PD98059

Name: PD98059
Brand: MedChemExpress
SKU: HY-12028
Rating: 5.0 (342 reviews)

Cat. No.: HY-12028 Purity: 99.96%: Data Sheet
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PD98059 is a potent and selective MEK inhibitor with an IC₅₀ of 5 µM. PD98059 binds to the inactive form of MEK, thereby preventing the activation of MEK1 (IC₅₀ of 2-7 µM) and MEK2 (IC₅₀ of 50 µM) by upstream kinases. PD98059 is a ERK1/2 signaling inhibitor. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR), and suppresses TCDD binding (IC₅₀ of 4 μM) and AHR transformation (IC₅₀ of 1 μM). PD98059 also inhibits Mycobacterium bovis Bacillus CalmetteGuerin (BCG)-induced autophagy.

For research use only. We do not sell to patients.

PD98059 Chemical Structure

CAS No. : 167869-21-8

Size	Stock	Quantity

Free Sample (0.1 - 0.5 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
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Based on 342 publication(s) in Google Scholar

333 Publications Citing Use of MCE PD98059

: PD98059 purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2023 Feb 1;116:109763. [Abstract]; PD98059 (0,10,30 μM; 24 h) inhibits the expression of p-ERK, Nrf2, Hif-1α, and IL-17D in NCM460 cells.

: PD98059 purchased from MedChemExpress. Usage Cited in: Redox Biol. 2019 Apr;22:101133. [Abstract]; The effects of inhibitor PD98059 on the phosphorylated-ERK1/2, total ERK1/2, Thr181-phosphorylated tau, Thr205-phosphorylated tau, total tau and ROS production in different groups with or without Aβ_25-35/FGF21.

: PD98059 purchased from MedChemExpress. Usage Cited in: Mol Cell. 2018 Feb 1;69(3):480-492.e7. [Abstract]; ERK is important for Nur77 phosphorylation. MV3 cells are pretreated with different kinase inhibitors (PD98059, 40 μM; SB202190, 20 μM; SP600125, 25 μM) before 3 hr of glucose starvation.

: PD98059 purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2018 Feb;98:36-44. [Abstract]; Resveratrol (RES) inhibits epithelial-mesenchymal transition (EMT) and extracellular matrix (ECM) remodeling of renal cell carcinoma (RCC) cells via the Akt and ERK1/2 signaling pathway. RCC cell lines are treated with RES (0, 50, 100 μM) and 50 μM PD98059 for 24 h. Levels of Akt, p-Akt, ERK1/2, p-ERK1/2 proteins are examined by Western blot.

: PD98059 purchased from MedChemExpress. Usage Cited in: Sci Rep. 2018 Feb 12;8(1):2848. [Abstract]; The expression of EGFR, p-EGFR, ERK, p-ERK and FOS in four groups (from left to right: 50 μM PD98059, 30 min; control; pretreatment with 50 μM PD98059, 30 min, then intervened with 0.1 mg/L BER 15 min; 0.1 mg/L BER for 15 min) are examined using western blot.

: PD98059 purchased from MedChemExpress. Usage Cited in: Toxicology. 2018 Dec 1;410:222-230. [Abstract]; SH-SY5Y cells are pretreated with MEK inhibitor PD98059 (10 μM) for 1 h, then incubated with NaF (60 mg/L) for 24 h. Representative images of western blotting for BDNF, TrkB and p-ERK1/2 in SH-SY5Y cells.

: PD98059 purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Jan 1;495(1):781-786. [Abstract]; Representative images of migrated cells. HUVECs are pretreated with PD98059 (10 μM), SCH772984 (500 nM) or mock control for 2 h, and seeded in upper chambers of transwell inserts. VEGF (100 ng/ml), Scg3 (1 μg/ml) or PBS in medium with reduced FBS is added to bottom chambers in the presence or absence of the inhibitor. After culturing for 4 or 20 h, cells migrated to the lower surface of transwell membrane are stained with DAPI.

: PD98059 purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Dec 9;507(1-4):253-259. [Abstract]; The expression of p-ERK1/2, ERK1/2, AGCAN and COL2 detected by Western blot in degenerated NP cells treated with or without rhLIF (100 ng/ml) and PD98059 (0 μM, 25 μM, 50 μM) for 48 h.

: PD98059 purchased from MedChemExpress. Usage Cited in: Exp Ther Med. 2017 Apr;13(4):1353-1359. [Abstract]; Hippocampal neuron lysates are subjected to western blotting to evaluate Nrf2 levels and the phosphorylation of ERK in the presence and absence of PD98059.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]^[3]

MEK1

2-7 μM (IC₅₀)

MEK2

50 μM (IC₅₀)

