A potent inhibitor of p38 MAPK
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Doramapimod

Item No. 10460

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]-1-naphthalenyl]-urea
CAS Number
285983-48-4
Synonyms
  • BIRB-796
Molecular Formula
C31H37N5O3
Formula Weight
527.7
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMSO: 30 mg/mlEthanol: 3 mg/ml
λmax
211, 238, 303 nm
SMILES
O=C(NC1=CC(C(C)(C)C)=NN1C2=CC=C(C)C=C2)NC3=CC=C(OCCN4CCOCC4)C5=C3C=CC=C5
InChi Code
InChI=1S/C31H37N5O3/c1-22-9-11-23(12-10-22)36-29(21-28(34-36)31(2,3)4)33-30(37)32-26-13-14-27(25-8-6-5-7-24(25)26)39-20-17-35-15-18-38-19-16-35/h5-14,21H,15-20H2,1-4H3,(H2,32,33,37)
InChi Key
MVCOAUNKQVWQHZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $29

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    5 mg

    $55

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    10 mg

    $96

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    25 mg

    $169

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    Product Description

    Doramapimod is a highly potent inhibitor of p38 MAPK with a Kd value of 0.1 nM that blocks TNFα release in LPS-stimulated THP-1 cells with an IC50 value of 18 nM.1 At 10 μM, doramapimod inhibits JNK2α2 in vitro, but at the low concentration necessary to inhibit p38 MAPK, it does not affect the phosphorylation of JNK substrates in cells.2,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Pargellis, C., Tong, L., and Churchill, L. Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site. Nat. Struct. Biol. 9(4), 268-272 (2002).

    2. Bain, J., Plater, L., Elliot, M., et al. The selectivity of protein kinase inhibitors: A further update. Biochem. J. 408(3), 297-315 (2007).

    3. Kuma, Y., Sabio, G., Bain, J., et al. BIRB796 inhibits all p38 MAPK isoforms in vitro and in vivo. The Journal of Biological Chemisty 280(20), 19472-19479 (2005).