 25740845
Solari et al (2015) Manganese Superoxide Dismutase Gene Expression Is Induced by Nanog and Oct4, Essential Pluripotent Stem Cells' Transcription Factors. Mol Syst Biol 10 e0144336 PMID: 26642061
Sladitschek and Neveu (2015) The bimodally expressed microRNA miR-142 gates exit from pluripotency. J Neuroinflammation 11 850 PMID: 26690966
Muthusamy et al (2014) A method to identify and isolate pluripotent human stem cells and mouse epiblast stem cells using lipid body-associated retinyl ester fluorescence. Stem Cell Reports 3 169 PMID: 25068130
Do you know of a great paper that uses PD 0325901 from Tocris? If so please let us know.
Literature in this Area
MAPK Signaling Scientific Review
MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.