An HNF4α antagonist
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BIM5078

Item No. 12031

Product Insert (PDF)GC-MS (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[(2-chloro-5-nitrophenyl)sulfonyl]-2-methyl-1H-benzimidazole
CAS Number
337506-43-1
Molecular Formula
C14H10ClN3O4S
Formula Weight
351.8
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 3 mg/mlDMSO: 5 mg/mlDMSO:PBS (pH 7.2) (1:2): 0.3 mg/ml
λmax
245 nm
SMILES
CC1=NC2=CC=CC=C2N1S(C3=C(Cl)C=CC([N+]([O-])=O)=C3)(=O)=O
InChi Code
InChI=1S/C14H10ClN3O4S/c1-9-16-12-4-2-3-5-13(12)17(9)23(21,22)14-8-10(18(19)20)6-7-11(14)15/h2-8H,1H3
InChi Key
DLUVMRPVZILBOE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $69

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    10 mg

    $127

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    25 mg

    $297

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    50 mg

    $525

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    Cayman Chemical
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    Product Description

    HNF4α is a nuclear receptor transcription factor that controls the expression of many genes including those involved in glucose and lipid homeostasis and maintenance of epithelial differentiation. BIM5078 is an HNF4α antagonist that can repress the expression of known HNF4α target genes, inhibiting endogenous insulin expression in T6PNE cells with an IC50 value of 930 nM.1 BIM5078 binds directly to the ligand binding pocket of HNF4α with an EC50 value of 11.9 nM.1 However, BIM5078 has unfavorable pharmacokinetic properties including low plasma and microsomal stability (8% remaining after 3 hours and 32% after 1.25 hours, respectively), high binding to plasma proteins (98% bound after 4 hours), and low solubility (0.17 mg/ml after 18 hours).1 BI6015 (Item No. 12032) is a structural analog of BIM5078 developed for more favorable pharmacokinetics.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kiselyuk, A., Lee, S.H., Farber-Katz, S., et al. HNF4α antagonists discovered by a high-throughput screen for modulators of the human insulin promoter. Chem. Biol. 19(7), 806-818 (2012).