antimetastatic

Ganoderic acid F exhibits antitumor and antimetastatic activities through inhibition of angiogenesis and alteration of proteins involving cell proliferation and/or cell death, carcinogenesis, oxidative stress, calcium signaling, and endoplasmic reticulum

Vactosertib (EW-7197) is an orally bioavailable inhibitor of the serine/threonine kinase, transforming growth factor (TGF)-beta receptor type 1 (TGFBR1), also known as activin receptor-like kinase 5 (ALK5), with potential antineoplastic activity.

Antimetastatic agent-1 (Compound A-23) is a MET inhibitor. It effectively suppresses cancer metastasis.

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

CLEFMA has anti-proliferative activity. CLEFMA inhibits tumor growth associated with NF-κB-regulated anti-inflammatory and anti-metastatic effects.

LY3200882 is a highly selective inhibitor of TGF-β receptor type 1 (TGFβRI).

Pivanex (Pivalyloxymethyl butyrate) is an orally active HDAC inhibitor and an antimetastatic and antiangiogenic agent. Pivanex downregulates the Bcr-Abl protein and enhances apoptosis.

1. Octyl Gallate is an antioxidant approved by the US Food and Drug Administration (FDA) as a food additive. 2. Octyl Gallate has antimetastatic activity. 3. Octyl Gallate shows antimicrobial activity against H. pylori, with a minimum inhibitory concentration (MIC) value of 125 ug/mL. 4. Combination therapy with octyl gallate and ferulic acid improves cognition and neurodegeneration in a transgenic mouse model of Alzheimer's disease.5. Octyl Gallate is a potential anticancer agent, it exhibited decreased MCF-7 & MDA-MB-231 survival and induced apoptosis, with IC50 value of 40 uM. 6. Octyl gallate (Octyl 3,4,5-trihydroxybenzoate) has antiviral activity, it shows an inhibitory effect on the growth of herpes simplex virus type 1 (HSV-1) in HEp-2 or Vero cells. 7. Octyl gallate shows antifungal activity against Saccharomyces cerevisiae ATCC7754 and Zygosaccharomyces bailii ATCC 60483.

(Rac)-SAR131675 is an effective and specific VEGFR-3 inhibitor. It inhibited VEGFR-3 tyrosine kinase activity (IC50: 20 nmol/L) and VEGFR-3 autophosphorylation (IC50: 45 nmol/L) in HEK cells, respectively. SAR131675 is highly specific for VEGFR-3 versus 107 receptors, enzymes, ion channels, and 65 kinases. SAR131675 is a highly specific VEGFR-3-TK inhibitor with significant antitumoral and antimetastatic activities in vivo through inhibition of lymphangiogenesis and TAM invasion.

Upamostat, also known as Mesupron and WX-671, is an orally bioavailable second-generation serine protease inhibitor prodrug derived from 3-amidinophenylalanine. It targets the human urokinase plasminogen activator (uPA) system and exhibits potential antineoplastic and antimetastatic properties. After oral administration, the serine protease inhibitor WX-671 is converted into its active form, Nα-(2,4,6-triisopropylphenylsulfonyl)-3-amidinophenylalanine-4-ethoxycarbonylpiperazinylamide (WX-UK1), which inhibits multiple serine proteases, especially uPA, potentially hindering tumor growth and metastasis.

PPIA-IN-1 (Compound 20b) is an inhibitor of peptidyl-prolyl isomerase A (PPIA) with a KD of 0.52 μM. It demonstrates antiproliferative activity across various cancer cell lines, including an IC50 of 0.69 μM in HCT116 cells, induces cell cycle arrest at the G0/G1 phase, and exhibits antimetastatic effects in HCT116 cells. PPIA-IN-1 elevates ROS levels, causing DNA damage, ER stress, and mitochondrial dysfunction, and induces apoptosis in HCT116 cells via the MAPK pathway. Additionally, PPIA-IN-1 shows antitumor activity in a CT26 xenograft mouse model.

ZG-126 is an agonist of the vitamin D receptor (VDR) and an inhibitor of histone deacetylase (HDAC) with an IC50 range of 0.63-67.6 μM. It demonstrates cytotoxicity in cancer cell lines MDA-MB-231 and 4T1. In mouse models, ZG-126 exhibits antitumor and antimetastatic effects against melanoma and triple-negative breast cancer (TNBC). Additionally, it shows anti-inflammatory activity by reducing macrophage infiltration and polarization to the immunosuppressive M2 subtype.

