hcc cells

Amantadine hydrochloride (CI-719) is an antiviral that is used in the prophylactic or symptomatic treatment of influenza A and Parkinson disease.

Amantadine (1-Aminoadamantane) is an antiviral, is a weak antagonist of the NMDA-type glutamate receptor, increases dopamine release, and blocks dopamine reuptake.

MNK8 (3-methyl-6-(naphthalen-1-yl)pyrimidine-2,4(1H,3H)-dione) is a potent STAT3 inhibitor that reduces the ability of STAT3 to bind to DNA and also has a good growth inhibition effect on liver cancer cells [1].

CIB-L43 is a high affinity and orally available TRBP inhibitor (KD = 4.78 nM), which can effectively inhibit the biosynthesis of oncogenic miR-21, increase the expression of PTEN and Smad7, and block the AKT and TGF-β signaling pathways to inhibit the proliferation and migration of hepatocellular carcinoma (HCC) cells.

ENMD-119 is a 2-methoxyestradiol analog with antiproliferative and antiangiogenic activity. It is suitable for inhibiting HIF-1α and STAT3 in human HCC cells.

MS 154 is a potent and selective cereblon-recruiting Degrader (PROTAC®) of mutant epidermal growth factor receptor (EGFR), comprising a cereblon-binding moiety joined by a linker to gefitinib(Iressa). MS 154 decreases EGFR protein levels, inhibits downstream signaling in and inhibits proliferation of mutant EGFR-bearing lung cancer cells (DC50values are 11 and 25 nM in HCC-827 and H3255 cells, respectively; Dmax> 95% at 50 nM), but not in WT-EGFR-bearing ovarian and lung cancer cells lines. Bioavailable in mice following ip administration.

MS 39 is a potent Proteolysis Targeting Chimera (PROTAC) designed to degrade the Epidermal Growth Factor Receptor (EGFR). The molecule is composed of three structural motifs: an EGFR target ligand (red part), a VHL E3 ligase ligand (S,R,S)-AHPC (blue part), and an undecanedioic acid linker (black part). By facilitating the formation of a ternary complex between EGFR and the VHL E3 ubiquitin ligase, MS 39 triggers the polyubiquitination and subsequent proteasomal degradation of the receptor. MS 39 effectively reduces EGFR protein levels and inhibits downstream oncogenic signaling in HCC-827 and H3255 cell lines, leading to significant suppression of H3255 cancer cell proliferation.

XST-14 is a competitive and specific inhibitor of ULK1 (IC50: 26.6 nM).XST-14 blocks autophagy by inhibiting the phosphorylation of ULK1 downstream substrates.XST-14 induces apoptosis and inhibits the growth of HCC cells.

Scutellarin (Breviscapin) is a natural flavonoid isolated from Scutellaria baicalensis that exhibits antioxidant, anti-inflammatory, antithrombotic, neuroprotective, and cardioprotective and neuroprotective activities. Scutellarin demonstrates antiviral activity against HIV-1 IIIB, HIV-1 (74V), and HIV-1 KM018. Scutellarin inhibits the RANKL-mediated MAPK/NF-κB pathway (IC₅₀ = 10 μM) and activates the Nrf2/HO-1 antioxidant pathway (EC₅₀ = 5 μM). Scutellarin can be used in natural product development and basic research on cardiovascular and cerebrovascular diseases.

Glabridin (KB-289522) may serve as an anti-inflammatory agent in diabetes-related vascular dysfunction, through regulating the synthesis and activity of iNOS under high-glucose levels; may possess a therapeutic effect on metabolic disorders( such as diabetes and hyperglycemia), by modulating glucose metabolism through AMPK in skeletal muscle cells. Glabridin may have potential as a chemopreventive agent against liver Y metastasis, by inhibiting the invasion of human HCC cells.

Arvanil (N-Vanillylarachidonamide) is a synthetic capsaicin-amphetamine hybrid and a ligand for vanilloid receptor 1 (VR1) and cannabinoid receptor 1 (CB1), exhibiting neuroprotective activity, inhibiting spasm, and enhancing cisplatin chemotherapy sensitivity by inducing ferroptosis in HCC cells in vivo. It induces ferroptosis in liver cancer cells via binding to MICU1.

Isoviolanthin reduces the migratory and invasive capacities of TGF-β1-treated HCC cells without cytotoxic effects on normal live cells and has potential as a therapeutic agent for the treatment of advanced-stage metastatic HCC. Isoviolanthin is a flavonoid glycoside extracted from the leaves of Dendrobium Officinale.

PMED-1, a β-catenin inhibitor, effectively suppresses β-catenin activity in hepatoblastoma cells and various HCC (Hepatocellular Carcinoma) cells with IC50 values ranging from 4.87 to 32 μM. It impedes cell proliferation by disrupting the interaction between β-catenin and CREB-binding protein, thus affecting Wnt signaling pathways. PMED-1 is utilized in cancer research studies.

MRTF-A-IN-2 (compound 16) is an inhibitor of MRTF-A. It effectively suppresses cell proliferation and induces senescence in HCC cells.

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).

MRTF-A-IN-1 (compound 14) is an inhibitor of MRTF-A. It effectively suppresses cell proliferation and induces senescence in HCC cells.

CRI9 effectively inhibits the c-MET/PI3K/Akt/mTOR axis, suppressing the proliferation of hepatocellular carcinoma (HCC) cells. This compound exhibits potent cytotoxicity against HCC cells and induces apoptosis.

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.

IDB-001 is an inhibitor of the ribosomal PTC that selectively represses protein synthesis by sequence. It inhibits the viability of HCC-1143 cells with an EC50 of 0.84 μM and also hinders the viability of MYC-dependent cancer cells.

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.

QC-182 is a potent p300/CBP PROTAC degrader. It reduces p300 protein levels in SK-HEP-1 cells with a DC50 of 93 nM. QC-182 effectively inhibits cell growth in SK-HEP-1 and JHH7 cell lines, with IC50 values of 0.733 μM and 0.477 μM, respectively. QC-182 is applicable for hepatocellular carcinoma (HCC) research.

anti-TNBC agent-7 (Compound 13c) exhibits anticancer activity and functions as a molecular probe to identify and regulate the signaling of the USP21/JAK2/STAT3 axis. It demonstrates nanomolar cytotoxicity against MDA-MB-231 and HCC-1806 cancer cells, effectively combating triple-negative breast cancer (TNBC).

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.

DNH28 is a potent NF-κB and MAPK inhibitor with an IC50 value of 0.93 μM in HepG2 cells. It induces apoptosis by downregulating Bcl-2 and upregulating BAX and Cleaved-caspase-3 expression. DNH28 can arrest the cell cycle and inhibit cell migration, and is applicable for research in hepatocellular carcinoma (HCC).