SB 239063 Property

Melting point:

206-207.2 °C

storage temp. 

2-8°C

solubility 

DMSO: 11 mg/mL

form 

White solid

color 

white

InChIKey

ZQUSFAUAYSEREK-WKILWMFISA-N

Safety

Safety Statements 

22-24/25

WGK Germany 

3

RTECS 

GV9458000

HS Code 

2933599590

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P330Rinse mouth.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P362Take off contaminated clothing and wash before reuse.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

SB 239063 Chemical Properties,Usage,Production

Uses

SB239063 is neuroprotective, decreases the number of activated microglia and facilitates neurogenesis in oxygen-glucose-deprived hippocampal slice cultures. A protein kinase inhibitor

Uses

SB 239063 has been used to determine the roles of c-Jun N-terminal kinase (JNK), p38 MAP kinase, and extracellular signal regulated protein kinase (ERK)/p42/p44 mitogen activated protein kinase (MAPK) on the viability and apoptosis of cardiomyocytes under glutathione S-transferase (GST) inhibition. It has also been used in neuron-microglia conditioned media (CM) experiments and pharmacokinetics.

Definition

ChEBI: A member of the class of imidazoles carrying 4-hydroxycyclohexyl, 4-fluorophenyl and 2-methoxypyrimidin-4-yl substituents at positions 1, 4 and 5 respectively.

General Description

SB 239063 helps to decrease neutrophilia, inflammatory cytokines, matrix metallopeptidase 9 (MMP-9) and fibrosis in the lung.

Hazard

A poison by ingestion.

Biological Activity

Potent and selective p38 MAP kinase inhibitor (IC 50 = 44 nM for p38a). Displays > 220-fold selectivity over ERK, JNK1 and other kinases; ~ 3-fold more selective than SB 203580 (4-[5-(4-Fluorophenyl)-2-[4-(methylsulfonyl)phenyl]-1H-i midazol-4-yl]pyridine and 4-[5-(4-Fluorophenyl)-2-[4-(methylsulphonyl)phenyl]-1H- imidazol-4-yl]pyridine hydrochloride ). Reduces inflammatory cytokine production and is neuroprotective following oral administration in vivo .

Biochem/physiol Actions

Potent p38 MAP kinase inhibitor. Selective for α and β. No activity against γ and δ isoforms.

in vitro

in oxygen-glucose-deprived hippocampal slice cultures, treatment with 20 μm and 100 μm sb239063 significantly reduced the levels of the pro-inflammatory cytokine il-1β and reduced cell death after oxygen-glucose deprivation and strikingly diminished microglia activation[2].

in vivo

oral administration of 3–30 mg/kg sb 239063 given twice a day dose-dependently inhibited airway neutrophil infiltration and interleukin (il)-6 levels 48 h after lipopolysaccharide (lps) inhalation [1]. in a bleomycin-induced pulmonary fibrosis model rats, sb 239063 treatment (2.4 or 4.8 mg/day via osmotic pump) significantly inhibited bleomycin-induced right ventricular hypertrophy (indicative of secondary pulmonary hypertension) and increased in lung hydroxyproline synthesis (indicative of collagen synthesis and fibrosis) (1). in conscious guinea pigs, administration of sb 239063 (10 or 30 mg/kg p.o.) showed approximately 50% inhibition of oa-induced pulmonary eosinophil influx, measured by bal 24 h after antigen(1). orally administration of sb 239063 (30 mg/kg) attenuated il-6 bronchoalveolar lavage fluid concentrations (> 90% inhibition) and mmp-9 activity (64% inhibition) measured 6 h after lps exposure. in guinea pig cultured alveolar macrophages, sb 239063 inhibited lps-induced il-6 production with ic50 of 362 nm. in lipopolysaccharide-stimulated human peripheral blood monocytes, sb 239063 inhibited il-1 and tnf-α production with an ic50 of 0.12 and 0.35 μm, respectively(1).

storage

Desiccate at +4°C

References

[1] underwood d c, osborn r r, bochnowicz s, et al. sb 239063, a p38 mapk inhibitor, reduces neutrophilia, inflammatory cytokines, mmp-9, and fibrosis in lung[j]. american journal of physiology-lung cellular and molecular physiology, 2000, 279(5): l895-l902.
[2] strassburger m, braun h, reymann k g. anti-inflammatory treatment with the p38 mitogen-activated protein kinase inhibitor sb239063 is neuroprotective, decreases the number of activated microglia and facilitates neurogenesis in oxygen–glucose-deprived hippocampal slice cultures[j]. european journal of pharmacology, 2008, 592(1): 55-61.