A competitive inhibitor of JNK
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BI-78D3

Item No. 21183

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-(2,3-dihydro-1,4-benzodioxin-6-yl)-2,4-dihydro-5-[(5-nitro-2-thiazolyl)thio]-3H-1,2,4-triazol-3-one
CAS Number
883065-90-5
Synonyms
  • JNK Inhibitor X
  • c-Jun N-terminal Kinase Inhibitor X
Molecular Formula
C13H9N5O5S2
Formula Weight
379.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 33 mg/mlDMSO: 33 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml
SMILES
O=C1NN=C(SC2=NC=C([N+]([O-])=O)S2)N1C(C=C3)=CC4=C3OCCO4
InChi Code
InChI=1S/C13H9N5O5S2/c19-11-15-16-12(25-13-14-6-10(24-13)18(20)21)17(11)7-1-2-8-9(5-7)23-4-3-22-8/h1-2,5-6H,3-4H2,(H,15,19)
InChi Key
QFRLDZGQEZCCJZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $129

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    10 mg

    $236

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    25 mg

    $502

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    Cayman Chemical
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    Product Description

    BI-78D3 is an inhibitor of JNK (IC50 = 280 nM in a TR-FRET assay) that is competitive for JNK1 binding with pepJIP1, a JNK-interacting protein, with an IC50 value of 500 nM.1 It is selective for JNK, being 100-fold less active for the structurally similar MAPK family protein p38α and inactive at mammalian target of rapamycin (mTOR) or phosphatidylinositol 3-kinase α (PI3Kα). In a cell-based kinase assay, BI-78D3 inhibits c-Jun phosphorylation induced by TNF-α (EC50 = 12.4 µM). In a mouse model of type 2 diabetes, BI-78D3 (25 mg/kg) restores insulin sensitivity, reducing blood glucose levels when administered 30 minutes prior to insulin. BI-78D3 (30 µM) reduces contractions in human prostate strips induced by phenylephrine (Item Nos. 17205 | 18619) or norepinephrine (Item No. 16673) and reduces phosphorylation of c-Jun, a JNK substrate.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Stebbins, J.L., De, S.K., Machleidt, T., et al. Identification of a new JNK inhibitor targeting the JNK-JIP interaction site. Proc. Natl. Acad. Sci. USA 105(43), 16809-16813 (2008).

    2. Strittmatter, F., Walther, S., Gratzke, C., et al. Inhibition of adrenergic human prostate smooth muscle contraction by the inhibitors of c-Jun N-terminal kinase, SP600125 and BI-78D3. Br. J. Pharmacol. 166(6), 1926-1935 (2012).