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Chemical Structure : BIM5078
Catalog No.: PC-72022Not For Human Use, Lab Use Only.
BIM5078 (BIM-5078) is a potent synthetic HNF4α antagonist, binds to HNF4α with high affinity (EC50=11.9 nM) and modulates HNF4α target genes and metabolic processes controlled by HNF4α.
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BIM 5078 (BIM-5078) is a potent synthetic HNF4α antagonist, binds to HNF4α with high affinity (EC50=11.9 nM) and modulates HNF4α target genes and metabolic processes controlled by HNF4α.
BIM 5078 potently repressed HNF4α expression in T6PNE and in the HepG2 hepatoma line, which has exceptionally high levels of HNF4α expression.
BIM 5078 also affected a subset of genes with no known HNF4α binding sites.
BIM5078 inhibited insulin gene expression, significantly decreased the association of E47 with the distal (E2) but not the proximal (E1) E-box of the insulin promoter, association of PDX-1 was significantly decreased.
| M.Wt | 351.761 | |
| Formula | C14H10ClN3O4S | |
| Appearance | Solid | |
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1. Alice Kiselyuk, et al. Chem Biol. 2012 Jul 27;19(7):806-18.
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