SB203580

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CAS: 152121-47-6

Name:

SB203580

Other names:

SB-203580; RWJ 64809; 4-(4-Fluorophenyl)-2-(4-methylsulfinylphenyl)-5-(4-pyridyl)1H-imidazole

SB 203580, a pyridinyl imidazole, has been observed to suppress p38 mediated activation of MAPKAP kinase-2 (MAPKAPK-2 or MK2), yet does not disrupt JNK activity.Mitogen-activated protein kinases (MAPK) are a group of serine and threonine-specific kinases sensitive to cellular stress, heat shock, and proinflammatory cytokines. p38 (p38 MAPK) is crucial for normal inflammatory and immune responses as it regulates the expression of varying cell surface receptors, cytokines and transcription factors. SB 203580 inhibits heat shock protein 27 (HSP 27) phosphorylation and has been shown to induce the activation of Raf-1. SB 203580 has also been shown to inhibit phosphoinositide-dependent protein kinase 1 (PKB Kinase), consequently preventing the activation of PKB/Akt. SB 203580 is a useful tool to assess the physiological roles of p38, and for deriving and maintaining embryonic stem cells. SB 203580 is an inhibitor of p38 α, p38 β, Cox-1, Cox-2, GSK, TXA Synthase and RICK.

Interactions

Description

UniProt ID

Protein: Serine/threonine-protein kinase A-Raf, Gene: ARAF
Protein: Arachidonate 5-lipoxygenase, Gene: ALOX5
Protein: Serine/threonine-protein kinase B-raf, Gene: BRAF
Protein: Bone morphogenetic protein 2, Gene: BMP2
Protein: RAF proto-oncogene serine/threonine-protein kinase, Gene: RAF1
Protein: Proto-oncogene tyrosine-protein kinase Src, Gene: SRC
Protein: Casein kinase I isoform delta, Gene: CSNK1D
Protein: Cholecystokinin receptor type A, Gene: CCKAR
Protein: Equilibrative nucleoside transporter 1, Gene: SLC29A1
Protein: Cyclin-G-associated kinase, Gene: GAK
Protein: Glucagon receptor, Gene: GCGR
Protein: Mitogen-activated protein kinase 9, Gene: MAPK9
Protein: Tyrosine-protein kinase Lck, Gene: LCK
Protein: Mitogen-activated protein kinase 14, Gene: MAPK14
Protein: Mitogen-activated protein kinase 11, Gene: MAPK11
Protein: Mitogen-activated protein kinase 13, Gene: MAPK13
Protein: Mitogen-activated protein kinase 12, Gene: MAPK12
Protein: Receptor-interacting serine/threonine-protein kinase 2, Gene: RIPK2
Protein: RAC-alpha serine/threonine-protein kinase, Gene: AKT1

Toxicity

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

Effects on organism

Anti Inflammation
Neuroprotective
Cardioprotective
Antibacterial

No

Antifungal

No

Antiviral

No

Longevity mechanisms activation

No data

Suppression of aging mechanisms

No data

Relation to biomarkers of Aging

Accelerated aging of Werner syndrome fibroblasts can be prevented by treatment with the p38 kinase inhibitor SB203580

20536832

Relation to aging associated genes

SHC1MAPK14AKT1MAPK9

Experimental conditions

Not available

Life Extension

Mean LS (%)
30.3
Median LS (%)
Mortality rate derease (%)
Max LS (%)
Cell CLS
Cell RLS

Concentration wth maximum effect

300 mkM

More info about experiment

22363408
Opposite effectNo