Takinib (EDHS-206) is a specific and effective TAK1 inhibitor(IC50= 9.5 nM).

Simvastatin (MK 733) is an HMG-CoA reductase inhibitor (Ki=0.2 nM) with oral activity. Simvastatin has hypolipidemic activity, inhibits hepatic production of cholesterol, and is also used for the prevention of cardiovascular disease.

ITMN4077 has antiviral activity against Hepatitis C virus infected in human HuH7 cells assessed as inhibition of HCV subgenomic replicon replication with an EC50 of 2.131μM.

HMGB1-IN-2 (compound 15) is a selective inhibitor of the highly conserved nuclear protein HMGB1, demonstrating no inhibitory effect at an IC50 of 20.2 μM in RAW264.7 cells. At a concentration of 30 μM, HMGB1-IN-2 reduces IL-1β, TNF-α, and caspase-1 p20 levels, and inhibits NF-κB p65 phosphorylation, providing anti-apoptotic effects. In vivo, HMGB1-IN-2 at a dose of 15 mg/kg administered intraperitoneally alleviates kidney injury in a mouse model of septic acute kidney injury. Furthermore, it inhibits Huh7 and A549 cells with IC50 values of 77.0 μM and 82.0 μM, respectively [1].

SQLE-IN-1 is a squalene epoxidase (SQLE) inhibitor with anti-tumor activity. It can inhibit the proliferation and migration of liver cancer cell line Huh7, inhibit the production of cellular cholesterol, and increase the expression of the tumor suppressor gene PTEN. expression, inhibiting the protein expression of PI3K and AKT.

Stephacidin B is a fungal metabolite that has been found inA. ochraceus.1Dimeric stephacidin B is rapidly converted to a monomer, avrainvillamide ,in vitro.2Stephacidin B is cytotoxic to a variety of cancer cells, including testosterone-independent PC3 and -sensitive LNCaP prostate cancer cells (IC50s = 0.37 and 0.06 μM, respectively) and estradiol-independent SK-BR-3 and -sensitive MCF-7 breast cancer cells (IC50s = 0.32 and 0.27 μM, respectively).1It induces apoptosis in HepG2 and Huh7 hepatocellular carcinoma cells when used at a concentration of 4 μM.3 1.Qian-Cutrone, J., Huang, S., Shu, Y.-Z., et al.Stephacidin A and B: Two structurally novel, selective inhibitors of the testosterone-dependent prostate LNCaP cellsJ. Am. Chem. Soc.124(49)14556-14557(2002) 2.Wulff, J.E., Herzon, S.B., Siegrist, R., et al.Evidence for the rapid conversion of stephacidin B into the electrophilic monomer avrainvillamide in cell cultureJ. Am. Chem. Soc.129(16)4898-4899(2007) 3.Hu, L., Zhang, T., Liu, D., et al.Notoamide-type alkaloid induced apoptosis and autophagy via a P38/JNK signaling pathway in hepatocellular carcinoma cellsRSC Adv.9(34)19855-19868(2019)

Tirbanibulin Mesylate (KX01 Mesylate) is an inhibitor of Src that targets the peptide substrate site of Src (GI50: 9-60 nM in cancer cell lines).

KKJ00626, an inhibitor of HBV virus, inhibits HBV replication in transfected Huh7 cells.

LDN-212854 (BMP Inhibitor III), a novel BMP inhibitor, exhibits greater selectivity for BMP versus the TGF-β type I receptors; possesses differences towards ALK2(IC50=1.3 nM) versus ALK1/3 compared to other inhibitors.

Betulinic aldehyde oxime is a pentacyclic triterpenoid and derivative of the cholesterol biosynthesis inhibitor betulin .1It is active againstE. aerogenes,E. coli,E. faecalis,P. aeruginosa,S. aureus, andC. albicans, as well asL. donovaniamastigotes, when used at a concentration of 50 μM.1,2Betulinic aldehyde oxime (50 μM) is cytotoxic to Huh7 hepatocellular carcinoma cells.2

Lin28 1632 is an inhibitor of RNA binding protein Lin28. It promotes mESC differentiation. Lin281632 is also bromodomain inhibitor.

Lupus autoantigen peptide (LAP), a derivative of the autoantigen La found in systemic lupus erythematosus (SLE) patients, spans amino acids 11-28 of La and functions as an antiviral peptide. It primarily blocks the hepatitis C virus (HCV) from interacting with internal ribosome entry site (IRES) trans-acting factors (ITAFs), notably the polypyrimidine tract-binding protein (PTB) and poly(rC)-binding protein 2 (PCBP2). In a Huh7 cell-based reporter assay, LAP at a concentration of 60 µM effectively hampers HCV IRES-mediated translation, a process reversible by adding recombinant forms of PTB and PCBP2.

