anti-metastasis

CCG-203971 is an inhibitor of SRE activation in the prostate cancer cell line PC-3 (IC50: 6.4 μM), with 87% inhibition of SRE activation achieved at 100 μM. This compound also inhibits PC-3 cell migration (IC50: 4.2 μM), as determined by a scratch wound assay. CCG-203971(CCG203971) causes no cytotoxicity when evaluated by the WST-1 assay. It is well tolerated in normal mice up to doses of 100 mg/kg given intraperitoneally over five days.

Selvigaltin (GB1211) is an orally administered, highly selective small-molecule inhibitor of galectin-3 (Gal-3) with an IC₅₀ value of 12 nM in rabbits, exhibiting anticancer and anti-fibrotic activity. Selvigaltin reduces galectin-3 levels in the liver and decreases biomarkers of inflammation (cellular foci) and fibrosis (PSR, SHG), while simultaneously lowering the mRNA and protein expression of inflammatory and fibrotic biomarkers (IL-6, TGF-β3, SNAI2, collagen). Selvigaltin also restores T-cell activity and reduces tumor growth and metastasis. Selvigaltin is suitable for use in studies of liver fibrosis, non-alcoholic steatohepatitis (NASH), and tumors.

MMP-9-IN-1 is an inhibitor of specific matrix metalloproteinase-9 (MMP-9).

OB 24 hydrochloride is a selective, orally active HO-1 inhibitor (IC50=1.9 μM) exhibiting antitumor and anti-metastatic properties, suitable for studying prostate cancer, melanoma, ovarian cancer, and lung cancer metastasis.

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.

NMac1 (Nm23 activator 1) is a natural compound, cassumunene, derived from Zingiber cassumunar Roxb. and traditionally used as an anti-inflammatory agent in East Asia. NMac1 exhibits anti-metastatic potential by directly interacting with the C-terminal of Nm23-H1, activating its NDP kinase (NDPK) enzymatic activity in vitro. NMac1 inhibits breast cancer metastasis in vivo.

AhR modulator-1 is a selective and orally active aryl hydrocarbon receptor (AhR) modulator. It inhibits metastasis, in part, by inhibiting prostatic VEGF production prior to tumor formation. It also possesses anti-estrogenic properties in rat uterus.

Borrelidin (Treponemycin) is a nitrogen-containing macrolide antibiotic isolated from Streptomyces rochei, which inhibits sugar-acyl-tRNA synthetase. It exhibits anticancer, antifungal, and anti-angiogenesis activities, inhibiting tumor growth and lung metastasis.

possesses anticancer, anti-invasive, anti-metastasis, anti-angiogenic and pro-apoptosis properties with high safety.Frondoside A, a natural glycoside extracted from the sea cucumber, Cucumaria frondosa,

R916562 is an orally active, selective Axl/VEGF-R2 inhibitor with IC50 values of 136 nM and 24 nM, respectively, demonstrating anti-angiogenesis and anti-metastasis properties.

CXCR4 antagonist 10 is a small-molecule antagonist of the chemokine receptor CXCR4 that inhibits related signaling pathways and cell migration by blocking the binding of CXCR4 to its ligand, CXCL12 (SDF-1). In vitro studies have shown that CXCR4 antagonist 10 can interfere with tumor cell metastasis and immune cell chemotaxis, demonstrating potential value in antitumor and anti-inflammatory research.

Pixatimod (also known as PG-545) is a synthetic carbohydrate-modified heparan sulfate mimetic and a Toll-like receptor 9 (TLR9) agonist. It exhibits potential immunostimulatory, antitumor, and antiviral effects. Pixatimod effectively inhibits SARS-CoV-2 by disrupting the spike protein-ACE2 interaction. Additionally, it blocks various cancer-promoting processes such as cell proliferation, invasion, metastasis, angiogenesis, and epithelial-mesenchymal transition. These effects have demonstrated significant efficacy in numerous mouse cancer models, including about 30 xenograft models and 20 syngeneic models. Pixatimod has been tested in combination with several approved anticancer compounds, showing clinical potential when used with gemcitabine, paclitaxel, sorafenib, platinum compounds, and anti-PD-1 antibodies.

