Pd-98059

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CAS: 167869-21-8

Name:

Pd-98059

Other names:

2-(2-amino-3-methoxyphenyl)-4H-1-benzopyran-4-one; PD-98059; PD98059; PD 98,059; 2-(2-amino-3-methoxyphenyl)-4H-chromen-4-one; 2-(2-amino-3-methoxyphenyl)chromen-4-one

PD 98059 is a potent, selective and reversible cell permeable inhibitor of MEK-1 (MAPKK1 or MAPKs ) that binds to the inactive form of MEK-1, blocking MEK-1 activation and leading to inhibition of phosphorylation and the activation of MAP kinase. In PC12 pheochromocytoma cells, it produced complete blockage of any increase in MAPK activity (IC50 = 2 μM) produced by nerve growth factor. It has been shown to enhance self-renewal of embryonic stem cells and has been used to unravel the role of the MAPK cascade in biological systems. The compound has been reported to induce GSTA2 (glutathione S-transferase A2) production in H4IIE cells. PD 98059 has also been shown to enhance insulin-mediated increase in glutathione levels as well as, independent of MEK1 inhibition, elevate primary cultured rat hepatocyte glutathione levels.

Interactions

Description

UniProt ID

Protein: Mitogen-activated protein kinase 3, Gene: MAPK3
Protein: Mitogen-activated protein kinase 1, Gene: MAPK1
Protein: Dual specificity mitogen-activated protein kinase kinase 5, Gene: MAP2K5
Gene: MAP2K1
Protein: Dual specificity mitogen-activated protein kinase kinase 2, Gene: MAP2K2
Gene: MAP2K3
Protein: Dual specificity mitogen-activated protein kinase kinase 4, Gene: MAP2K4
Gene: MAP2K6
Protein: Mitogen-activated protein kinase kinase kinase 1, Gene: MAP3K1
Protein: Dual specificity mitogen-activated protein kinase kinase 7, Gene: MAP2K7

Toxicity

oral LD50 [mouse] mg/kg
Unavailable
oral LD50 [rat] mg/kg
Unavailable
oral LD50 [rabbit] mg/kg
Unavailable

Effects on organism

No data
Antibacterial

No

Antifungal

No

Antiviral

No

Longevity mechanisms activation

No data

Suppression of aging mechanisms

No data

Relation to biomarkers of Aging

Prevents neurite degeneration induced by fibrillar beta-amyloid in mature hippocampal neurons

10617113

Relation to aging associated genes

MAPK14MAPK3

Experimental conditions

Not available

Life Extension

Mean LS (%)
27.0
Median LS (%)
Mortality rate derease (%)
Max LS (%)
Cell CLS
Cell RLS

Concentration wth maximum effect

300-1000 mkM

More info about experiment

22363408
Opposite effectNo