mgc-803

Anticancer agent 46 is a potent anti-cancer agent, showing anti-proliferative activity in cellular assays, with an IC50 of 0.986 μM against MGC803 cells.

WS-383 is a selective, potent and reversible DCN1-UBC12 interaction inhibitor(IC50 of 11 nM).

YSY01A is a proteasome inhibitor that suppresses cancer cell survival by inducing apoptosis (Apoptosis). It demonstrates IC50 values against various cell lines such as HEK293T, A549, MCF-7, MGC-803, and PC-3M with values of 51.01, 9.21, 5.21, 8.9, and 35.4 nM respectively. Additionally, YSY01A serves as a degrader of gp130 and JAK2, eliminating constitutive STAT3 signaling in human A549 lung cancer cells by downregulating gp130 and JAK2. YSY01A holds potential for research in cancer therapeutics.

c-Fos-IN-1 (Compound P16) acts as a c-Jun inhibitor, effectively reducing the mRNA and protein levels of c-Fos. It also inhibits the phosphorylation activity of ERK and the transcriptional activity of AP-1. This compound demonstrates anticancer properties through the inhibition of the ERK c-Fos Jun pathway. c-Fos-IN-1 curbs the proliferation and migration of gastric cancer cells, with an IC50 of 2.31 μM for MGC-803 cells, causing cell cycle arrest at the G2 M phase and inducing apoptosis in cancer cells. Additionally, c-Fos-IN-1 hampers the growth of gastric cancer tumors.

Tubulin polymerization-IN-76 (compound 20b) is a potent and orally active inhibitor of tubulin polymerization. It acts at the colchicine binding site to inhibit tubulin polymerization with an IC50 value of 2.505 μM, effectively disrupting the intracellular microtubule network and interfering with mitosis. Tubulin polymerization-IN-76 shows significant inhibitory effects on MGC-803 and HGC-27 cells, with IC50 values of 1.61 and 1.82 nM, respectively. It effectively suppresses colony formation and cell migration activities in these cell lines, inducing G2 M phase cell cycle arrest and apoptosis (Apoptosis). Furthermore, Tubulin polymerization-IN-76 exhibits broad-spectrum antiproliferative activity.

(Rac)-Shikonin (Anchusin) is a natural red naphthoquinone pigment, has antimicrobial, anti-tumor, and anti-inflammatory effects; a purified shikonin preparation is widely used for the production of medicinals, cosmetics, and some food products; shikonin also enters into the antiinflammatory ointment and cream compositions used for the treatment of burns. It can suppress the cell viability, adhesion, invasion and migratory ability of MGC-803 cells through TLR2- or NF-κB-mediated pathway.

(-)-Alkannin (Shikonin) is a natural red naphthoquinone pigment, has antimicrobial, anti-tumor, and anti-inflammatory effects; a purified shikonin preparation is widely used for the production of medicinals, cosmetics, and some food products; shikonin also enters into the antiinflammatory ointment and cream compositions used for the treatment of burns. It can suppress the cell viability, adhesion, invasion and migratory ability of MGC-803 cells through TLR2- or NF-κB-mediated pathway.

p53 Activator 2 (compound 10ah) intercalates into DNA, causing significant double-strand breaks and upregulating the expression of p53, p-p53, CDK4, and p21, leading to cell cycle arrest at the G2 M phase. It induces apoptosis, reduces anti-apoptosis proteins Bcl-2, Bcl-xL, and cyclin B1 levels, and shows anti-proliferative activity against MGC-803 cells with an IC50 of 1.73 μM. Additionally, p53 Activator 2 exhibits potent anticancer effectiveness in MGC-803 xenograft tumor models [1].

Keap1-Nrf2-IN-4, a powerful neddylation inhibitor, demonstrates significant anti-proliferation activity against MGC-803 cells (IC50 = 2.55 μM), effectively impeding their migration and inducing apoptosis. Additionally, it effectively inhibits tumor growth while exhibiting minimal toxicity [1].

Tubulin inhibitor 22 (compound 4c) is a potent tubulin inhibitor exhibiting anti-angiogenic and anti-cancer activity, which blocks the cell cycle of MGC-803 cells in the G2 M phase and induces Caspase-mediated apoptosis through mitochondrial dysfunction in a dose-dependent manner.

