| Identification | More | [Name]
PD 98059 | [CAS]
167869-21-8 | [Synonyms]
CS-398
PD 98059
PD090859
PD 098,059
PD 98059 NEW
Amino chromone
PD 98059, 99+%
PD 98059, >=98%
PD-98059/PD98059
PD 98059 USP/EP/BP
InSolution? PD 98059
PD 98059 in Solution
PD 98059 - NSC 679828
2'-AMINO-3'-METHOXYFLAVONE
2-(2-AMino-3-Methoxyphenyl)chroMone
PD 98059 - CAS 167869-21-8 - Calbiochem
2-(2-Amino-3-methoxyphenyl)chromone >
2-(2-AMINO-3-METHOXY-PHENYL)CHROMEN-4-ONE
2-(2-AMINO-3-METHOXYPHENYL)-4H-CHROMEN-4-ONE
2-(2-AMINO-3-METHOXYPHENYL)-4H-1-BENZOPYRAN-4-ONE
InSolution PD 98059 - CAS 167869-21-8 - Calbiochem
4H-1-Benzopyran-4-one, 2-(2-amino-3-methoxyphenyl)-
4H-1-Benzopyran-4-one,2-(2-amino-3-methoxyphenyl)-(9CI)
PD 098,059 (2-(2-AMINO-3-METHOXYPHENYL)- 4H-1-BENZOPYRAN-4-ONE
PD 98059
2-(2-Amino-3-methoxyphenyl)-4H-1-benzopyran-4-one
2-(2-Amino-3-methoxy-phenyl)chromen-4-one, 98%, a non-ATP competitive MEK inhibitor
2-(2-Amino-3-methoxyphenyl)-4H-1-benzopyran-4-one PD 98059 | [Molecular Formula]
C16H13NO3 | [MDL Number]
MFCD00671789 | [Molecular Weight]
267.28 | [MOL File]
167869-21-8.mol |
| Chemical Properties | Back Directory | [Melting point ]
164～165℃ | [Boiling point ]
453.1±45.0 °C(Predicted) | [density ]
1.300±0.06 g/cm3(Predicted) | [storage temp. ]
−20°C
| [solubility ]
ethanol: 0.6 mg/mL
| [form ]
solid
| [pka]
1.21±0.10(Predicted) | [color ]
yellow
| [Stability:]
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. | [InChIKey]
QFWCYNPOPKQOKV-UHFFFAOYSA-N | [CAS DataBase Reference]
167869-21-8(CAS DataBase Reference) |
| Hazard Information | Back Directory | [Description]
PD 98059 is a noncompetitive inhibitor of the MAPK pathway.1,2 It prevents the activation of MEK by Raf or MEK kinase (a MAP3K) with an IC50 value of 2-7 μM but does not inhibit Raf-activated MAP2K1.3 It inhibits Raf activation of MAP2K2 with an IC50 value of 50 μM.3 PD 98059 also phosphorylates and activates AMP-activated protein kinase (AMPK) in a dose-dependent manner (EC50 = 35 μM in HEK293 cells).4 It increases the ratios of ADP to ATP and AMP to ATP and increases phosphorylation of the AMPK target acetyl-CoA carboxylase (ACC). | [Uses]
A selective inhibitor of MEK and blocker of MAP | [Definition]
ChEBI: A member of the class of monomethoxyflavones that is 3'-methoxyflavone bearing an additional amino substituent at position 2' | [General Description]
Selective, reversible, and cell-permeable inhibitor of MAP kinase kinase (MEK) that acts by inhibiting the activation of MAP kinase and subsequent phosphorylation of MAP kinase substrates. Pretreatment of PC-12 cells with PD 98059 completely blocks the 4-fold increase in MAP kinase activity produced by nerve growth factor (NGF; IC50 = 2 μM); however, it has no effect on NGF-dependent tyrosine phosphorylation of the p140trk receptor or its substrate Shc and does not block NGF-dependent activation of PI 3-kinase. Blocks LPS-induced activation of TNF-α gene expression. Inhibits cell growth and reverses the phenotype of ras-transformed BALB3T3 mouse fibroblasts and rat kidney cells. A 5 mg/ml solution of PD 98059 (Cat. No. 513001) in anhydrous DMSO is also available. | [Biological Activity]
Specific inhibitor of mitogen-activated protein kinase kinase (MAPKK / MEK). Acts by binding to the inactivated form of MEK, thereby preventing its phosphorylation by cRAF or MEK kinase (IC 50 = 2-7 μ M). Inhibits cell growth and proliferation in acute myelogenous leukemia (AML) cell lines; causes G 1 arrest by blocking p53-dependent p21 induction. Also available as part of the MAPK Cascade Inhibitor Tocriset™ and MAPK Inhibitor Tocriset™ . | [Biochem/physiol Actions]
PD 98,059 is a flavonoid and specific inhibitor of mitogen-activated protein kinase kinase (MAPKK). In mice, PD 98,059 helps to block zymosan stimulated organ dysfunction syndrome and non-septic shock. It is known to inhibit in vitro hypertrophy. PD 98,059 also induces cartilage formation in mesenchymal stromal cells. | [storage]
4°C, protect from light | [References]
1) Alessi et al. (1995), PD 098059 is a specific inhibitor of the activation of mitogen-activated protein kinase kinase in vitro and in vivo; J. Biol. Chem., 270 27489
2) Dudley et al. (1995), A synthetic inhibitor of the mitogen-activated protein kinase cascade; Proc. Natl. Acad. Sci., 92 7686
3) Hotokezaka et al. (2002) U0126 and PD98059, specific inhibitors of MEK, accelerate differentiation of RAW264.7 cells into osteoclast-like cells; J. Biol. Chem., 277 47366
4) Xiaoxia et al. (2004) BMP4 supports self-renewal of embryonic stem cells by inhibiting mitogen-activated protein kinase pathways; Proc. Natl. Acad. Sci. USA 101 6027 |
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