anti-hepatocellular

GYY4137 (GYY 4137 morpholine salt) is a novel water-soluble and slow releasing H2S donor with vasodilator and antihypertensive activity. GYY4137 also exhibits anti-inflammatory and anticancer activity.

Mollugin (Rubimaillin) may be a JAK2 inhibitor and inhibits LPS-induced inflammatory responses by blocking the activation of the JAK-STAT pathway. Mollugin as a candidate for a chemotherapeutic agent in OSCCs via the upregulation of the HO-1 and Nrf2 pathways and the downregulation of NF- κ B. Mollugin may be a novel therapeutic candidate for bone loss-associated disorders including osteoporosis, rheumatoid arthritis, and periodontitis. Also, it has anticancer efficacy, can modulate the HER2 pathway in HER2-overexpressing Y cells with a potential role in the treatment and prevention of human breast and ovarian Y with HER2 overexpression.

S-Allylmercaptocysteine (SAMC) is an organic sulfur compound extracted from garlic, with anti-cancer, anti-inflammatory, and antioxidant properties. It protects against hepatocellular damage, improves alcoholic liver disease by modulating insulin receptor signaling, and enhances anti-tumor immunity by inhibiting PD-L1 expression.

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.

CDK-IN-14 (B34) is a CDK2 inhibitor (IC50=0.097 μM) that exhibits anti-hepatocellular carcinoma activity. It inhibits the cell cycle in HepG-2 cancer cells and induces apoptosis (apoptosis) through a caspase-mediated mechanism.

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).

ROS-ERS inducer 2 (Complex 3f) promotes the generation of intracellular ROS, affects mitochondrial function, facilitates the release of damage-associated molecular patterns (DAMPs), induces immunogenic cell death (ICD), and activates endoplasmic reticulum stress (ERS). It plays a significant role in anti-hepatocellular carcinoma research.

ZSNI-21 is a dual inhibitor targeting ADAM17 and HDAC2. It effectively suppresses the proliferation of Bel-7402 cells and exhibits significant anti-metastatic properties against HCC-LM3 cells, making it a promising candidate for hepatocellular carcinoma (HCC) research.

TRBP-IN-1 (Compound 13j) is an orally active inhibitor of TAR RNA-binding protein 2 (TRBP) with an IC50 of 12.72 μM. It exhibits significant anti-hepatocellular carcinoma (HCC) activity, effectively suppressing proliferation and metastasis of HCC cells [HCCLM3 cells (IC50: 18.96 μM) and SK-Hep-1 cells (IC50: 16.45 μM)]. TRBP-IN-1 modulates miRNA biosynthesis by targeting TRBP, inhibiting the expression of oncogenic miRNAs. It induces apoptosis and pyroptosis in HCC cells by decreasing miRNA levels. TRBP-IN-1 is suitable for research on targeted HCC therapy.

c-Met degrader-1 (Compound H11) is an orally active c-Met degrader that operates via the ubiquitin-proteasome system. It exhibits anti-hepatocellular carcinoma (HCC) activity and hampers tumor growth in MHCC97H xenografts. Additionally, c-Met degrader-1 suppresses the proliferation of HCC cells, disrupts the cell cycle, and induces apoptosis. It may also potentially overcome resistance to Type I c-Met inhibitors.

PQ32 is an anti-tumor agent targeting c-MYCPu27 and KRASG-quadruplexes. It hinders the proliferation of tumor cells, arrests the cell cycle at the G2 phase, and induces apoptosis (apoptosis). PQ32 suppresses the expression of c-MYC and KRAS genes. It can inhibit tumor growth in mice and is applicable for research in cancers such as lymphoma, breast cancer, lung cancer, hepatocellular carcinoma, and colorectal cancer.

D574-0246 is a dual-active inhibitor of OXCT1, targeting the enzyme's keto-dehydrogenase and succinyl-transferase activities. It reduces substrate-specific (LACTB K284) and global protein succinylation in HepG2 cells and lowers the ketolytic activity of OXCT1. The compound decreases the viability of HCC cells with an IC50 of 16.49 μM in PLC cells and 6.656 μM in HepG2 cells. In nude mice with HepG2 xenograft tumors overexpressing OXCT1, D574-0246 demonstrates anti-tumor effects. It is applicable for studies on hepatocellular carcinoma (HCC).

(R)-Etodolac is an enantiomer of the non-steroidal anti-inflammatory drug etodolac, known for its ability to inhibit the transcriptional repression of β-catenin. It also exhibits antitumor properties and can be utilized in hepatocellular carcinoma research.

IRAK1-IN-2 is an orally active inhibitor of IRAK1 and an anti-tumor agent with high selectivity for IRAK4 and other kinases in the same group. It functionally inhibits IRAK1, disrupting TLR/IL-1R signaling pathways. In both in vitro studies and animal models, IRAK1-IN-2 suppresses processes related to hepatocellular carcinoma. It also serves as a chemical probe for IRAK1 research in the study of hepatocellular carcinoma.

