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Signal Inhibitors and Activators

GSK256066

$1118.4/ 10mg
Quantity
Total: $1118

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Product Information

Kinase Inhibitor Name GSK256066
FormulaC27H26N4O5S
SolubilityDMSO ≥5 mg/mL   Water <1 mg/mL   Ethanol <1 mg/mL
Stability:
2 years       -20℃     Powder
1 week        -4℃     in DMSO
1 month     -80℃     in DMSO
CAS No.801312-28-7
Biological ActivityGSK256066 is an exceptionally high affinity and selective PDE4 inhibitor with an IC50 of 3.2 pM for PDE4B. GSK256066 suppressed tumor necrosis factor α production by lipopolysaccharide (LPS)-stimulated human peripheral blood monocytes with 0.01 nM IC50 (compared with IC50 values of 5, 22, and 389 nM for roflumilast, tofimilast, and cilomilast, respectively) and by LPS-stimulated whole blood with 126 pM IC50. GSK256066 also inhibited LPS-induced increases in exhaled nitric oxide (ED50=35 µg/kg). In addition, GSK256066 prevented pulmonary eosinophilia in rats exposed to ovalbumin (ED50=0.4 μg/kg). In ferrets, inhaled GSK256066 inhibited LPS-induced pulmonary neutrophilia (ED50=18 μg/kg) and no emetic episodes were observed. [1][2]
M.W.518.58
ReferencesIn vivo characterization of GSK256066, a high-affinity inhaled phosphodiesterase 4 inhibitor. Nials AT et al. J Pharmacol Exp Ther. 2011 Apr;337(1):137-44.
The inhaled phosphodiesterase 4 inhibitor GSK256066 reduces allergen challenge responses in asthma. Singh D et al. Respir Res. 2010 Mar 1;11:26.
The pharmacological and toxicological properties of this product have not been fully investigated. Exercise caution in use and handling. This product must not be used in humans.
Price1118.4$
Research AreaStem Cells Cancer Cardiovascular Cell Biology Epigenetics & Nuclear Signaling Developmental Biologys Immunology Drug Discovery Products Metabolism Neuroscience Signal Transduction
an exceptionally high affinity and selective PDE4 inhibitor with an IC50 suppressed tumor necrosis factor α production by human peripheral blood monocytes with 0.01 nM IC50 (compared with roflumilast, tofimilast, and cilomilast, respectively) and by LPS-stimulated GSK256066 also inhibited LPS-induced increases in exhaled nitric GSK256066 prevented pulmonary eosinophilia in rats exposed
an exceptionally high affinity and selective PDE4 inhibitor with an IC50 suppressed tumor necrosis factor α production by human peripheral blood monocytes with 0.01 nM IC50 (compared with roflumilast, tofimilast, and cilomilast, respectively) and by LPS-stimulated GSK256066 also inhibited LPS-induced increases in exhaled nitric GSK256066 prevented pulmonary eosinophilia in rats exposed
GSK256066 | EnoGene Biotech Co. Ltd