BI 6015 - CAS 93987-29-2
Category: Inhibitor
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Molecular Formula:
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BI 6015 is a hepatocyte nuclear factor 4α (HNF4α) antagonist that suppresses expression of known HNF4α target genes. BI 6015 produces cytotoxicity in a range of tumor cell lines, including human hepatocellular carcinoma.
Brife Description:
HNF4α antagonist
≥98% by HPLC
BI6015; BI 6015; BI-6015. 2-Methyl-1-[(2-methyl-5-nitrophenyl)sulfonyl]-1H-benzimidazole
Canonical SMILES:
1.Protein kinase C-dependent regulation of human hepatic drug transporter expression.
Mayati A;Le Vee M;Moreau A;Jouan E;Bucher S;Stieger B;Denizot C;Parmentier Y;Fardel O Biochem Pharmacol. 2015 Dec 15;98(4):703-17. doi: 10.1016/j.bcp.2015.10.007. Epub 2015 Oct 14.
Hepatic drug transporters are now recognized as major actors of hepatobiliary elimination of drugs. Characterization of their regulatory pathways is therefore an important issue. In this context, the present study was designed to analyze the potential regulation of human hepatic transporter expression by protein kinase C (PKC) activation. Treatment by the reference PKC activator phorbol 12-myristate 13-acetate (PMA) for 48h was shown to decrease mRNA expression of various sinusoidal transporters, including OATP1B1, OATP2B1, NTCP, OCT1 and MRP3, but to increase that of OATP1B3, whereas mRNA expression of canalicular transporters was transiently enhanced (MDR1), decreased (BSEP and MRP2) or unchanged (BCRP) in human hepatoma HepaRG cells. The profile of hepatic transporter mRNA expression changes in PMA-treated HepaRG cells was correlated to that found in PMA-exposed primary human hepatocytes and was similarly observed in response to the PKC-activating marketed drug ingenol mebutate. It was associated with concomitant repression of OATP1B1 and OATP2B1 protein expression and reduction of OATP, OCT1, NTCP and MRP2 activity. The use of chemical PKC inhibitors further suggested a contribution of novel PKCs isoforms to PMA-mediated regulations of transporter mRNA expression.
2.Hnf4α is involved in the regulation of vertebrate LC-PUFA biosynthesis: insights into the regulatory role of Hnf4α on expression of liver fatty acyl desaturases in the marine teleost Siganus canaliculatus.
Wang S;Chen J;Jiang D;Zhang Q;You C;Tocher DR;Monroig Ó;Dong Y;Li Y Fish Physiol Biochem. 2018 Jun;44(3):805-815. doi: 10.1007/s10695-018-0470-8. Epub 2018 Jan 19.
Long-chain polyunsaturated fatty acid (LC-PUFA) biosynthesis is an important metabolic pathway in vertebrates, especially fish, considering they are the major source of n-3 LC-PUFA in the human diet. However, most fish have only limited capability for biosynthesis of LC-PUFA. The rabbitfish (Siganus canaliculatus) is able to synthesize LC-PUFA as it has all the key enzyme activities required including Δ6Δ5 Fads2, Δ4 Fads2, Elovl5, and Elovl4. We previously reported a direct interaction between the transcription factor Hnf4α and the promoter regions of Δ4 and Δ6Δ5 Fads2, which suggested that Hnf4α was involved in the transcriptional regulation of fads2 in rabbitfish. For functionally investigating it further, a full-length cDNA of 1736-bp-encoding rabbitfish Hnf4α with 454 amino acids was cloned, which was highly expressed in intestine, followed by liver and eyes. Similar to the expression characteristics of its target genes Δ4 and Δ6Δ5 fads2, levels of hnf4α mRNA in liver and eyes were higher in fish reared at low salinity than those reared in high salinity. After the rabbitfish primary hepatocytes were, respectively, incubated with alverine, benfluorex or BI6015, which were anticipated agonists or antagonist for Hnf4α, the mRNA level of Δ6Δ5 and Δ4 fads2 displayed a similar change tendency with that of hnf4α mRNA.
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CAS 93987-29-2 BI 6015

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