A p38α MAPK inhibitor
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p38α MAPK-IN-1

Item No. 40839

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3-(1,1-dimethylethyl)-1-(4-methylphenyl)-1H-pyrazol-5-yl]-N′-[4-[2-(4-morpholinyl)ethoxy]phenyl]-urea
CAS Number
443913-15-3
Synonyms
  • p38α MAPK Inhibitor 1
  • p38α Mitogen-activated Protein Kinase-IN-1
  • p38α Mitogen-activated Protein Kinase Inhibitor 1
Molecular Formula
C27H35N5O3
Formula Weight
477.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Sparingly soluble: 1-10 mg/mlDMSO: Soluble: ≥10 mg/mlEthanol: Soluble: ≥10 mg/ml
SMILES
O=C(NC1=CC(C(C)(C)C)=NN1C2=CC=C(C)C=C2)NC3=CC=C(C=C3)OCCN4CCOCC4
InChi Code
InChI=1S/C27H35N5O3/c1-20-5-9-22(10-6-20)32-25(19-24(30-32)27(2,3)4)29-26(33)28-21-7-11-23(12-8-21)35-18-15-31-13-16-34-17-14-31/h5-12,19H,13-18H2,1-4H3,(H2,28,29,33)
InChi Key
FRZNJFWQVYAVCE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    25 mg

    $620

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    Product Description

    p38α MAPK-IN-1 is an inhibitor of p38α MAPK (IC50 = 5,500 nM in a homogeneous time-resolved fluorescence (HTRF) assay).1 It inhibits TNF-α production induced by LPS in THP-1 cells (EC50 = 6,200 nM).2 p38α MAPK-IN-1 has been used in the study of p38α MAPK inhibitor binding interactions and kinetics.1,2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Klüter, S., Grütter, C., Naqvi, T., et al. Displacement assay for the detection of stabilizers of inactive kinase conformations. J. Med. Chem. 53(1), 357-367 (2010).

    2. Regan, J., Breitfelder, S., Cirillo, P., et al. Pyrazole urea-based inhibitors of p38 MAP kinase: From lead compound to clinical candidate. J. Med. Chem. 45(14), 2994-3008 (2002).