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Chemical Structure| 193551-21-2 Chemical Structure| 193551-21-2

Structure of SB 239063
CAS No.: 193551-21-2

Chemical Structure| 193551-21-2

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SB 239063 is a potent, selective, and orally active p38 MAPK inhibitor with an IC50 of 44 nM for recombinant human p38α. It has similar inhibitory activity against p38α and p38β, with no effect on p38γ or p38δ. It is used for anti-asthma treatment and memory enhancement in conditions such as Alzheimer's disease.

Synonyms: SB 239063

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Product Details of SB 239063

CAS No. :193551-21-2
Formula : C20H21FN4O2
M.W : 368.40
SMILES Code : COC1=NC=CC(C2=C(N=CN2[C@H]3CC[C@H](O)CC3)C4=CC=C(F)C=C4)=N1
Synonyms :
SB 239063
MDL No. :MFCD03792786
InChI Key :ZQUSFAUAYSEREK-UHFFFAOYSA-N
Pubchem ID :5166

Safety of SB 239063

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of SB 239063

MAPK
TLR

Isoform Comparison

Biological Activity

Target
  • p38β

    p38β, IC50:44 nM

  • p38α

    p38α, IC50:44 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
bronchial rings 10^-6 M 1 hour SB239063 inhibited acetylcholine (ACh)-induced bronchial contraction, indicating that p38 MAPK plays an important role in the maximal isometric contractile response. PMC3331993
HaCaT cells 20 µmol/L 2 hours Evaluate the effect of SB 239063 on CuONP-induced cytotoxicity, results showed SB 239063 had no significant effect on cell viability PMC4200036
MEF cells 20 µmol/L 2 hours Evaluate the effect of SB 239063 on CuONP-induced cytotoxicity, results showed SB 239063 had no significant effect on cell viability PMC4200036
SOD1G93A motor neurons 2 μM Correct deficits in axonal retrograde transport in SOD1G93A motor neurons PMC5964181

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
mice endotoxin-induced liver injury model intraperitoneal injection 25 or 50 mg/kg Weekly To investigate the protective effect of SB 239063 on endotoxin-induced liver injury, results showed that SB 239063 significantly reduced liver enzyme levels, hepatocellular apoptosis, and leukocyte infiltration PMC1409872
mice MKP-1-/- mice and C57/BL6 mice in vitro organ bath 15mg/kg Weekly SB239063 inhibited bronchial contraction in both air- and ozone-exposed C57/BL6 and MKP-1-/- mice, indicating that p38 MAPK plays an important role in the maximal isometric contractile response. PMC3331993
Rats Myocardial infarction model Intramyocardial injection 10^-6 M 1 hour To test the inhibitory effect of PK-p38 i microspheres on p38 phosphorylation, superoxide production, and TNF-α generation in a myocardial infarction model, results showed that PK-p38 i significantly inhibited p38 phosphorylation at 3 and 7 days, and reduced superoxide and TNF-α levels, while free inhibitor and empty PK treatment had no effect. PMC2705946
Mice SOD1G93A mouse model Intraperitoneal injection 2 µM Single injection Correct deficits in axonal retrograde transport in SOD1G93A mice PMC5964181

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.71mL

0.54mL

0.27mL

13.57mL

2.71mL

1.36mL

27.14mL

5.43mL

2.71mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

[1]Strassburger M, Braun H, et al. 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. Eur J Pharmacol. 2008 Sep 11;592(1-3):55-61.

[2]Underwood DC, Osborn RR, et al. SB 239063, a potent p38 MAP kinase inhibitor, reduces inflammatory cytokine production, airways eosinophil infiltration, and persistence. J Pharmacol Exp Ther. 2000 Apr;293(1):281-8.

[3]Zarubin T, Han J. Activation and signaling of the p38 MAP kinase pathway. Cell Res. 2005 Jan;15(1):11-8. doi: 10.1038/sj.cr.7290257. PMID: 15686620.

[4]Underwood DC, Osborn RR, Kotzer CJ, Adams JL, Lee JC, Webb EF, Carpenter DC, Bochnowicz S, Thomas HC, Hay DW, Griswold DE. SB 239063, a potent p38 MAP kinase inhibitor, reduces inflammatory cytokine production, airways eosinophil infiltration, and persistence. J Pharmacol Exp Ther. 2000 Apr;293(1):281-8. PMID: 10734180.

[5]Legos JJ, McLaughlin B, Skaper SD, Strijbos PJ, Parsons AA, Aizenman E, Herin GA, Barone FC, Erhardt JA. The selective p38 inhibitor SB-239063 protects primary neurons from mild to moderate excitotoxic injury. Eur J Pharmacol. 2002 Jun 28;447(1):37-42. doi: 10.1016/s0014-2999(02)01890-3. PMID: 12106800.

[6]Strassburger M, Braun H, Reymann KG. 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. Eur J Pharmacol. 2008 Sep 11;592(1-3):55-61. doi: 10.1016/j.ejphar.2008.06.099. Epub 2008 Jul 3. PMID: 18638472.

[7]Joko T, Shiraishi A, Akune Y, Tokumaru S, Kobayashi T, Miyata K, Ohashi Y. Involvement of P38MAPK in human corneal endothelial cell migration induced by TGF-β(2). Exp Eye Res. 2013 Mar;108:23-32. doi: 10.1016/j.exer.2012.11.018. Epub 2012 Dec 17. PMID: 23257207.

 

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