- InSolution PD 98059
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- $1.00 / 1KG
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2019-09-02
- CAS:167869-21-8
- Min. Order: 1KG
- Purity: 98%
- Supply Ability: 1lg; 2kg; 5kg; 10kg; 100kg
- InSolution PD 98059
-
- $1.00 / 1KG
-
2019-09-02
- CAS:167869-21-8
- Min. Order: 1KG
- Purity: 98%
- Supply Ability: 1lg; 2kg; 5kg; 10kg; 100kg
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| | PD 98059 Basic information |
| | PD 98059 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. | | InChIKey | QFWCYNPOPKQOKV-UHFFFAOYSA-N | | CAS DataBase Reference | 167869-21-8(CAS DataBase Reference) |
| Hazard Codes | Xn | | Risk Statements | 22 | | Safety Statements | 22-60-36 | | RIDADR | UN 2811 6.1/PG 3 | | WGK Germany | 3 | | HS Code | 29322090 |
| | PD 98059 Usage And Synthesis |
| 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 | PD 98059 is a selective inhibitor of MEK and blocker of MAPK. | | 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 | Room temperature | | 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 |
| | PD 98059 Preparation Products And Raw materials |
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