WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 401680
CAS#: 167869-21-8
Description: PD98059 also known as PD-98059, is a potent and selective inhibitor of MAP kinase kinase (also known as MAPK/ERK kinase or MEK kinase). It mediates its inhibitory properties by binding to the ERK-specific MAP kinase MEK, therefore preventing phosphorylation of ERK1/2 (p44/p42 MAPK) by MEK1/2. MAPK ERK1/2 is involved in TLR-induced production of cytokines.
MedKoo Cat#: 401680
Name: PD98059
CAS#: 167869-21-8
Chemical Formula: C16H13NO3
Exact Mass: 267.08954
Molecular Weight: 267.28
Elemental Analysis: C, 71.90; H, 4.90; N, 5.24; O, 17.96
Synonym: PD98059; PD-98059; PD 98059; PD098059
IUPAC/Chemical Name: 2-(2-amino-3-methoxyphenyl)-4H-chromen-4-one
InChi Key: QFWCYNPOPKQOKV-UHFFFAOYSA-N
InChi Code: InChI=1S/C16H13NO3/c1-19-14-8-4-6-11(16(14)17)15-9-12(18)10-5-2-3-7-13(10)20-15/h2-9H,17H2,1H3
SMILES Code: O=C1C=C(C2=CC=CC(OC)=C2N)OC3=C1C=CC=C3
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
| Biological target: | PD98059 is a MEK inhibitor with an IC50 of 5 µM. |
| In vitro activity: | To determine the antiproliferative effects of PD98059 on breast cancer cells, MCF-7 and MDA-MB-231 breast cancer cells were treated with 1, 5, 10 and 20 µM PD98059 for 24 h. As shown in Fig. 1A and B, after incubation of the MCF-7 and MDA-MB-231 cells with 1, 5, 10 and 20 µM PD98059 for 24 h, the expression of phosphorylated MEK1 which is an indicator of MEK1 activation was markedly decreased from 5 to 20 µM compared with the control group. PD98059 inhibited MCF-7 and MDA-MB-231 cell proliferation in a dose-dependent manner using MTT assay (Fig. 1C and D). For example, the cell growth inhibition ratio was increased from 4.7% at the dose of 1 µM to 33.1% at the dose of 50 µM in MCF-7 breast cancer cells. Similarly, the cell growth inhibition ratio was increased from 4.2% at the dose of 1 µM to 40.5% at the dose of 50 µM in the MDA-MB-231 breast cancer cells. Reference: Oncol Rep. 2017 Nov;38(5):3055-3063. https://www.spandidos-publications.com/or/38/5/3055 |
| In vivo activity: | In CCI (chronic constriction injury) exposed rats single intrathecal PD98059 (2.5 mcg) administration produced significant antiallodynic effect after 30 min as assessed at day 7 by the von Frey test (18.5 g ± 0.55, n = 10; Fig 4C and 4D). Single intrathecal PD98059 (2.5 mcg) administration enhanced morphine-induced analgesia (24.2 ± 0.63, n = 8, Fig 4C). Single intrathecal PD98059 (2.5 mcg) administration also enhanced buprenorphine-induced analgesia (23.25 ± 0.62, n = 7, Fig 4D). Reference: PLoS One. 2015 Oct 1;10(10):e0138583. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4591269/ |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 15.0 | 56.1 |
The following data is based on the product molecular weight 267.28 Batch specific molecular weights may vary from batch to batch due to the degree 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 | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | 1. Zhao Y, Ge CC, Wang J, Wu XX, Li XM, Li W, Wang SS, Liu T, Hou JZ, Sun H, Fang D, Xie SQ. MEK inhibitor, PD98059, promotes breast cancer cell migration by inducing β-catenin nuclear accumulation. Oncol Rep. 2017 Nov;38(5):3055-3063. doi: 10.3892/or.2017.5955. Epub 2017 Sep 13. PMID: 29048617. 2. Rojewska E, Popiolek-Barczyk K, Kolosowska N, Piotrowska A, Zychowska M, Makuch W, Przewlocka B, Mika J. PD98059 Influences Immune Factors and Enhances Opioid Analgesia in Model of Neuropathy. PLoS One. 2015 Oct 1;10(10):e0138583. doi: 10.1371/journal.pone.0138583. PMID: 26426693; PMCID: PMC4591269. |
| In vitro protocol: | 1. Zhao Y, Ge CC, Wang J, Wu XX, Li XM, Li W, Wang SS, Liu T, Hou JZ, Sun H, Fang D, Xie SQ. MEK inhibitor, PD98059, promotes breast cancer cell migration by inducing β-catenin nuclear accumulation. Oncol Rep. 2017 Nov;38(5):3055-3063. doi: 10.3892/or.2017.5955. Epub 2017 Sep 13. PMID: 29048617. |
| In vivo protocol: | 1. Rojewska E, Popiolek-Barczyk K, Kolosowska N, Piotrowska A, Zychowska M, Makuch W, Przewlocka B, Mika J. PD98059 Influences Immune Factors and Enhances Opioid Analgesia in Model of Neuropathy. PLoS One. 2015 Oct 1;10(10):e0138583. doi: 10.1371/journal.pone.0138583. PMID: 26426693; PMCID: PMC4591269. |
1: Huang CT, Huang DY, Hu CJ, Wu D, Lin WW. Energy adaptive response during parthanatos is enhanced by PD98059 and involves mitochondrial function but not autophagy induction. Biochim Biophys Acta. 2014 Mar;1843(3):531-43. PubMed PMID: 24321770.