ERK1

ERK2

Autophagy

Cellular Effect

Cell Line	Type	Value	Description	References
C6	IC₅₀	4.2 μM Compound: PD98059	Inhibition of MEK1/2 in rat IEC6 cells assessed as reduction in ERK1/2 loop phosphorylation dosed 30 mins before to stimulation with 10% serum for 5 mins by immunoblotting method Inhibition of MEK1/2 in rat IEC6 cells assessed as reduction in ERK1/2 loop phosphorylation dosed 30 mins before to stimulation with 10% serum for 5 mins by immunoblotting method	[PMID: 25078316]
HT-29	IC₅₀	4 μM Compound: PD98059	Antiproliferative activity against human HT-29 cells after 5 days by WST1 assay Antiproliferative activity against human HT-29 cells after 5 days by WST1 assay	[PMID: 25078316]

In Vitro

PD98059 (20 μM; 24 hours) causes G1-phase cell cycle arrest in OCI-AML-3 cells^[4].
PD98059 (10 μM; 22 hours) results in concentration-dependent reductions in the dually phosphorylated forms of ERK1 and ERK2^[1]. PD98059 both prevents ERK activation and blocks formation of TDP-43 and HuR-positive SGs^[7].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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

PD98059 (10 mg/kg; i.p.; 1 and 6 hours after Zymosan) significantly reduces the level of p-ERK1/2 in zymosan-injected mice^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Molecular Weight

267.28

Formula

C₁₆H₁₃NO₃

CAS No.

167869-21-8

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C=C(OC2=CC=CC=C21)C3=CC=CC(OC)=C3N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

Solvent & Solubility

In Vitro:

DMSO : 33.33 mg/mL (124.70 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.7414 mL	18.7070 mL	37.4139 mL
5 mM	0.7483 mL	3.7414 mL	7.4828 mL
10 mM	0.3741 mL	1.8707 mL	3.7414 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (7.78 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 10 mg/mL (37.41 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.96%

Select Batch:

Data Sheet (280 KB) SDS (479 KB)

COA (249 KB) LCMS (92 KB)

Handling Instructions (2659 KB)

References

[1]. Reiners JJ Jr, et al. PD98059 is an equipotent antagonist of the aryl hydrocarbon receptor and inhibitor of mitogen-activated protein kinase kinase. Mol Pharmacol. 1998 Mar;53(3):438-45. [Content Brief]

[2]. Alessi DR, et al. PD 098059 is a specific inhibitor of the activation of mitogen-activated protein kinase kinase in vitro and in vivo. J Biol Chem, 1995, 270(46), 27489-27494. [Content Brief]

[3]. Jia Luo, et al. DUSP5 (dual-specificity protein phosphatase 5) suppresses BCG-induced autophagy via ERK 1/2 signaling pathway.

[4]. Di Paola R, et al. PD98059, a specific MAP kinase inhibitor, attenuates multiple organ dysfunction syndrome/failure (MODS) induced by zymosan in mice. Pharmacol Res. 2010 Feb;61(2):175-87. [Content Brief]

[5]. Kojima K, et al. Mitogen-activated protein kinase kinase inhibition enhances nuclear proapoptotic function of p53 in acute myelogenous leukemia cells. Cancer Res. 2007 Apr 1;67(7):3210-9. [Content Brief]

[6]. Kim KY, et al. Inhibition of Autophagy Promotes Salinomycin-Induced Apoptosis via Reactive Oxygen Species-Mediated PI3K/AKT/mTOR and ERK/p38 MAPK-Dependent Signaling in Human Prostate Cancer Cells. Int J Mol Sci. 2017 May 18;18(5). pii: E1088. [Content Brief]

[7]. Sarah J Parker, et al. Inhibition of TDP-43 accumulation by bis(thiosemicarbazonato)-copper complexes. PLoS One. 2012;7(8):e42277. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.7414 mL	18.7070 mL	37.4139 mL	93.5349 mL
	5 mM	0.7483 mL	3.7414 mL	7.4828 mL	18.7070 mL
	10 mM	0.3741 mL	1.8707 mL	3.7414 mL	9.3535 mL
	15 mM	0.2494 mL	1.2471 mL	2.4943 mL	6.2357 mL
	20 mM	0.1871 mL	0.9353 mL	1.8707 mL	4.6767 mL
	25 mM	0.1497 mL	0.7483 mL	1.4966 mL	3.7414 mL
	30 mM	0.1247 mL	0.6236 mL	1.2471 mL	3.1178 mL
	40 mM	0.0935 mL	0.4677 mL	0.9353 mL	2.3384 mL
	50 mM	0.0748 mL	0.3741 mL	0.7483 mL	1.8707 mL
	60 mM	0.0624 mL	0.3118 mL	0.6236 mL	1.5589 mL
	80 mM	0.0468 mL	0.2338 mL	0.4677 mL	1.1692 mL
	100 mM	0.0374 mL	0.1871 mL	0.3741 mL	0.9353 mL

PD98059 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PD98059167869-21-8PD 98059PD-98059MEKERKAryl Hydrocarbon ReceptorAutophagyMitogen-activated protein kinase kinaseMAPKKMAP2KExtracellular signal regulated kinasesAhRInhibitorinhibitorinhibit

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PD98059

Customer Review

PD98059 Related Antibodies

333 Publications Citing Use of MCE PD98059

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References

Customer Review

PD98059 Related Antibodies

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Complete Stock Solution Preparation Table

PD98059 Related Classifications

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