| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C16H13NO3 |
| Purity | |
| Activity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
PD98059 is a potent, selective inhibitor of MEK, acting with an IC50 of 5 μM. It binds the inactive form of MEK, blocking activation of MEK1 (IC50 2-7 μM) and MEK2 (IC50 50 μM) by upstream kinases, and thereby inhibits ERK1/2 signaling. The compound also acts as a ligand for the aryl hydrocarbon receptor (AHR), suppressing TCDD binding (IC50 4 μM) and AHR transformation (IC50 1 μM), and it inhibits Mycobacterium bovis Bacillus CalmetteGuerin (BCG)-induced autophagy[1][2][3]. It is supplied as a light yellow to yellow solid (C16H13NO3, MW 267.28) at 99.27% purity.
Physical & Chemical Properties
| CAS Number | 167869-21-8 |
|---|---|
| Molecular Formula | C16H13NO3 |
| Molecular Weight | 267.28 g/mol |
| Purity | 99.27% |
| Appearance | Solid |
| Color | Light yellow to yellow |
| SMILES | O=C1C=C(OC2=CC=CC=C21)C3=CC=CC(OC)=C3N |
| Target | MEK1, MEK2, ERK1, ERK2 |
| Signaling Pathway | MAPK/ERK Pathway; Stem Cell/Wnt; Immunology/Inflammation; Autophagy |
| Bioactivity Class | Autophagy |
| Solubility | In Vitro: DMSO: 33.33 mg/mL (124.70 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) H2O: < 0.1 mg/mL (insoluble) |
| Storage | 4°C, protect from light. In solvent: -80°C, 1 year; -20°C, 6 months (protect from light). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target
[1][3]
|
MEK1 2-7 μM (IC50) |
MEK2 50 μM (IC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 33.33 mg/mL (124.70 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
| H2O | < 0.1 mg/mL | insoluble |
Aliquot the stock solution and store it at -80°C (up to 1 year) or -20°C (up to 6 months); protect from light; avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | 2.08 mg/mL (7.78 mM); suspension; requires sonication |
| How to prepare | Gives a suspension at 2.08 mg/mL. The suspension is suitable for oral and intraperitoneal dosing. For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Direct preparation of the working solution
These formulations are prepared directly, without a DMSO stock; use them promptly after preparation.
Protocol 2
| Composition | 50% PEG300 + 50% saline |
|---|---|
| Result | 10 mg/mL (37.41 mM); suspension; requires sonication |
Data provided by the manufacturer.
In Vitro
In OCI-AML-3 cells, PD98059 (20 μM; 24 hours) causes G1-phase cell cycle arrest[4]. PD98059 (10 μM; 22 hours) reduces the dually phosphorylated forms of ERK1 and ERK2 in a concentration-dependent manner[1]. PD98059 prevents ERK activation and also blocks the formation of TDP-43 and HuR-positive SGs[7].
Cell Cycle Analysis[4]
| Cell Line | OCI-AML-3 cells |
|---|---|
| Concentration | 20 μM |
| Incubation Time | 24 hours |
| Result | Caused G1-phase cell cycle arrest. |
Western Blot Analysis[1]
| Cell Line | MCF10A-Neo, MCF10ANeoT cells |
|---|---|
| Concentration | 10 μM |
| Incubation Time | 22 hours |
| Result | Phosphorylated ERK forms were almost completely eliminated in both cell lines. |
In Vivo
In zymosan-injected mice, PD98059 (10 mg/kg; i.p.; 1 and 6 hours after Zymosan) significantly lowers the level of p-ERK1/2[3].
| Animal Model | Male CD mice[3] |
|---|---|
| Dosage | 10 mg/kg |
| Administration | Intraperitoneal injection; 1 and 6 hours after Zymosan |
| Result | Significantly reduced the level of p-ERK1/2. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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