Antitumor agent-58 is an antitumour agent that effectively inhibits colony formation and cell migration in MGC-803 cells and induces mitochondrial dysfunction in MGC-803 cells. Antitumor agent-58 exhibited potent inhibitory activity against tumour growth in xenograft models carrying MGC-803 cells.

LSD1-IN-26 (compound 12u), a potent LSD1 inhibitor, exhibits an IC50 of 25.3 nM. It also demonstrates inhibition of MAO-A (IC50 = 1234.57 nM) and MAO-B (IC50 = 3819.27 nM), significantly inducing apoptosis in MGC-803 cells. This compound is applicable in gastric cancer research [1].

Tubulin inhibitor 35 (Tubulin IN 35) is a potent dual inhibitor of topoisomerase I and microtubule protein polymerization with antitumor activity, inhibits migration and invasion of MGC-803 and RKO cell lines, interrupts the cell cycle and induces apoptosis.

MY-1076 is a potent YAP inhibitor with antigastric cancer activity.MY-1076 dose-dependently induced G2 M phase block, induced YAP degradation and apoptosis, and inhibited microtubule protein polymerization.MY-1076 inhibited the proliferation of MGC-803, SGC-7901, HCT-116, and KYSE450 cells.

Antitumor agent-97 (compound 42), an anticancer agent, effectively inhibits proliferation and autophagy in MGC 803 cells, induces apoptosis, and enhances ROS accumulation, proving useful in cancer research [1].

Marsdenoside B (compound 8), an isolate from the Alocasia genus, exhibits antitumor activity by inhibiting the proliferation of MGC-803 and HT-29 tumor cell lines with IC50 values of 25.6 μg mL and 32.4 μg mL, respectively.

Marsdenoside A (compound 7), an isolated compound from the Alocasia genus, exhibits a weak inhibitory effect on the growth of two tumor cell lines, MGC-803 and HT-29, with IC50 values exceeding 50 μg mL.

FAK-IN-12 (Compound 12S) is a selective FAK inhibitor with an IC50 of 47 nM, effectively suppressing proliferation of MGC-803, HCT-116, and KYSE30 cells with IC50 values of 0.24, 0.45, and 0.44 μM, respectively. Additionally, FAK-IN-12 promotes apoptosis and cellular senescence [1].

Cannogenol 3-O-β-gentiobiosyl-(1→4)-α-L-thevetoside (Compound 12), a cardiac glycoside extracted from Thevetia peruviana seeds, exhibits cytotoxic effects on SW1990 and MGC-803 cells with IC50 values of 9.52 and 7.70 μM, respectively [1].

Antitumor Agent-122 (Compound 5j), characterized by its effective antitumor properties and minimal toxicity and resistance, exhibits strong antiproliferative effects against various cancer cell lines, including MGC-803, HepG2, SKOV3, and T24. It demonstrates IC 50 values of 5.23 μM, 3.60 μM, 1.43 μM, and 3.03 μM, respectively [1].

HDAC6-IN-38 (Compound Z-7), characterized as a potent histone deacetylase 6 (HDAC6) inhibitor, exhibits an IC50 of 3.25 nM. It effectively inhibits the proliferation of MGC‑803 cells [1].

Skp2 inhibitor 1 is a Skp2-Cks1 interaction inhibitor (IC50: 2.8μM) with antitumor activity and can be used to study cancer.

VEGFR-2-IN-51 (compound 19) is an orally active dual-target inhibitor of VEGFR-2 (IC50=15.33 μM) and tubulin (IC50=0.76 μM) that exhibits antitumor activity. This compound induces apoptosis in tumor cells by reducing mitochondrial membrane potential and increasing levels of reactive oxygen species (ROS). Additionally, VEGFR-2-IN-51 suppresses angiogenesis through inhibition of the VEGFR-2 PI3K AKT signaling pathway. Moreover, it demonstrates significant antiproliferative effects on the gastric cancer cell line MGC-803 (IC50=0.005 μM).

Uralsaponin C shows the cytotoxic activity against the human cancer cell lines MGC-803, SW620, and SMMC-7721 with IC50 > 100 μmol/L.