BIM5078
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
EC50: 11.9 nM for HNF4α
BIM5078 is a HNF4α antagonist.
Hepatocyte nuclear factor (HNF)4α is a key regulator of gene expression in cell types playing a important role in metabolic homeostasis, such as hepatocytes, enterocytes, as well as pancreatic β cells.
In vitro: The EC50 of BIM5078 was calculated to be 11.9 nM and further analyses of the data using the Hill equation showed that the Hill coefficient for BIM5078 was 0.9, consistent with a single binding complex between BIM5078 and HNF4α. In docking study, the high GoldScore indicated that it was reasonable for BIM5078 to bind in the LBP in a position similar to that of the putative endogenous ligand. Moreover, BIM5078 could potently repress HNF4α expression in T6PNE, the murine insulinoma cell line MIN6, and in the HepG2 hepatoma line, which had exceptionally high levels of HNF4α expression [1].
In vivo: BI6015, a analog of BIM5078, could induce a loss of HNF4α protein in the liver, but not in the intestine or kidney, which was consistent with the in vitro effects of BIM5078 on HNF4α expression both in human- and murine-derived cell lines. In addition, no difference in the cell number expressing the proliferation marker Ki67 was observed in liver, intestine, or kidney with BI6015, when compared with vehicle-treated animals [1].
Clinical trial: Up to now, BIM5078 is still in the preclinical development stage.
Reference:
[1] A. Kiselyuk, S. H. Lee, S. Farber-Katz, et al. HNF4α antagonists discovered by a high-throughput screen for modulators of the human insulin promoter. Chemistry & Biology 19, 806-818 (2012).
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 351.8 |
Cas No. | 337506-43-1 |
Formula | C14H10ClN3O4S |
Solubility | ≤5mg/ml in DMSO;3mg/ml in dimethyl formamide |
Chemical Name | 1-[(2-chloro-5-nitrophenyl)sulfonyl]-2-methyl-1H-benzimidazole |
SDF | Download SDF |
Canonical SMILES | CC1=NC2=CC=CC=C2N1S(C3=C(Cl)C=CC([N+]([O-])=O)=C3)(=O)=O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |