bel-7402

Vadimezan (DMXAA) is a vascular disrupting agent, a murine STING agonist, and an inducer of cytokines such as type I IFN. Vadimezan has antitumor activity and induces a rapid cessation of blood flow in tumors without affecting blood flow in normal tissues.

Ursolic acid (Prunol) is a natural product, a pentacyclic triterpene carboxylic acid extracted from Rhododendron caprifolium. Ursolic acid has anti-tumor, anti-inflammatory, anti-bacterial and hypoglycemic activities.

Sodium dichloroacetate (BCA) , a specific inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50 values of 183 and 80 μM for PDK2 and PDK4 respectively, has been shown to derepress a mitochondrial potassium-ion channel axis, trigger apoptosis in cancer cells, and inhibit tumor growth.

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.

Sertindole (Lu 23-174) is an atypical antipsychotic that binds to dopamine D2 receptors and serotonin (5-HT) receptor subtypes 5-HT1D, 5-HT2A, and 5-HT2C, with Kds of 2.7, 20, 0.14, and 6 nM, respectively.

Demethoxydeacetoxypseudolaric acid B analog has potent activities against HMEC-1, HL-60, A-549, MB-MDA-468, BEL-7402, HCT116, and Hela cells with IC50s ranging from 0.136 to 1.162 μM. and is semi-synthesized by efficient routines from Pseudolaric acid B.

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.

Cyclopamine-KAAD is a potent inhibitor of hedgehog signaling with an IC50 value of 20 nM in a Shh-LIGHT2 assay. It blocks binding of BODIPY-cyclopamine to cells expressing Smoothened (Smo) in a dose-dependent manner. Cyclopamine-KAAD is cell-permeable and binds to SmoA1 to promote its exit from the endoplasmic reticulum. It inhibits the invasion and migration (45.9 and 43.3% inhibition, respectively) of Bel-7402 hepatocarcinoma cells and decreases the expression of nuclear glioma-associated oncogene 1 (Gli1) and cytosolic MMP-9, pERK1, and pERK2 proteins in a dose-dependent manner. Cyclopamine-KAAD also increases TRAIL-mediated cell death in NCH82 and NCH89 human glioblastoma cultures and upregulates expression of the death receptors DR4 and DR5 in LN229 and U251 glioma cells.

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.

CAY10773 is a derivative of the ferroptosis inducer sorafenib .1It selectively inhibits proliferation of BEL-7402, MGC803, and T24 bladder cancer cells (IC50s = 5.77, 5.21 and 3.97 μM, respectively) over non-cancerous HCV-29 cells (IC50= 23.19 μM). CAY10773 induces apoptosis in T24 cells when used at concentrations ranging from 2 to 6 μM but induces ferroptosis at concentrations greater than or equal to 6 μM with 10 hour or longer incubation times. It increases the production of reactive oxygen species (ROS) and decreases the mitochondrial membrane potential in T24 cells. CAY10773 (≥6 μM) also induces autophagy with incubation times longer than eight hours. 1.Chen, J.-N., Li, T., Cheng, L., et al.Synthesis and in vitro anti-bladder cancer activity evaluation of quinazolinyl-arylurea derivativesEur. J. Med. Chem.205112661(2020)

Ardisiacrispin A (Deglucocyclamin) has cytotoxic activity toward HepG2 cancer cell with the GI(50) value of 1.56μM, it could inhibit the proliferation of Bel-7402 cells by inducing apoptosis and disassembling microtubule.Ardisiacrispin(A+B) exhibit prominent abilities to inhibit the proliferation of HL-60 cells by blocking the cell cycle at S phase and inducing apoptosis.

Ursonic acid methyl ester, an esterified derivative of Ursolic acid, exhibits growth inhibitory activity against four tumor cell lines: HL-60, BGC, Bel-7402, and Hela, and the ED50 values for inhibition are >100 μg ml.

AKT-IN-11 is a highly potent antibacterial agent against the human hepatocellular carcinoma Bel-7402 cell line (IC50: 1.15 μM).

Anticancer agent 62 is an effective anticancer agent. anticancer agent 62 exhibited anti-proliferative effects on HepG2, Bel-7402 and MCF-7 cancer cells with IC50 values of 0.019, 0.060 and 0.016 μM, respectively. anticancer agent 62 was able to inhibit tumor growth.

Anticancer agent 61 is an orally active anticancer agent. anticancer agent 61 was able to inhibit the proliferation of HepG2, Bel-7402 and MCF-7 cancer cells with IC50 values of 1.12, 1.97 and 1.08 μM respectively. anticancer agent 61 inhibited tumour Anticancer agent 61 was able to inhibit tumour growth.

HDAC-IN-61 (compound 12k) is a potent, orally active histone deacetylase (HDAC) inhibitor with anticancer activity, exhibiting an IC50 of 30 nM against Bel-7402 cells and is utilized for cancer research [1].

Changnanic acid (schisandrin), a triterpene compound, has demonstrated potential anti-tumor properties, exhibiting moderate cytotoxicity against human tumor cell lines Bel-7402 and MCF-7 with IC50s of 100 μM, and against HL-60 with an IC50 of 50.51 μM [1].

Flemiphilippin A has antioxidant activity, it shows DPPH radical scavenging activity with effective half maximal concentration (EC50) of 18.36 ug mL. Flemiphilippinin A (5 ug mL) exhibits some level of antitumor activity against human hepatocellular carci

Schisanlactone E may show moderate cytotoxic activity against the human tumor cell lines Bel-7402, BGC-823, MCF-7 and HL-60.

11alpha,12alpha-Oxidotaraxerol palmitate shows selective cytotoxicity against HCT-8, Bel-7402, BGC-823, A549 and A2780.

Aphagranin A exhibits strong antiproliferative activity against the growth of six lines of human cancer cells (MCF-7, A549, HepG2, Bel-7402, SGC-7901, and BGC-823.

Chlorovaltrate K shows moderate cytotoxicity against lung adenocarcinoma (A 549), metastatic prostate cancer (PC-3M), colon cancer (HCT-8) and hepatoma (Bel 7402) cell lines with IC50 values of 0.89-9.76 uM.

Marginatoxin may be a promising chemopreventive agent for treating hepatocellular carcinoma, it induces human hepatoma BEL-7402 cells apoptosis in vitro and in vivo via activation of Fas FasL-mediated apoptotic pathway.

3-Oxo-cinobufagin (compound 8), a potential anticancer agent, is extracted from M. spinosus broth using high performance liquid chromatography. This compound is unique among its isolated counterparts because its C-5 hydroxyl group is further oxidized or isomerized, which significantly reduces its cytotoxic activity against most cell lines, except for HEL. However, it demonstrates increased activity in BEL cell strains. The IC50 values of 3-Oxo-cinobufagin for cytotoxicity against cancer cells are: 71.3 μM (HepG2), 90.2 μM (SMMC-7221), 0.11 μM (BEL-7402), 72.5 μM (K562), 5.3 μM (HL-60), and 12 nM (HEL).