huh7

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.

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.

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 FGFR4, leading to the inhibition of tumor cell proliferation in FGFR4-overexpressing cells. It is a receptor tyrosine kinase upregulated in certain tumor cells and involved in proliferation, differentiation, angiogenesis, and survival.

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

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

PK11000 is a p53 targeting compound, has anti-tumor activities through activation of unstable p53.

Sorafenib (Bay 43-9006) is a multikinase inhibitor that targets Raf-1, B-Raf, VEGFR2, VEGFR3, VEGFR4, PDGFRβ, FLT3, c-Kit, and others (IC50=6 22 90 15 20 20 57 58 nM) with oral activity. It exhibits antitumor properties and can induce autophagy, apoptosis, and agonistic iron death.

BLU0588 is a selective PRKACA inhibitor. BLU0588 inhibits PRKACA catalytic activity with a half-maximal inhibitory concentration (IC50) of 1 nM.

Leupeptin hemisulfate is a protease inhibitor with cell membrane-permeable, reversible, competitive, and oral activities. Leupeptin hemisulfate inhibits the activity of Cathepsin B, Cathepsin H, and Cathepsin L, and blocks fusion of amphipathic lysosomes. Leupeptin hemisulfate also has anti-inflammatory activity.

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

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

Tirbanibulin (KX2-391) is a highly selective Src kinase inhibitor that has demonstrated efficacy in pre-Clinicalal animal models of colon, pancreatic, prostate and breast cancer. It is a substrate-targeted kinase inhibitor. KX2-391, belongs to an emerging new family of targeted cancer treatments called protein kinase inhibitors.

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.

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

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).

SARS-CoV-2-IN-96 (compound 12b) acts as an inhibitor for both HCoV-OC43 (EC50= 97 nM) and SARS-CoV-2 (EC50= 45 nM), while displaying low cytotoxicity in Huh7 cells (CC50=10 μM).

CV-4-26 (Compound 22) acts as a covalent inhibitor of TEAD. By inhibiting YAP TEAD-driven transcription, it diminishes the expression of CTGF and CYR61. Furthermore, CV-4-26 impedes colony formation in Huh7 and HepG2 cells, inducing cell cycle arrest and apoptosis (apoptosis). This compound demonstrates anti-tumoral activity against hepatocellular carcinoma (HCC) and hepatoblastoma (HB).

Antiproliferative agent-59 (Compound 14u) acts as an inhibitor of tubulin polymerization. Demonstrating anticancer activity in Huh7, SGC-7901, and MCF-7 cell lines, this compound achieves IC50 values of 0.03, 0.18, and 0.13 μM, respectively. Additionally, it arrests the cell cycle at the G2 M phase and induces apoptosis in Huh7 cells. In a xenograft mouse model utilizing Huh7 cells, Antiproliferative agent-59 exhibits antitumor effects against hepatocellular carcinoma without significant toxicity.

MAGL-IN-20 (compound ±34) is a reversible inhibitor of monoacylglycerol lipase (MAGL). It exhibits significant antiproliferative activity against a range of cancer cell lines, including H460, HT29, CT-26, Huh7, and HCCLM-3.

MTI013 is a selective inhibitor of SARS-CoV-2 nsp14 Mtase (IC50: 2.98 µM) and an antiviral agent (IC50: 10.33 µM in HCoV-229E infected Huh7 cells). Additionally, MTI013 demonstrates synergistic antiviral effects when used in conjunction with the RdRp inhibitor SHEN26.

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.

SHP2-IN-33 (Compound D13) is an allosteric inhibitor of SHP2, exhibiting an IC50 of 1.2 μM against SHP2. It demonstrates an antiproliferative IC50 of 38 μM in Huh7 cells by blocking the G0 G1 cell cycle, inducing apoptosis (Apoptosis), and inhibiting the MAPK signaling pathway. In a Huh7 xenograft mouse model, SHP2-IN-33 shows significant antitumor activity and favorable pharmacokinetic properties, including 54% oral bioavailability and a half-life of 10.57 hours. SHP2-IN-33 holds potential for research involving SHP2-associated tumor diseases.

Tubulin polymerization-IN-75 (Compound 6) is an inhibitor of tubulin polymerization, with an IC50 value of 30 μM. It effectively suppresses the proliferation of cancer cells Huh7 and 293T, demonstrating IC50 values of 14.3 μM and 13.8 μM, respectively.

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