human hepg2

Relacorilant is a selective and orally bioavailable antagonist of glucocorticoid receptor(Ki of 7.2 nM in HepG2 TAT assay, and also shows Kis of 12, 81.2, 210 nM for rat, human and monkey glucocorticoid receptor in cell-based assay, respectively). Relacorilant has the potential for Cushing's syndrome treatment.

Polyphyllin D induces apoptosis via the mitochondrial apoptotic pathway as evidenced by decreased Bcl-2 expression levels, disruption of MMP and increased Bax, cytochrome C, and cleaved-caspase-3 levels. Polyphyllin D has an anti-angiogenic effect. Polyphyllin D has toxicity in human RBCs as well as its underlying mechanism for the hemolysis and eryptosis erythroptosis. Polyphyllin D has strong anticancer activity, can overcome drug resistance in R-HepG2 cells and elicit programmed cell death via mitochondrial dysfunction.

Azalanstat (RS 21607) is an orally available selective mammalian lanosterol 14-alpha-demethylase inhibitor with hypocholesterolemic activity that inhibits cholesterol synthesis in HepG2 cells, human fibroblasts, hamster hepatocytes, and hamster livers through inhibition of the cytochrome P450 enzyme, lanosterol 14 alpha demethylase.

Diosmetin (Luteolin 4-methyl ether) has been found to act as a weak TrkB receptor agonist.

Tolvaptan (OPC-41061) is an orally bioavailable, selective, arginine vasopressin receptor 2 (V2, AVPR2) antagonist that can be used to treat hyponatremia.

Guanosine 5'-diphosphate disodium salt (5'-GDP-Na2) is a nucleoside diphosphate, is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulating the interleukin-6 (IL-6) stat-3 pathway.

5,6-Benzoflavone (β-Naphthoflavone) is an exogenous ligand for the aryl hydrocarbon receptor, which disrupts zinc homeostasis in human hepatocellular carcinoma HepG2 cells. 5,6-Benzoflavone (β-Naphthoflavone) possesses anti-inflammatory and antioxidant activities, inhibits LPS-induced inflammation through the AKT Nrf-2 HO-1-NF-kappaB signaling axis, inhibits TNF-α-induced ICAM-1 and VCAM-1 expression, which can be used to study neurodegenerative diseases.

CAY10566 shows excellent cellular activity in blocking the conversion of saturated long-chain fatty acid-CoAs (LCFA-CoAs) to monounsaturated LCFA-CoAs in HepG2 cells (IC50=7.9 nM or 6.8 nM). CAY10566 is a potent, orally bioavailable and selective stearoyl

Rotundic acid (Rutundic acid), a natural compound, exhibit cytotoxic activities toward human hepatocellular carcinoma (HepG2), malignant melanoma (A375), SCLC (NCI-H446), breast cancer (MCF-7), and colon cancer (HT-29) cell lines.

1. Ganoderic acid A exhibits antitumor activity, mediated through its inhibitory effect on nuclear transcription factor-kappaB and activator protein-1. 2. Ganoderic acid A can induce proliferation inhibition, apoptosis and suppression of invasion in human

LysRs-IN-2 is a lysine tRNA synthetase (KRS) inhibitor with antiparasitic activity that inhibits Plasmodium falciparum KRS (PfKRS) and Cryptosporidium minum KRS (CpKRS), and is used in the study of malaria infections.

Neriifolin (17β-Neriifolin), a cardiac glycoside extracted from the unripe fruit of Cerbera manghas, is a Na+K+-ATPase inhibitor with anticancer activity that inhibits cell proliferation by suppressing HOXA9-dependent gene expression and inducing apoptosis in the human acute myeloid cell line, THP-1. Neriifolin induces cell cycle arrest and apoptosis in human hepatocellular carcinoma HepG2 cells and can be used in prostate cancer research.

SLC13A5-IN-1 is a selective inhibitor of the sodium-citrate co-transporter (SLC13A5) that completely blocks the uptake of 14C-citrate, with an IC50 of 0.022 μM in HepG2 cells.

Gardiquimod is a TLR7 8 agonist. When used at concentrations below 10 μM, Gardiquimod specifically activates TLR7. Gardiquimod could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells.

CP-640186 is an isozyme-nonselective Acetyl-CoA carboxylase (ACCase) inhibitor. The IC50s of CP-640186(CP 640186) is 53 nM and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2 respectively.

SET-171 is a JNK (c-Jun N-terminal kinase) inhibitor that exhibits significant anticancer activity by suppressing the expression of hepatic pyruvate kinase (PKL) and offers potential in regulating lipid metabolism. In antitumor studies, SET-171 shows notable cytotoxicity against human liver cancer cell lines HepG2 and Huh7, with IC50 values of 8.82 μM and 2.97 μM, respectively. Additionally, in research related to non-alcoholic fatty liver disease (NAFLD), SET-171 significantly reduces triglyceride (TAG) levels and inhibits the expression of proteins associated with steatosis. This compound holds promise for hepatocellular carcinoma (HCC) and NAFLD research.

