ChemicalBook CAS DataBase List 167869-21-8

167869-21-8

Name	PD 98059
CAS	167869-21-8
Molecular Formula	C16H13NO3
MDL Number	MFCD00671789
Molecular Weight	267.28
MOL File	167869-21-8.mol

Chemical Properties

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.
InChI	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
InChIKey	QFWCYNPOPKQOKV-UHFFFAOYSA-N
SMILES	C1(C2=CC=CC(OC)=C2N)OC2=CC=CC=C2C(=O)C=1
CAS DataBase Reference	167869-21-8(CAS DataBase Reference)

Safety Data

Hazard Codes	Xn
Risk Statements	R22:Harmful if swallowed. less more
Safety Statements	22-60-36 less more
RIDADR	UN 2811 6.1/PG 3
WGK Germany	3
HS Code	29322090
Storage Class	10 - Combustible liquids

Hazard Information

Description

PD 98059 is a noncompetitive inhibitor of the MAPK pathway. 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. It inhibits Raf activation of MAP2K2 with an IC₅₀ value of 50 μM. PD 98059 also phosphorylates and activates AMP-activated protein kinase (AMPK) in a dose-dependent manner (EC₅₀ = 35 μM in HEK293 cells). 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 p140^trk 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

Spectrum Detail

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