Home MAPK p38 MAPK inhibitor SB239063

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SB239063 p38 MAPK inhibitor

Cat.No.S7741

SB239063 is a potent and selective p38 MAPKα/β inhibitor with IC50 of 44 nM, showing no activity against the γ- and δ-kinase isoforms.
SB239063 p38 MAPK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 368.4

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Quality Control

Batch: S774101 DMSO]60 mg/mL]false]Ethanol]7 mg/mL]false]Water]Insoluble]false Purity: 99.85%
99.85

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
THP1 cells Function assay Inhibition of LPS-stimulated TNFalpha production in human THP1 cells, IC50=0.12 μM
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 60 mg/mL (162.86 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 7 mg/mL

Water : Insoluble

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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight 368.4 Formula

C20H21FN4O2

 Storage (From the date of receipt)
CAS No. 193551-21-2 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles COC1=NC=CC(=N1)C2=C(N=CN2C3CCC(CC3)O)C4=CC=C(C=C4)F

Mechanism of Action

Targets/IC50/Ki
p38α
(Cell-free assay)
44 nM
p38β
(Cell-free assay)
44 nM
In vitro
SB 239063 potently inhibits IL-1 and TNF-α production in LPS-stimulated human peripheral blood monocytes with IC50 of 120 and 350 nM, respectively. In oxygen-glucose-deprived hippocampal slice cultures, SB239063 strikingly reduces the levels of the pro-inflammatory cytokine IL-1beta, causes cell death after oxygen-glucose deprivation and significantly diminishes microglia activation. In human corneal endothelial cell, SB 239063 inhibits TGF-β(2) and FGF-2-induced cell migration.
In vivo
In both guinea pigs and mice, SB 239063 (10 mg/kg, p.o.) reduces antigen-induced airway eosinophilia. In air- and ozone-exposed C57/BL6 and MKP-1(-/-) mice, SB239063 inhibits bronchial contraction.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/23257207/

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