Pixatimod (also known as PG-545) is a synthetic modified heparan sulfate mimetic and an agonist of Toll-like receptor 9 (TLR9), showcasing potential immunostimulatory, antitumor, and antiviral properties. It effectively inhibits SARS-CoV-2 by disrupting the interaction between the spike protein and ACE2. Moreover, Pixatimod blocks cancer-promoting processes such as cell proliferation, invasion, metastasis, angiogenesis, and epithelial-mesenchymal transition. These activities have demonstrated significant efficacy across various murine cancer models, including approximately 30 xenograft models and 20 syngeneic models. Pixatimod has been tested in combination with several approved anticancer compounds, underscoring its clinical potential, with drugs like gemcitabine, paclitaxel, sorafenib, platinum-based compounds, and an anti-PD-1 antibody.

iHAC is an inhibitor-HSP90 anchoring chimera that covalently binds to the BRD4 ligand (+)-JQ-1, targeting HSP90 and thereby inhibiting cancer cell proliferation. This compound also triggers an anti-tumor immune response and is effective in suppressing the recurrence and metastasis of 4T1 breast cancer in mouse models.

2-Deoxy-L-ribose is the stereoisomer of 2-Deoxy-D-ribose and can inhibit the anti-apoptotic effects of 2-Deoxy-D-ribose. Additionally, 2-Deoxy-L-ribose is capable of suppressing tumor cell metastasis by downregulating thymidine phosphorylase overexpression.

HPH-15 is an anti-cell migration compound that inhibits cell movement by binding to hnRNP U or suppressing TGF-β. Additionally, it prevents epithelial-to-mesenchymal transition (EMT). HPH-15 holds potential for research in areas such as anti-tumor metastasis and anti-fibrosis.

Platelet aggregation-IN-3 (Compound 5) acts as a ligand for H2 histamine receptors, α2(A,C)-adrenergic receptors (α2-AR), and 5-HT2(B,C) serotonin receptors. This compound can inhibit platelet aggregation induced by ADP and collagen, and it also modulates tumor cell-induced platelet aggregation (TCIPA). Platelet aggregation-IN-3 is a promising candidate for anti-platelet therapy in cardiovascular disease and the prevention of cancer-associated thrombosis and tumor metastasis.

ST6GAL1-IN-1 (compound 4e) is a potent selective inhibitor of ST6GAL1, with an IC50 value of 20.0 μM. It demonstrates anti-metastatic activity by effectively inhibiting the migration of MDA-MB-231 cells. Furthermore, ST6GAL1-IN-1 is capable of suppressing tumor growth and metastasis in vivo.

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.

VEGFR-2-IN-68 (13b) is an inhibitor of VEGFR-2 with an IC50 value of 41.51 nM. It can induce apoptosis and cause G2/M cell cycle arrest, as well as exhibit anti-cancer metastasis properties.

Anti-TNBC agent-5 (compound 10C) is an inhibitor of triple-negative breast cancer (TNBC) that exhibits favorable stability and pharmacokinetic properties. It demonstrates antiproliferative activity across various cancer cell types. Additionally, in the MDA-MB-231 xenograft model, anti-TNBC agent-5 effectively suppresses TNBC lung metastasis activity. This compound is useful for cancer research.

CPS-021 is a selective PAK4PROTAC degrader with a DC50 of 50 nM. It demonstrates potent anti-migration and anti-invasion properties, significantly inhibiting the invasion and metastasis of tumor cells in an A549-luc lung metastasis mouse model.

Rac1-IN-5 is a selective, reversible inhibitor of the RAC1 protein with a dissociation constant (KD) of 30 nM. It competes specifically with guanine nucleotides for binding to RAC proteins, effectively blocking RAC1 activity and RAC1-dependent cellular functions. In vivo, Rac1-IN-5 exhibits anti-tumor metastasis effects and can improve survival rates. This compound is applicable for research on aggressive cancers such as triple-negative breast cancer and colon cancer.

Tubulin/VEGFR-2-IN-2 is an orally active dual inhibitor of tubulin and VEGFR-2, with IC50 values of 3.27 μM and 0.09 μM, respectively. This compound exerts antitumor effects through multiple pathways, including enhancing reactive oxygen species (ROS) production, disrupting mitochondrial membrane potential, inducing apoptosis, and causing cell cycle arrest. Tubulin/VEGFR-2-IN-2 also demonstrates significant anti-angiogenic properties in vitro, effectively inhibiting endothelial cell migration, invasion, and tube formation. Furthermore, in vivo, it inhibits angiogenesis, tumor growth, and metastasis. Tubulin/VEGFR-2-IN-2 is applicable for research on non-small cell lung cancer, breast cancer, gastric cancer, and lymphoma.