PeS-9 is an androgen receptor (AR) degrader that induces the degradation of androgen receptors. It enhances the production of cytotoxic reactive oxygen species (ROS), leading to mitochondrial and endoplasmic reticulum stress, which results in the release of mitochondrial cytochrome C and AIF. PeS-9 activates caspase-9 and caspase-3, causing DNA fragmentation and apoptosis. It exhibits anti-prostate cancer activity and demonstrates antitumor and antimetastatic effects in vivo with minimal side effects. PeS-9 is applicable for targeted therapy research in GLUT-1 overexpressing tumors.

FAK-IN-28 is an orally active FAK inhibitor with an IC50 of 0.4 nM. It exhibits both antiproliferative and antimetastatic effects. FAK-IN-28 induces apoptosis by triggering caspase-3-dependent pathways through increased ROS levels. This compound effectively inhibits tumor growth without causing weight loss or hepatorenal toxicity. FAK-IN-28 is suitable for research on FAK-driven malignancies, including colon cancer, cervical cancer, triple-negative breast cancer, and melanoma.

ZINC69391 (CysHHC10 acetate(1408311-03-4 free base)) is a selective inhibitor of Rac1 with antiproliferative and antimetastatic effects. ZINC69391 interferes with the interaction of Rac1 with Dock180, reduces Rac1-GTP levels and induces apoptosis.

LY 189332 is an drug with antimetastatic activity.

Irigenin mediates its antimetastatic effect by specifically and selectively blocking the α9β1 and α4β1 integrin binding sites on the C-C loop of the Extra Domain A domain. It can sensitize TRAIL-induced apoptosis by enhancing the expression of pro-apoptotic molecules in gastric cancer cells and has anti-cancer effects.

HDAC-IN-36 is an orally active HDAC (histone deacetylase) inhibitor with an IC50 value of 11.68 nM for HDAC6. HDAC-IN-36 induces apoptosis, autophagy and inhibits migration. HDAC-IN-36 exhibits antitumor and antimetastatic effects and can be used to study breast cancer. HDAC-IN-36 exhibits antitumor and antimetastatic effects and can be used to study breast cancer.

Cathepsin L/S-IN-1, a dual inhibitor targeting Cathepsin L and Cathepsin S, exhibits potent and selective inhibition with IC50 values of 4.10 μM and 1.79 μM, respectively. Demonstrating significant antimetastatic and invasive effects, it effectively impacts pancreatic cancer BxPC-3 and PANC-1 cells.

Stem bromelain (EC 3.4.22.32), a cysteine proteinase from pineapple (Ananas comosus) stem, is a significant type of bromelain known for its fibrinolytic, antiedematous, antithrombotic, and anti-inflammatory properties. It also demonstrates in vivo antitumoral, antileukemic, and antimetastatic activities [1] [2].

Compound Rh1 (Anticancer agent 132) acts as an inducer of apoptosis and autophagy, exhibiting both antitumor and antimetastatic activities. It also arrests the cell cycle and inhibits cell proliferation [1].

Compound Rh2 (Anticancer agent 133) is a cytotoxic and antimetastatic agent that induces cell cycle arrest, apoptosis, and autophagy. Additionally, it suppresses cell metastasis through the inhibition of EGFR expression, which is mediated by FAK-regulated integrin β1 [1].

22-(4′-py)-JA, a semisynthetic derivative of junamycin A isolated from the Thai blue sponge (Xestospongia sp.), exhibits antimetastatic properties by inhibiting the AKT/mTOR/p70S6K signaling pathway. It also impedes tumor cell invasion and angiogenesis in human umbilical vein endothelial cells (HUVEC), while suppressing the expression of metalloproteinases (MMP-2 and MMP-9), hypoxia-inducible factor 1α (HIF-1α), and vascular endothelial growth factor (VEGF). Its potent anticancer activity is particularly noted against non-small cell lung cancer (NSCLC) [1].

Mal-va-mac-SN38 is a conjugate molecule functioning as an ADC (Antibody-Drug Conjugate) drug-linker. This compound comprises the cytotoxic ADC agent SN-38 and a linker. Once inside the body, Mal-va-mac-SN38 rapidly forms a covalent bond with endogenous albumin, resulting in the formation of HSA-va-mac-SN38. It demonstrates remarkable stability in human plasma and exhibits both antitumor and antimetastatic properties.