A potent PDE4 inhibitor
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GSK256066

Item No. 28012

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-[[3-[(dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamide
CAS Number
801312-28-7
Molecular Formula
C27H26N4O5S
Formula Weight
518.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
λmax
251, 359 nm
SMILES
O=C(N(C)C)C1=CC=CC(S(C2=CC(C(NC3=CC=CC(OC)=C3)=C(C(N)=O)C=N4)=C4C(C)=C2)(=O)=O)=C1
InChi Code
InChI=1S/C27H26N4O5S/c1-16-11-21(37(34,35)20-10-5-7-17(12-20)27(33)31(2)3)14-22-24(16)29-15-23(26(28)32)25(22)30-18-8-6-9-19(13-18)36-4/h5-15H,1-4H3,(H2,28,32)(H,29,30)
InChi Key
JFHROPTYMMSOLG-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Cayman Chemical
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    Product Description

    GSK256066 is a potent phosphodiesterase 4 (PDE4) inhibitor (IC50s = 4.9, 3.2, 3.8, and 1.1 pM for PDE4A, PDE4B, PDE4C, and PDE4D, respectively).1 It is greater than 380,000-fold selective for PDE4 over PDE1-3, -5, and -6 and greater than 2,500-fold selective over PDE7. GSK256066 inhibits LPS-induced TNF-α production in human peripheral blood monocytes (IC50 = 0.01 nM) and human whole blood (IC50 = 126 pM). Intratracheal administration of GSK256066 inhibits LPS-induced pulmonary neutrophilia in rats (ED50 = 1.1 µg/kg). It inhibits ovalbumin-induced pulmonary eosinophilia in rats (ED50 = 0.4 µg/kg) and LPS-induced pulmonary neutrophilia in ferrets (ED50 = 18 µg/kg).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tralau-Stewart, C.J., Williamson, R.A., Nials, A.T., et al. GSK256066, an exceptionally high-affinity and selective inhibitor of phosphodiesterase 4 suitable for administration by inhalation: In vitro, kinetic, and in vivo characterization. J. Pharmacol. Exp. Ther. 337(1), 145-154 (2011).

    2. Nials, A.T., Tralau-Stewart, C.J., Gascoigne, M.H., et al. In vivo characterization of GSK256066, a high-affinity inhaled phosphodiesterase 4 inhibitor. J. Pharmacol. Exp. Ther. 337(1), 137-144 (2011).