PD98059

Cat. No.: HY-12028 Purity: 99.84%: FAQs
Data Sheet SDS COA Handling Instructions

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	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solution
10 mM * 1 mL in DMSO	USD 66	In-stock	Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL ready for reconstitution	USD 66	In-stock	Estimated Time of Arrival: December 31
Solid
10 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 132	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 228	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 259 publication(s) in Google Scholar

241 Publications Citing Use of MCE PD98059

: PD98059 purchased from MCE. 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 MCE. 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 MCE. 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 MCE. Usage Cited in: Mol Oncol. 2018 Mar;12(3):305-321. [Abstract]; Western blot analysis of the expression level of EGFR, Sp1, total and phosphorylated Erk1/2 proteins in cell lysates from two breast cancer cells pretreated with PD98059 and then stimulated with TGF-β for the indicated times

: PD98059 purchased from MCE. Usage Cited in: Cell Mol Life Sci. 2018 Mar;75(6):1117-1132. [Abstract]; Sertoli cells (SC) are pretreated with the PD98059 for 1 h followed by a 24-h treatment with MC-LR. Expression levels of MMP-8, c-Jun, c-Fos, p-ERK, ERK, p-JNK, and JNK are determined by western blotting.

: PD98059 purchased from MCE. Usage Cited in: Cell Mol Life Sci. 2018 Jul;75(14):2627-2641. [Abstract]; RAW264.7 macrophages are pre-treated with the inhibitor of ERK, JNK, P38, P65, and AKT signal pathway.Western blot analyzes the non- and phosphorylation of ERK, JNK, P38, P65, and AKT.

: PD98059 purchased from MCE. 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 MCE. Usage Cited in: J Agric Food Chem. 2018 Jun 27;66(25):6317-6325. [Abstract]; HepG2 cells are pre-incubated with 20 µM SB203580, SP600125 and PD98059 for 1 h and then treated with tangeretin(20µM) for 24 h.

: PD98059 purchased from MCE. 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 MCE. 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 MCE. Usage Cited in: World J Gastroenterol. 2018 Feb 21;24(7):819-832. [Abstract]; HSCs are pretreated with AICAR (500 μM), LY294002 (20 μM), PD98059 (10 μM), or Rapamycin (100 nM) for 2 h and then incubated with or without CoCl₂ (150 μM) for 12 h. Expression levels of HIF-1α and VEGF are measured by Western blot analysis;

: PD98059 purchased from MCE. 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 MCE. 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 MCE. Usage Cited in: Mol Cell Biochem. 2018 Feb;439(1-2):117-129. [Abstract]; Protein expression levels of E-cadherin N-cadherin, p-ERK, ERK, TGF-β1, p-Smad2, and p-Smad3 in each group are analyzed by western blotting.

: PD98059 purchased from MCE. Usage Cited in: Hum Mol Genet. 2017 Sep 15;26(18):3553-3563. [Abstract]; Immunofluorescence analysis for expression of the I-cell marker ΔNP63 on proximal sections of ureters explanted from E12.5 wildtype (control) embryos and cultured for 6 d in the presence of solvent (DMSO) (A), the AKT inhibitor (AKT-i) MK2206 (B), the P38 inhibitor (P38-i) SB203580 (C), the ERK1/2 inhibitor (ERK1/2-i) PD98059 (D) or combinations as indicated (E and F).

: PD98059 purchased from MCE. Usage Cited in: Mol Immunol. 2017 Jul;87:161-170. [Abstract]; Effect of TLR2 on autophagy activation via ERK1/2 signaling pathway activation in MG-infected RAW264.7 cells. RAW264.7 cells transfected with TLR2 siRNA/control siRNA is then infected with MG for 30 min prior to PD98059. The expression levels of Beclin1, LC3-II/I, p-JNK, p-ERK1/2 and p-p38 are examined by Western blot.

: PD98059 purchased from MCE. 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.

: PD98059 purchased from MCE. Usage Cited in: Biomed Res. 2017; 28 (8): 3383-3386; Effects of various protease inhibitors on HO-1 and P-gp protein expressions.

Featured Recommendations

•Related Screening Libraries:

View All MEK Isoform Specific Products:

View All Isoforms

MEK1 MEK2 MEK5 MEK

View All ERK Isoform Specific Products:

View All Isoforms

ERK ERK1 ERK2 ERK5 ERK8

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]^[3]

MEK1

2-7 μM (IC₅₀)

MEK2

50 μM (IC₅₀)

ERK1

ERK2

Autophagy

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].

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].

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

Appearance

Solid

Formula

C₁₆H₁₃NO₃

CAS No.

167869-21-8

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, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

DMSO : 33.33 mg/mL (124.70 mM; Need ultrasonic)

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

*Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 50% PEG300 50% saline
Solubility: 10 mg/mL (37.41 mM); Suspended solution; Need ultrasonic
2.

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

*All of the co-solvents are available by MCE.

Purity & Documentation

Purity: 99.94%

Select Batch:

Data Sheet (281 KB) SDS (392 KB)

COA (248 KB) LCMS (111 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]

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.

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Keywords:

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

Please select a local distributor ナミキ商事株式会社コスモ・バイオ株式会社
Product Name			Salutation
Applicant Name *			Email address *
Phone number *			Organization name *
Department *			Requested quantity *
Country or Region *
Remarks

Product Name			Lot #
Applicant Name *			Email address *
Phone number			Department *
Organization name *			Country or Region *
Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

PD98059

Customer Review

241 Publications Citing Use of MCE PD98059

Featured Recommendations

•Related Screening Libraries:

View All MEK Isoform Specific Products:

View All ERK Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

Request for HNMR Report