Warning! Toxic compound!

Sp600125

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CAS: 129-56-6

Name:

Sp600125

Other names:

anthra(1,9-cd)pyrazol-6(2H)-one; 1,9-Pyrazoloanthrone; SP600125; Pyrazolanthrone; Pyrazoleanthrone; Anthra[1,9-cd]pyrazol-6(2H)-one; JNK Inhibitor II; C.I. 70300

SP600125 is a potent, selective and reversible inhibitor of the three JNK enzymes (c-Jun N-terminal kinases), with IC50 = 40 nM for JNK1 and JNK2, and 90 nM for JNK3. Inhibition is competitive with respect to ATP, and over 300-fold more selective for JNK as compared to ERK1 and p38-2 MAP kinases. SP600125 was shown to cause a dose-dependent inhibition of the phosphorylation of c-Jun, and thereby the expression of inflammatory genes COX-2, IFN-γ, IL-2, TNF-α, and block the activation and differentiation of primary human CD4 cell cultures. SP 600125 has also been shown to prevent apoptosis in an array of cell types, and inhibit autophagy in HeLa cells.

Interactions

Description

UniProt ID

Protein: Aryl hydrocarbon receptor, Gene: AHR
Protein: Tyrosine-protein kinase JAK1, Gene: JAK1
Protein: Tyrosine-protein kinase JAK2, Gene: JAK2
Protein: Tyrosine-protein kinase JAK3, Gene: JAK3
Protein: Mitogen-activated protein kinase 8, Gene: MAPK8
Protein: Mitogen-activated protein kinase 9, Gene: MAPK9
Protein: Mitogen-activated protein kinase 10, Gene: MAPK10
Protein: Cyclin-dependent kinase 2, Gene: CDK2
Protein: Serine/threonine-protein kinase Chk1, Gene: CHEK1
Protein: Serine/threonine-protein kinase Sgk1, Gene: SGK1

Toxicity

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

Effects on organism

Anti Cancer
Anti Amiloid
Neuroprotective
Antibacterial

No

Antifungal

No

Antiviral

No

Longevity mechanisms activation

No data

Suppression of aging mechanisms

No data

Relation to biomarkers of Aging

Data not available

Relation to aging associated genes

MAPK8MAPK9JAK2

Experimental conditions

Not available

Life Extension

Mean LS (%)
23.5
Median LS (%)
Mortality rate derease (%)
Max LS (%)
Cell CLS
Cell RLS

Concentration wth maximum effect

10 mM

More info about experiment

22363408
Opposite effectNo