2: Lee JM, Kim JD, Oh EJ, Oh SH, Lee JH, Im GI. PD98059-impregnated functional PLGA Scaffold for direct tissue engineering promotes chondrogenesis and prevents hypertrophy from mesenchymal stem cells. Tissue Eng Part A. 2014 Mar;20(5-6):982-91. doi: 10.1089/ten.TEA.2013.0290. Epub 2013 Dec 11. PubMed PMID: 24188591; PubMed Central PMCID: PMC3938927.
3: Pathania AS, Joshi A, Kumar S, Guru SK, Bhushan S, Sharma PR, Bhat WW, Saxena AK, Singh J, Shah BA, Andotra SS, Taneja SC, Malik FA, Kumar A. Reversal of boswellic acid analog BA145 induced caspase dependent apoptosis by PI3K inhibitor LY294002 and MEK inhibitor PD98059. Apoptosis. 2013 Dec;18(12):1561-73. doi: 10.1007/s10495-013-0889-4. PubMed PMID: 23948751.
4: Yao J, Qian C, Shu T, Zhang X, Zhao Z, Liang Y. Combination treatment of PD98059 and DAPT in gastric cancer through induction of apoptosis and downregulation of WNT/β-catenin. Cancer Biol Ther. 2013 Sep;14(9):833-9. doi: 10.4161/cbt.25332. Epub 2013 Jun 14. PubMed PMID: 23792588; PubMed Central PMCID: PMC3909552.
5: Han YH, Moon HJ, You BR, Yang YM, Kim SZ, Kim SH, Park WH. The MEK inhibitor PD98059 attenuates growth inhibition and death in gallic acid-treated Calu-6 lung cancer cells by preventing glutathione depletion. Mol Med Rep. 2010 May-Jun;3(3):519-25. doi: 10.3892/mmr_00000291. PubMed PMID: 21472273.
6: Cotrim CZ, Amado FL, Helguero LA. Estrogenic effect of the MEK1 inhibitor PD98059 on endogenous estrogen receptor alpha and beta. J Steroid Biochem Mol Biol. 2011 Mar;124(1-2):25-30. doi: 10.1016/j.jsbmb.2010.12.020. Epub 2011 Jan 12. PubMed PMID: 21236341.
7: Di Paola R, Crisafulli C, Mazzon E, Genovese T, Paterniti I, Bramanti P, Cuzzocrea S. Effect of PD98059, a selective MAPK3/MAPK1 inhibitor, on acute lung injury in mice. Int J Immunopathol Pharmacol. 2009 Oct-Dec;22(4):937-50. PubMed PMID: 20074457.
8: Di Paola R, Galuppo M, Mazzon E, Paterniti I, Bramanti P, Cuzzocrea S. 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. doi: 10.1016/j.phrs.2009.09.008. Epub 2009 Oct 9. PubMed PMID: 19819333.
9: Al-Shanti N, Stewart CE. PD98059 enhances C2 myoblast differentiation through p38 MAPK activation: a novel role for PD98059. J Endocrinol. 2008 Jul;198(1):243-52. doi: 10.1677/JOE-08-0151. Epub 2008 May 8. PubMed PMID: 18467380.
10: Kanda S, Kanetake H, Miyata Y. Long-term exposure of human renal carcinoma cells to PD98059 induces epithelial-mesenchymal transition-like phenotype and enhanced motility. Mol Cell Biochem. 2008 Feb;309(1-2):69-76. Epub 2007 Nov 14. PubMed PMID: 18000741.
