A potent, cell-permeable inhibitor of ERK1/2
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FR180204

Item No. 15544

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-(2-phenylpyrazolo[1,5-a]pyridin-3-yl)-1H-pyrazolo[3,4-c]pyridazin-3-amine
CAS Number
865362-74-9
Synonyms
  • ERK Inhibitor II
Molecular Formula
C18H13N7
Formula Weight
327.3
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:1): 0.5 mg/mlDMSO: 25 mg/ml
λmax
252, 299, 409 nm
SMILES
NC1=NNC(N=N2)=C1C=C2C3=C4N(N=C3C5=CC=CC=C5)C=CC=C4
InChi Code
InChI=1S/C18H13N7/c19-17-12-10-13(20-22-18(12)23-21-17)15-14-8-4-5-9-25(14)24-16(15)11-6-2-1-3-7-11/h1-10H,(H3,19,21,22,23)
InChi Key
XVECMUKVOMUNLE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $69

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    5 mg

    $132

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    10 mg

    $233

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    25 mg

    $525

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    Product Description

    FR180204 is a potent cell-permeable inhibitor of ERK1 and ERK2 (Ki = 310 and 140 nM, respectively).1 It is much less effective against p38α (IC50 = 10 µM) and does not inhibit a range of other serine/threonine or tyrosine kinases.1 FR180204 blocks ERK-mediated signaling from TGF-β to AP-1 (IC50 = 3.1 μM).1 It attenuates delayed-type hypersensitivity in collagen-immunized mice and ameliorates collagen-induced arthritis in mice.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ohori, M., Kinoshita, T., Okubo, M., et al. Identification of a selective ERK inhibitor and structural determination of the inhibitor-ERK2 complex. Biochem. Biophys. Res. Commun. 336(1), 357-363 (2005).

    2. Ohori, M., Takeuchi, M., Maruki, R., et al. FR180204, a novel and selective inhibitor of extracellular signal-regulated kinase, ameliorates collagen-induced arthritis in mice. Naunyn Schmiedebergs Arch. Pharmacol. 374(4), 311-316 (2007).