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PD0325901

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PD0325901 is a selective, non-ATP-competitive inhibitor of the mitogen-activated protein kinase (MAPK/ERK kinase, or MEK) that suppresses expression of p-ERK1/2 and induces apoptosis. PD0325901 enhances generation of induced pluripotent stem cells (iPSCs).
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SML24B 10 mg $225.00
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Description
Specifications
More Information
SKUSML24B
Size10 mg
Molecular NamePD0325901
FormPowder
Alternative NamesPD325901; Mirdametinib
Chemical NameN-[(2R)-2,3-dihydroxypropoxy]-3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-benzamide
Chemical FormulaC16H14F3IN2O4
Molecular Weight482.19
CAS Number391210-10-9
PurityGreater than 98% by HPLC
Physical AppearanceWhite to off-white (solid)
TargetMEK
Shelf-Life≥ 2 years (powder)
ShippingRoom Temperature
StorageStore at -20°C
Quality StatementThis product is for Research Use Only and is not intended for therapeutic or diagnostic use.

PD0325901 is a potent non-ATP-competitive MEK inhibitor (IC50 = 0.33 nM), exhibiting an apparent Ki of 1 nM against activated MEK1 and MEK2. PD0325901 selectively inhibits MEK, which may result in the inhibition of phosphorylation and activation of the MAPK/ERK pathways and tumor cell proliferation.

PD0325901 has been shown to promote OCT4-mediated reprogramming methods4 and increase reprogramming efficiency of fibroblasts to induced pluripotent stem cells (iPSC) when used along with the ALK5 inhibitor SB4315423. When used with CHIR99021 and A83-01, PD0325901 has been shown to generate “ground state” iPSC from somatic cells6.

Alternative names: PD325901; Mirdametinib
Applications: Pluripotent Stem Cell Culture; Reprogramming; Mouse ES Cell Culture; Cancer research

Features & Benefits
  • Non-ATP-competitive MEK inhibitor
  • Increases iPSC reprogramming efficiency with SB431542
  • Promotes OCT4-mediated reprogramming to iPSC
Solubility Table

Stock Concentration Compound Mass
1 mg 5 mg 10 mg
1 mM 2.0739 mL 10.3694 mL 20.7387 mL
5 mM 0.4148 mL 2.0739 mL 4.1477 mL
10 mM 0.2074 mL 1.0369 mL 2.0739 mL
50 mM 0.0415 mL 0.2074 mL 0.4148 mL
 Solvent Volume

Preparation & Reconstitution
  1. From the lyophilized compound, prepare a concentrated stock solution using the appropriate solvent (DMSO), according to the solubility table or custom calculations. Example: To generate a 5 mM concentrated stock solution of PD0325901, add 2.074 mL of DMSO to 5 mg of PD0325901.
  2. Ensure the compound is completely dissolved in the solvent. This may require gentle warming and/or vortexing/sonication to fully reconstitute the compound.
  3. Aliquot the concentrated stock solution in single-use volumes, and either use immediately or freeze at -20°C or -80°C for later use. Avoid freeze/thaw cycles.
  4. Concentrated stock solutions are designed to be diluted just prior to use (e.g. 1:1000 dilution in cell culture medium). For use in cell culture, warm the medium just prior to adding the reconstituted compound.

Resources
Documents
References and Publications
  1. Tojo, M., et al. The ALK-5 inhibitor A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growth factorβ. Cancer Sci 96: 791-800 (2005).
  2. Li, W., et al. Generation of rat and human induced pluripotent stem cells by combining genetic reprogramming and chemical inhibitors. Cell Stem Cell 4: 16-19 (2009).
  3. Zhou et al. Conversion of mouse epiblast stem cells to an earlier pluripotency state by small molecules. J Bio Chem 285(39); 29676-80 (2010).
  4. Zhu et al., Reprogramming of human primary somatic cells by OCT4 and chemical compounds. Cell Stem Cell 7(6): 651-5 (2010).
  5. Zhang et al. Pharmacological reprogramming of fibroblasts into neural stem cells by signaling-directed transcriptional activation. Cell Stem Cell 18(5): 653-67 (2016).
  6. Taniguchi Y, et al. Enhanced antitumor efficacy of folate-linked liposomal Adriamycin with TGF-β type I receptor inhibitor. Cancer Sci. 2010 Oct;101(10):2207-13.
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