MI-883 is an orally active Constitutive Androstane Receptor (CAR, EC50=73 nM) agonist and a Pregnane X Receptor (PXR, IC50=0.1 μM) antagonist. It enhances CAR LBD assembly (EC50=0.38 µM) and activates the CAR3 variant (EC50=0.074 µM), inducing CYP2B6 mRNA expression in HepaRG and primary human hepatocytes. Additionally, MI-883 inhibits the basal activity of PXR (IC50=2.03 µM) and reduces CYP3A4 mRNA expression in transiently transfected HepG2 cells. It also regulates cholesterol metabolism and bile acid excretion, improving hypercholesterolemia in mouse models.

Enterocin (Vulgamycin) is a bacteriocin and polyketide antibiotic produced by Enterococcus spp. bacteria that is readily degraded by proteolytic hydrolysis in the gastrointestinal tract and is capable of controlling foodborne pathogens such as L. monocytogenes, Listeria, and Bacillus through human consumption. and and Bacillus.

YM-53601 is a potent squalene synthase (SQS) inhibitor that inhibits adipogenic biosynthesis and lipid secretion in rodents.YM-53601 is a cholesterol-lowering agent that inhibits farnesyl diphosphate farnesyltransferase 1 (FDFT1).YM-53601 exhibits potential antiviral activity and enhances adriamycin-mediated HCC arrest and cell death in vivo. MJN228 is a lipid-based enzyme.

meso-Dihydroguaiaretic acid is an LXR-α antagonist, it inhibits hepatic lipid accumulation by activating AMP-activated protein kinase in human HepG2 cells.

CP-868388 free base (CP-868388) is an orally active, potent and selective PPARα agonist with hypolipidemic and anti-inflammatory activity for the study of dyslipidemia.

SC-III3 is a novel scopoletin derivative, induces autophagy of human hepatoma HepG2 cells through AMPK/mTOR signaling pathway by acting on mitochondria. SC-III3 reduces the viability of HepG2 cells and tumor growth of HepG2 xenograft mouse model. It induc

Pinolenic acid is a polyunsaturated fatty acid found in Korean pine (Pinus orientalis) and maritime pine (Pinus pinaster) seed oils, which exhibit lipid-lowering properties. In transgenic mice expressing human ApoA1, a diet containing maritime pine seed oil (MPSO) reduced high-density lipoprotein and ApoA1 levels and diminished cholesterol efflux in vitro. Korean pine seed oil supplements may aid in reducing obesity by decreasing appetite, as evidenced by increased levels of satiety hormones CCK and GLP-1 and reduced desire to eat. Pinolenic acid, which is not metabolically converted to arachidonic acid, can lower arachidonic acid levels in the phosphatidylinositol fraction of HepG2 cells from 15.9% to 7.0%. The neutral, more lipophilic form of pinolenic acid is pinolenic acid ethyl ester.

HT-2 toxin-13C22is intended for use as an internal standard for the quantification of HT-2 toxin by GC- or LC-MS. HT-2 toxin is a type A trichothecene mycotoxin and an active, deacetylated metabolite of the trichothecene mycotoxin T-2 toxin .1,2Like T-2 toxin, HT-2 toxin inhibits protein synthesis and cell proliferation in plants.2HT-2 toxin also reduces viability of HepG2, A549, HEp-2, Caco-2, A-204, U937, Jurkat, and RPMI-8226 cancer cells with IC50values ranging from 3.1 to 23 ng/ml and human umbilical vein endothelial cells with an IC50value of 56.4 ng/ml.1It induces oxidative stress, DNA damage, and autophagy in, as well as halts the development of, cultured mouse embryos when used at a concentration of 10 nM.3HT-2 toxin has been found in cereal grains and food products.4,5 1.Nielsen, C., Casteel, M., Didier, A., et al.Trichothecene-induced cytotoxicity on human cell linesMycotoxin Res.25(2)77-84(2009) 2.Nathanail, A.V., Varga, E., Meng-Reiterer, J., et al.Metabolism of the fusarium mycotoxins T-2 toxin and HT-2 toxin in wheatJ. Agric. Food Chem.63(35)7862-7872(2015) 3.Zhang, L., Li, L., Xu, J., et al.HT-2 toxin exposure induces mitochondria dysfunction and DNA damage during mouse early embryo developmentReprod. Toxicol.85104-109(2019) 4.Langseth, W., and Rundberget, T.The occurrence of HT-2 toxin and other trichothecenes in Norwegian cerealsMycopathologia147(3)157-165(1999) 5.Al-Taher, F., Cappozzo, J., Zweigenbaum, J., et al.Detection and quantitation of mycotoxins in infant cereals in the U.S. market by LC-MS/MS using a stable isotope dilution assayFood Control72(Part A)27-35(2017)