FGFR4-IN-14 (Compound 27i) is a selective FGFR4 inhibitor with an IC50 of 2.4 nM, showing potent inhibition of cell proliferation in the V550L and N535K mutant strains. Specifically, it registers IC50 values of 21 nM against Huh7 cells, 2.5 nM against BaF3/ETV6-FGFR4-V550L cells, and 171 nM against BaF3/ETV6-FGFR4-N535K cells. Demonstrating significant antitumor efficacy in the Huh7 xenograft model, FGFR4-IN-14 is utilized in the research of hepatocellular carcinoma (HCC) [1].

Geranylgeranoic acid (GGA) is an isoprenoid that has been found inS. chinensisand has anticancer activity.1It induces apoptosis in Huh7 and PLC/PRF/5 human hepatoma cells and MLE-10 transformed mouse hepatocytes, but not primary mouse hepatocytes, when used at concentrations ranging from 1 to 20 μM. GGA (10 μM) induces apoptosis in Huh7 cellsvialoss of the mitochondrial membrane potential and activation of interleukin-1β-converting enzyme (ICE) and cysteine protease precursor 32 (CPP32).2It also inhibits lysine-specific demethylase 1 (LSD1; IC50= 46.97 μM).3 1.Shidoji, Y., and Ogawa, H.Natural occurrence of cancer-preventive geranylgeranoic acid in medicinal herbsJ. Lipid Res.45(6)1092-1103(2004) 2.Shidoji, Y., Nakamura, N., Moriwaki, H., et al.Rapid loss in the mitochondrial membrane potential during geranylgeranoic acid-induced apoptosisBiochem. Biophys. Res. Commun.230(1)58-63(1997) 3.Sakane, C., Okitsu, T., Wada, A., et al.Inhibition of lysine-specific demethylase 1 by the acyclic diterpenoid geranylgeranoic acid and its derivativesBiochem. Biophys. Res. Commun.444(1)24-29(2014)

KSJ0001, a HBV virus inhibitor, inhibits HBV replication in transfected Huh7 cells.

YW1128 is an inhibitor of Wnt/β-catenin signaling with an IC50 value of 4.1 nM in a reporter assay.1 It decreases protein levels of β-catenin in the presence of the GSK3β inhibitor lithium chloride and increases protein levels of Axin1 in HEK293 cells. YW1128 decreases lipid accumulation and the expression of gluconeogenic and lipogenic genes in Huh7 cells. It decreases the hepatic expression of Wnt target genes, improves glucose tolerance, and prevents body weight increases and hepatic lipid accumulation in mice fed a high-fat diet, but not mice fed normal chow, when administered at a dose of 40 mg/kg every other day for 11 weeks.References1. Obianom, O.N., Ai, Y., Li, Y., et al. Triazole-based inhibitors of the Wnt/β-catenin signaling pathway improve glucose and lipid metabolism in diet-induced obese mice. J. Med. Chem. 62(2), 727-741 (2019). YW1128 is an inhibitor of Wnt/β-catenin signaling with an IC50 value of 4.1 nM in a reporter assay.1 It decreases protein levels of β-catenin in the presence of the GSK3β inhibitor lithium chloride and increases protein levels of Axin1 in HEK293 cells. YW1128 decreases lipid accumulation and the expression of gluconeogenic and lipogenic genes in Huh7 cells. It decreases the hepatic expression of Wnt target genes, improves glucose tolerance, and prevents body weight increases and hepatic lipid accumulation in mice fed a high-fat diet, but not mice fed normal chow, when administered at a dose of 40 mg/kg every other day for 11 weeks. References1. Obianom, O.N., Ai, Y., Li, Y., et al. Triazole-based inhibitors of the Wnt/β-catenin signaling pathway improve glucose and lipid metabolism in diet-induced obese mice. J. Med. Chem. 62(2), 727-741 (2019).

Topoisomerase I/II inhibitor 2 (compound 1a) can significantly reduce the xenograft tumor growth in mice model which can be used in treating liver cancer. Topoisomerase I/II inhibitor 2 is a DNA topoisomerase I/II dual inhibitor. Topoisomerase I/II inhibitor 2 is a potent Topoisomerase inhibitor with IC50 values of 6.83 μM and 9.82 μM for LM9 cells and Huh7 cells [1].

