hepatic gene

GSK4112 (SR6452) is a Rev-erbα agonist with an EC50 of 0.4 μM and serves as a small molecule chemical probe for studying the cell biology of the nuclear heme receptor Rev-erbα.

SBI993 is an analog of SBI-477 and can be used as a biomarker to confirm the expected action of MondoA target gene expression in vivo. SBI993 reduces muscle TAG levels and hepatic steatosis.

HPG1860, an agonist of the farnesoid X receptor (FXR), induces luminescence in reporter gene assays utilizing HEK293T cells expressing human FXR, with an EC50 value of 18 nM. In vivo studies demonstrate that HPG1860 (administered at 1, 3, or 10 mg kg daily) reduces serum alanine aminotransferase (ALT) and total cholesterol levels in a mouse model of non-alcoholic steatohepatitis (NASH), which was induced by a high-fat diet and carbon tetrachloride (CCl4). Additionally, this compound decreases hepatic inflammation, fat levels, and fibrosis.

4-Epidoxycycline is a hepatic metabolite of the antibiotic doxycycline and lacks antibiotic properties in mice. In both in vitro assays and in vivo mouse models, 4-Epidoxycycline regulates HER2 gene expression similarly to doxycycline and exhibits comparable efficacy in tumor tissues, achieving over 95% tumor regression rates.

Anti-NASH agent 2 (compound 21) is an inhibitor of neolipogenesis activity and α-SMA gene expression. It improves hepatic steatosis, edema, inflammatory infiltration, and liver fibrosis in NASH mouse models.

Givinostat (ITF-2357) is an HDAC inhibitor with IC50 values of 198 nM for HDAC1 and 157 nM for HDAC3.

3,7-Dimethylfumarate (3,7-DMF) serves as an oral inhibitor of transforming growth factor-beta 1 (TGF-β1)-mediated hepatic stellate cell (HSC) activation. By inducing antioxidant gene expression and scavenging reactive oxygen species (ROS), 3,7-DMF is useful for researching liver fibrosis [1].