hepatocellular carcinoma

Palbociclib (PD 0332991) is a CDK inhibitor that inhibits CDK4 and CDK6 (IC50=11/16 nM) and is orally active. Palbociclib has anti-tumorigenic activity and has investigational potential for use in ER-positive and HER2-negative breast cancer.

Palbociclib monohydrochloride (PD 0332991 hydrochloride) is a selective inhibitor of CDK4/6 (IC50s: 11/16 nM). It exhibits no inhibition against a panel of 36 additional protein kinases.

Palbociclib Isethionate (PD 0332991 isethionate) is a selective inhibitor of CDK4 6 (IC50s: 11 16 nM). It exhibits no inhibition against a panel of 36 additional protein kinases.

Rosiglitazone (BRL49653) is a PPARγ agonist, TRPC5 activator, and TRPM3 inhibitor with oral activity. Rosiglitazone is also a hypoglycemic agent and a thiazolidinedione insulin sensitizer.

Conteltinib (CT-707) is an enzyme inhibitor with antitumor activity targeting FAK, ALK, and Pyk2.Conteltinib exhibits significant inhibition of FAK, overcomes hypoxia-mediated sorafenib resistance in hepatocellular carcinoma through inhibition of YAP signaling, and can be used in advanced ALK-positive non-small-cell lung cancer and lymphoma.

Lagociclovir (MIV-210), a nucleoside analogue, is an antiviral compound available for the treatment of HBV82 that inhibits the replication of wild-type hepatitis B virus (HBV) in human hepatocellular carcinoma cell lines that permanently express HBV.

R1498 is an inhibitor of cyclin-dependent kinase 2. It also acts by targeting angiogenesis and mitosis pathways. It is well-tolerated and orally active for hepatocellular carcinoma and gastric cancer treatment.

SC-2001 is a MCL-1 inhibitor. SC-2001 inhibits STAT3 phosphorylation through enhancing SHP-1 expression and induces apoptosis in human breast cancer cells. SC-2001 overcomes STAT3-mediated sorafenib resistance through RFX-1 SHP-1 activation in hepatocellu

Vacquinol-1 is an MKK4 activator, which rapidly and selectively induces glioma cell death.

Triglycidyl isocyanurate (Teroxirone) is a triazene triepoxide with antineoplastic and antiangiogenic activity. It inhibits growth of human non-small cell lung cancer cells by activating p53. Triglycidyl isocyanurate alkylates and cross-links DNA, thereby inhibiting DNA replication. It induces cell apoptosis and can be used for cancer research[1][2]. Triglycidyl isocyanurate is also used in various polyester powder coatings in the metal finishing industry.

Mitoxantrone (mitozantrone) is an anthracenedione antibiotic with antineoplastic activity. Mitoxantrone intercalates into and crosslinks DNA, thereby disrupting DNA and RNA replication. This agent also binds to topoisomerase II, resulting in DNA strand breaks and inhibition of DNA repair. Mitoxantrone is less cardiotoxic compared to doxorubicin.

Rosiglitazone hydrochloride (BRL-49653 HCl) is a blood glucose-lowering drugs, stimulating insulin secretion by binding to the PPAR receptors in fat cells.

Silymarin (Silybin B) (Silybin B) is a polyphenolic flavonoid that extracts from the milk thistle or seeds of Silybum marianum. It is used in the prevention and treatment of liver diseases.

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.

Rubone (2'-Hydroxy-2,4,4',5,6'-pentamethoxychalcone), a natural product and a modulator of miR-34a (microRNA-34), upregulates miR-34a expression in a p53-dependent manner, which in turn downregulates the expression of downstream targets Bcl-2, cyclin-D1, CDK6, SIRT1, and FOXP1, thereby inhibiting tumor growth and reversal of hepatocellular carcinoma (HCC) and chemoresistance in prostate cancer.

1. 6-Shogaol (6-Shogaol) has antipyretic and analgesic effects in addition to inhibitory effect on lipoxygenase activity. 2. 6-shogaol has anti-inflammatory property, reduces the inflammatory response and protected the femoral cartilage from damage produced in a CFA monoarthritic model of the knee joint of rats. 3. 6-Shogaol inhibits the growth of human cancer cells and induces apoptosis in COLO 25 cells through modulation of mitochondrial functions regulated by reactive oxygen species (ROS). 4. 6-Shogaol effectively inhibit invasion and metastasis of hepatocellular carcinoma through diverse molecular mechanisms, including inhibition of the MAPK and PI3k Akt pathways and NF-κB and STAT3 activities to suppress expression of MMP-2 -9 and uPA and block angiogenesis, could further regulate urokinase-type plasminogen activity.

Droxinostat (NS 41080) is a selective HDAC inhibitor, primarily targeting HDACs 6 and 8 with IC50 values of 2.47 μM and 1.46 μM, respectively. It is over 8-fold more selective against HDAC3 and shows no inhibition for HDAC1, 2, 4, 5, 7, 9, and 10.

Tubulin polymerization-IN-47 is a tubulin polymerization inhibitor and mitotic inhibitor with antitumor activity and inhibitory effects on neuroblastoma cancer cell proliferation, with IC50s of 7 and 12 nM for Chp-134 and Kelly cell lines, respectively. Tubulin polymerization-IN-47 is a candidate compound for the treatment of hepatocellular carcinoma, colon cancer, lung cancer and breast cancer.

5-HT2B antagonist-1 is an orally active 5-HT2B receptor antagonist with an IC50 of 33.4 nM, suitable for studies of diseases characterized by 5-HT2B receptor signaling, such as hepatocellular carcinoma, cardiovascular disease, or gastrointestinal disease [1] [2].

4,6-Benzilidine-D-Glucose is a clinical antitumor compound showing antitumor activity in rats with chemically induced hepatocellular carcinoma.

Durvalumab (MEDI 4736) is a humanized monoclonal antibody targeting PD-L1. It can block the interaction of PD-L1 with PD-1 and CD80, with IC50 values of 0.1 and 0.04 nM, respectively. Durvalumab is often used in combination with platinum-based compounds for the treatment of non-small cell lung cancer and advanced hepatocellular carcinoma cells.

FAPI-4 FAPI-4 is a fibroblast activating protein (FAP) inhibitor, a FAPI ligand, which shows strong liver uptake in PET imaging of primary liver cancer hepatocellular carcinoma (HCC) and is commonly used in PET imaging for the study of cancer.

Glutaminase-IN-1 (CB839 derivative), a novel 1,3,4-selenodiazepine inhibitor of the renal-type glutaminase (KGA) variant, exhibited antitumor activity in an aggressive H22 hepatocellular carcinoma xenograft model.

PIM447 (LGH447) is an oral, selective pan-PIM kinase inhibitor with antitumor and bone-protective effects. It inhibits PIM1, PIM2, and PIM3, induces apoptosis, and decreases the viability, proliferation, and motility of HuH6 and COA67 cells. PIM447 suppresses tumorigenesis in hepatocellular carcinoma and can be used in the study of multiple myeloma.