human hepg2

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.

CVT-12012 is an orally bioavailable inhibitor of stearoyl-CoA desaturase (SCD; IC50 = 6.1 nM in HepG2 cells).

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 active, selective, competitive vasopressin receptor 2 (V2R) antagonist (IC50 = 1.28 μM) that inhibits AVP-induced platelet aggregation. Tolvaptan is used in studies of 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.

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.

3-O-Caffeoylshikimic acid (Compound 8) is a phenolic compound isolated from Livistona chinensis that exhibits antioxidant activity and inhibits the proliferation of multiple human cancer cell lines, including HepG2, HL-60, K562, and CNE-1, with IC50 values ranging from 5 to 150 μM, supporting its relevance in anticancer and oxidative stress research.

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

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.

GJ19 is a PD-L1 inhibitor with an IC50 of 32.06 nM. It binds effectively to human and mouse PD-L1 proteins, exhibiting KD values of 171 nM and 290 nM, respectively. In a co-culture model of HepG2/hPD-L1 and Jurkat T/hPD-1 cells, GJ19 promotes HepG2 cell death in a concentration-dependent manner. In the B16-F10 melanoma mouse model, GJ19 demonstrates significant tumor growth inhibition. GJ19 is applicable in tumor immunotherapy research.

Antiproliferative agent-73 (Compound 7) is an antiproliferative compound that effectively inhibits the proliferation of human cancer cells and exhibits excellent cytotoxicity. It demonstrates potent anticancer activity, with IC50 values of 15.20 μM, 18.18 μM, 20.20 μM, and 13.23 μM for HepG2, MCF-7, HCT-116, and WI38 cells, respectively. Antiproliferative agent-73 is applicable in research involving cancers such as breast cancer, colorectal cancer, and liver cancer.

Anticanceragent 276 (Compound 5) is a multitarget anticancer compound. It exhibits potent antitumor activity against human cancer cells, with IC50 values of 6.90 μM for HEPG2 cells and 4.48 μM for MCF7 cells. Anticanceragent 276 interacts strongly and stably with multiple targets, including topoisomerase II, VEGFR2, c-Met, EGFR, and ERα.

LAB687 (Compound 2a) is an inhibitor of microsomal triglyceride transfer protein (MTP) with an IC50 of 0.9 nM for inhibiting the secretion of apolipoprotein B (apoB) in HepG2 cells. Additionally, LAB687 acts as a Smoothened (Smo) antagonist, exhibiting IC50 values of 2.48 μM and 3.42 μM for mouse and human Smo receptors, respectively. This compound is effective in reducing triglyceride and low-density lipoprotein cholesterol (LDL-C) levels and in inhibiting the Hedgehog signaling pathway.

VEGFR-2-IN-72 is a selective inhibitor of VEGFR-2 with an IC50 of 22.2 nM. It exhibits anticancer activity against human liver cancer cell lines HepG2 and Hep3B, with IC50 values of 15.7 μM and 2.4 μM, respectively. VEGFR-2-IN-72 can cause mild cell cycle arrest and induces apoptosis (aopoptosis). It is suitable for research in hepatocellular carcinoma (HCC).

IKE16 is a fungal-selective eukaryotic topoisomerase II inhibitor with an IC50 value of 13.68 μM. It selectively inhibits the DNA relaxation and decatenation activities of yTOPOII. IKE16 shows moderate activity against standard fungal strains [Candida albicans ATCC 10231, Saccharomyces cerevisiae ATCC 89763], with a minimum inhibitory concentration (MIC) of 2 μg/mL for S. cerevisiae ATCC 89763. It exhibits high cytotoxicity to human cells, with EC50 values of 0.07 μM in HepG2 cells and 0.045 μM in HEK-293 cells. IKE16 is utilized in antifungal infection research.

Tubulin-IN-59 (Compound 8g) is an orally effective microtubule (Tubulin) inhibitor. It exhibits potent antiproliferative activity against HCT116 colorectal cancer, HeLa cervical cancer, and HepG2 liver cancer cell lines, with IC₅₀ values ranging from 16-35 nM. Tubulin-IN-59 arrests HeLa cells in the G2/M phase and induces apoptosis. It also demonstrates significant antitumor activity in the HT29 human colon cancer mouse xenograft model. Tubulin-IN-59 is applicable for research on colorectal and cervical cancers.

Antitrypanosomal agent 27 (Compound 5c) is a quinazoline derivative with antitrypanosomal activity. It inhibits Trypanosoma brucei (T.b. brucei) with a GI50 value of 31 nM. The compound exhibits a selectivity index of ≥50 towards human liver cancer HepG2 cells and demonstrates no significant cytotoxicity. Antitrypanosomal agent 27 is applicable in the study of human African trypanosomiasis.

CDK1-IN-8 is an inhibitor of CDK1. It effectively hinders cell migration, induces apoptosis, and arrests the cell cycle at the G2/M phase. CDK1-IN-8 significantly reduces the expression level of CDK1 protein in HepG2 cells and can be utilized in research related to human hepatocellular carcinoma.