Purfalcamine is an orally active, selective Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1) inhibitor with an IC50 of 17 nM and an EC50 of 230 nM. Purfalcamine has antimalarial activity and causes malaria parasites developmental arrest at the schizont stage[1][2]. Purfalcamine has low activity against Toxoplasma gondii calcium-dependent protein kinase 3 (TgCDPK3)[1]. Purfalcamine (225, 450 nM) has no effect on the parasitemia in the first 32 hours. After about 40 hours, parasite level remains stable and then begins dropping[1]. Purfalcamine inhibits proliferation with EC50s of 171-259 nM for P. falciparum strains (3D7, Dd2, FCB, HB3 and W2), which indicates effectiveness against drug-resistant parasites[1]. Given that the EC50 value for P. falciparum (3D7) is 230 nM, Purfalcamine shows a therapeutic window ranging from 23-fold to 36-fold (EC50s for CHO=12.33 μM, HEp2=7.235 μM, HeLa=7.029 μM and Huh7=5.476 μM)[1]. Purfalcamine (10 mg/kg; oral gavage; BID; for 6 days) demonstrates a delay in the onset of parasitemia in treated mice[1]. Purfalcamine (20 mg/kg; orally gavage) exhibits a Cmax of 2.6 μM with a half-life of 3.1 hours[1]. Animal Model: Male BALB/c mice, 7 weeks of age with the malaria parasite[1] [1]. Nobutaka Kato, et al. Gene expression signatures and small-molecule compounds link a protein kinase to Plasmodium falciparum motility. Nat Chem Biol. 2008 Jun;4(6):347-56. [2]. Rajshekhar Y Gaji, et al. Expression of the essential Kinase PfCDPK1 from Plasmodium falciparum in Toxoplasma gondii facilitates the discovery of novel antimalarial drugs. Antimicrob Agents Chemother. 2014 May;58(5):2598-607.

Inarigivir ammonium (SB-9200 ammonium) is a dinucleotide antiviral compound that significantly reduces HBV DNA in transgenic mice expressing hepatitis B virus. Inarigivir is an agonist of retinoic acid-inducible gene-I (RIG-I) that activates intracellular innate immunity.

AP-III-a4 (ENOblock) (ENOblock) is the first nonsubstrate analogue inhibitor of enolase with IC50 of 0.576 μM.

PF 06446846 is a potent and selective PCSK9 inhibitor

Indinavir sulfate (L735524 sulfate) is a HIV protease inhibitor.It inhibits the HIV-1 protease with an IC50 value of 0.41 nM and Ki value of 0.24 nM.

Roblitinib (FGF-401) is an inhibitor of human fibroblast growth factor receptor 4 (FGFR4), with potential antineoplastic activity. Upon administration, Roblitinib binds to and inhibits the activity of FGFR4, which leads to an inhibition of tumor cell proliferation in FGFR4-overexpressing cells. Roblitinib is a receptor tyrosine kinase upregulated in certain tumor cells and involved in tumor cell proliferation, differentiation, angiogenesis, and survival.

Antiproliferative agent-32 (Compound 1c) impedes phosphorylation within the PI3K/Akt/mTOR signaling pathway, restrains proliferation of Huh7 and SK-Hep-1 cells, induces apoptosis, and inflicts mitochondrial damage, rendering it a potential subject for hepatocellular carcinoma research [1].

1-O-p-Coumaroyl-β-D-glucose, a compound extractable from Luffa cylindrica (L.) Roem (sponge gourds) [1] [2], has been found to enhance glucose uptake in HuH7 cells.

2'-Deoxy-2'-fluorocytidine, an nucleoside analog, is a potent inhibitor of Crimean-Congo hemorrhagic fever virus (CCHFV) replication. 2′-deoxy-2′-fluorocytidine can act synergistically with T705 to increase the potency of both compounds antiviral effects on CCHFV replication[1]. 2'-Deoxy-2'-fluorocytidine has antiviral activities, showing 50% effective concentrations (EC50) of 61 nM and 31 nM against CCHFV and CCHFV/ZsG in Huh7 cells, respectively. And it shows a 50% cytotoxicity concentration (CC50) of >50.0 μM in Huh7 cells[1]. [1]. Stephen R Welch, et al. Identification of 2'-deoxy-2'-fluorocytidine as a potent inhibitor of Crimean-Congo hemorrhagic fever virus replication using a recombinant fluorescent reporter virus. Antiviral Res. 2017 Nov;147:91-99.

Combretastatin A-1 is a potent microtubule inhibitor with anti-tumour and anti-vascular activity, acting through microtubule protein depolymerisation-mediated inactivation of AKT to inhibit the Wnt/β-catenin pathway, and can be used to study hepatocellular carcinoma.

IMP2-IN-1 (compound 4) is an effective IMP2 inhibitor with an IC50 of 81.3-127.5 μM for IMP2 RNA . IMP2-IN-1 decreased the level of IMP2 in SW480 cells. IMP2-IN-1 significantly inhibited the activity of differentiated and undifferentiated Huh7 cells.

Simeprevir (TMC435) is a potent HCV NS3/4A protease inhibitor, and inhibits HCV replication with EC50 of 8 nM.

LAP is a photocrosslinker for hydrogels.