VEGFR2/HDAC-IN-1 is an orally active dual-selective enzyme inhibitor targeting VEGFR2 kinase and HDAC6. It has an IC50 of 19.19 nM for VEGFR2 and 0.165 μM for HDAC6. This compound enhances acetylation of α-tubulin, exhibits antiproliferative effects, inhibits tumor growth, and possesses anti-angiogenic activity. VEGFR2/HDAC-IN-1 is applicable in research related to colorectal cancer and hepatocellular carcinoma.

Bcl-2/Mcl-1-IN-5 (Compound S6) is an inhibitor targeting Bcl-2 and Mcl-1. It facilitates apoptosis by downregulating anti-apoptotic proteins Bcl-2 and Mcl-1, induces mitochondrial membrane depolarization, and activates caspase-dependent apoptotic cascades, as evidenced by Caspase-3 activation and PARP1 cleavage. Additionally, Bcl-2/Mcl-1-IN-5 exhibits anti-hepatocellular carcinoma activity.

Myrtenal is a natural monoterpene. It is found to attenuate diethylnitrosamine-induced hepatocellular carcinoma in rats by stabilizing intrinsic antioxidants and modulating apoptotic and anti-apoptotic cascades. Myrtenal also inhibits acetylcholinesterase

Fisogatinib (BLU-554) is a highly potent, selective and orally active FGFR4 inhibitor with an IC50 value of 5 nM and significant anti-tumor activity in hepatocellular carcinoma models dependent on FGFR4 signaling.

Adenosine 5'-methylenediphosphate is an inhibitor of ecto-5'-nucleotidase, also known as CD73, with a Kivalue of 37 nM.1It inhibits cAMP accumulation induced by adenosine 5'-monophosphate , adenosine 5'-diphosphate , or adenosine 5'-triphosphate but not adenosine in VA-13 human fibroblasts when used at a concentration of 100 μM. Adenosine 5'-methylenediphosphate reduces proliferation of U138MG glioma cells, as well as inhibits the invasion and migration of MHCC97H hepatocellular carcinoma (HCC) cells in a migration assay.2,3It increases tumor infiltration of CD3+CD8+T cells and reduces tumor growth in a K1735 murine melanoma model when administered at a dose of 400 μg/mouse.4 1.Bruns, R.F.Adenosine receptor activation by adenine nucleotides requires conversion of the nucleotides to adenosineNaunyn Schmiedebergs Arch. Pharmacol.315(1)5-13(1980) 2.Braganhol, E., Tamajusuku, A.S.K., Bernardi, A., et al.Ecto-5′-nucleotidase/CD73 inhibition by quercetin in the human U138MG glioma cell lineBiochim. Biophys. Acta1770(9)1352-1359(2007) 3.Shali, S., Yu, J., Zhang, X., et al.Ecto\5′\nucleotidase (CD73) is a potential target of hepatocellular carcinomaJ. Cell Physiol.234(7)10248-10259(2018) 4.Forte, G., Sorrentino, R., Montinaro, A., et al.Inhibition of CD73 improves B cell-mediated anti-tumor immunity in a mouse model of melanomaJ. Immunol.189(5)2226-2233(2021)

Streptochlorin is a bacterial metabolite originally isolated from Streptomyces sp. SF2583 that has diverse biological activities, including antiangiogenic, antiproliferative, and anti-allergic properties. It inhibits TNF-α-induced NF-κB transcriptional activity and decreases proliferation of human umbilical vein endothelial cells (HUVECs) when used at concentrations ranging from 5 to 20 μM. Streptochlorin (12 μg/ml) decreases viability of, as well as induces apoptosis and increases the production of reactive oxygen species (ROS) in, Hep3B human hepatocellular carcinoma cells. It does not induce cytotoxicity in RBL-2H3 mast cells at concentrations up to 100 μM. Streptochlorin prevents degranulation in antigen-stimulated mast cells, as well as inhibits Syk kinase and the Src family kinases LYN and Fyn and reduces the secretion of TNF-α and IL-4 induced by dinitrophenyl-human serum album (DNP-HSA) in RBL-2H3 mast cells. It also decreases swelling and reduces scratching behavior in a mouse model of allergic dermatitis induced by dinitrofluorobenzene (DNFB).

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.

FGFR4-IN-5, a covalent FGFR4 inhibitor, demonstrates potency and selectivity with an IC50 value of 6.5 nM. Exhibiting significant in vivo anti-tumor activity, it is applicable for research in hepatocellular carcinoma [1].

HBV-IN-23 (Compound 5k) is an inhibitor of HBV DNA replication with an IC50 of 0.58 μM, inhibiting both drug-sensitive and drug-resistant strains. It induces apoptosis in HepG2 cells and demonstrates anti-hepatocellular carcinoma (HCC) effects.

Palbociclib hydrochloride (pabociclib hydrochloride) is the salt form of Palbociclib, a selective and orally available CDK4 and CDK6 inhibitor with anti-tumor proliferative activity for use in breast and hepatocellular carcinoma.