anti-angiogenesis

JK-P3 is a pyrazole-based inhibitor of VEGFR-2 (IC50: 7.8 μM). JK-P3 inhibits FGFR 1 3 kinase activity in vitro, but has no effect on FGFR signaling in cell-based assays. The compound blocks wound healing and tube formation in HUVEC without effecting endo

Chiauranib is a multi-target inhibitor against tumor angiogenesis and exhibits potent anticancer effects. Chiauranib potently inhibits the angiogenesis-related kinases (VEGFR1, VEGFR2, VEGFR3, PDGFRα and c-Kit), mitosis-related kinase Aurora B, and chronic inflammation-related kinase CSF1R, with IC50 values ranging from 1-9 nM.

TIE-2 VEGFR-2 kinase-IN-5 (TIE-2 and VEGFR-2 tyrosine kinase receptor inhibitor) is a potent agent with anti-angiogenic activity, commonly used in biomedical research focused on angiogenesis.

(±)4-HDHA (4-Hydroxy docosahexaenoic acid) is a PPARγ agonist with anti-inflammatory activity that directly inhibits endothelial cell proliferation and sprouting angiogenesis via PPARγ, which can be used in the study of diabetes.

MMPP is a novel VEGFR2 inhibitor with anti-inflammatory and potential anticancer activity, inhibits STAT3, inhibits angiogenesis via VEGFR2 AKT ERK NF-kappaB pathway, and can be used to alleviate myocardial injury.

Hexylresorcinol (4-Hexylresorcinol) is a substituted dihydroxybenzene utilized topically as an antiseptic for minor skin infection treatment.

Etoricoxib (MK-663) is a synthetic, nonsteroidal anti-inflammatory drug (NSAID) with antipyretic, analgesic, and potential antineoplastic properties. Etoricoxib specifically binds to and inhibits the enzyme cyclooxygenase-2 (COX-2), resulting in inhibition of the conversion of arachidonic acid into prostaglandins. Inhibition of COX-2 may induce apoptosis and inhibit tumor cell proliferation and angiogenesis.

Rofecoxib (MK 966) binds to and inhibits the enzyme cyclooxygenase-2 (COX-2), resulting in an inhibition of the conversion of arachidonic acid to prostaglandins. Rofecoxib is a synthetic, nonsteroidal derivative of phenyl-furanone with anti-inflammatory, antipyretic and analgesic properties and potential antineoplastic properties. COX-related metabolic pathways may represent key regulators of cell proliferation and neo-angiogenesis. Some epithelial tumor cell types overexpress pro-angiogenic COX-2.

Oltipraz (RP 35972) is a synthetic dithiolethione with potential chemopreventive and anti-angiogenic properties. Oltipraz induces phase II detoxification enzymes, such as glutathione S transferase (GST) and NAD(P)H: quinone oxidoreductase 1 (NQO1). The induction of detoxification enzymes enhances the detoxification of certain cancer-causing agents, thereby enhancing their elimination and preventing carcinogen-induced DNA damages. Although the exact mechanism through which the anti-angiogenesis effect remains to be fully elucidated, oltipraz maybe able to modulate the expression of a number of angiogenic factors, thereby blocking the sustained and focal neovascularization in multiple tumor cell types.

Tanshinone IIA (Tanshinone B) is a diterpene quinone natural product that targets the protein kinase domain of VEGF VEGFR2. Tanshinone IIA inhibits angiogenesis and exhibits anti-inflammatory, antioxidant, and therapeutic activities against coronary heart disease.

Ibuprofen (Advil) is a propionic acid derivate and nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic, and antipyretic effects. Ibuprofen inhibits the activity of cyclo-oxygenase I and II, resulting in a decreased formation of precursors of prostaglandins and thromboxanes.

Tranilast (SB 252218), an antiallergic drug, suppresses lipid mediator and cytokine release from inflammatory cells, therefore utilized in the treatment of allergic disorders.

Formononetin (Flavosil) is an O-methylated isoflavone and a phytoestrogen from the root of Astragalus membranaceus.

Theaflavin 3,3'-digallate, a major polyphenol found in black tea, is an inducer of oxidative stress which has anti-inflammatory and cancer chemopreventive actions, it reduces tumor angiogenesis by downregulating HIF-1αand VEGF.

20(S)-Ginsenoside Rg3 (Rg3) possess an ability to inhibit the lung metastasis of tumor cells via inhibition of the adhesion and invasion of tumor cells. It inhibits the proliferation of human umbilical vein endothelial cells(HUVEC) and has anti-angiogenesis activities.

SC144 is an orally active small-molecule gp130 inhibitor.

1. 6-Shogaol (6-Shogaol) has antipyretic and analgesic effects in addition to inhibitory effect on lipoxygenase activity. 2. 6-shogaol has anti-inflammatory property, reduces the inflammatory response and protected the femoral cartilage from damage produced in a CFA monoarthritic model of the knee joint of rats. 3. 6-Shogaol inhibits the growth of human cancer cells and induces apoptosis in COLO 25 cells through modulation of mitochondrial functions regulated by reactive oxygen species (ROS). 4. 6-Shogaol effectively inhibit invasion and metastasis of hepatocellular carcinoma through diverse molecular mechanisms, including inhibition of the MAPK and PI3k Akt pathways and NF-κB and STAT3 activities to suppress expression of MMP-2 -9 and uPA and block angiogenesis, could further regulate urokinase-type plasminogen activity.

IMS2186 is a reagent with activity of antichoroidal neovascularization (CNV). IMS2186 could arrest cancer cell cycle in G2 M phase, result in exerting anti-proliferation and anti-angiogenesis effects. IMS2186 reduces the amount of eye leakage and diseased cells with no intraocular toxicity.

PNU-145156E (FCE26644) a novel angiogenesis inhibitor, has been shown to block circulating angiogenesis promoting growth factor in animal studies and has shown anti-tumor effects in solid tumors in mice.

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.

Suramin is a dual-function inhibitor of SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) and protein tyrosine phosphatases (PTPases), with antiparasitic, anticancer, and anti-angiogenesis properties, inhibiting sirtuins and DNA topoisomerase II.

MYLS22 is a first-in-class and selective inhibitor of optic atrophy 1 (OPA1) . MYLS22 can target endothelial OPA1 to curtail tumor growth and inhibits angiogenesis by impinging on NFkB activity and on angiogenic gene expression. It with anti-angiogenesis and anti-cancer activity.

Tanshinol borneol ester, an angiogenesis stimulator, enhances multiple critical phases of angiogenesis via the Akt and MAPK signaling pathways and exhibits anti-ischemic and anti-atherosclerosis properties [1].

Apricoxib, also known as Benzenesulfonamide 42(4ethoxyphenyl)4methyl1Hpyrrol1yl, is an orally bioavailable nonsteroidal anti-inflammatory agent (NSAID) with potential antiangiogenic and antineoplastic activities. Apricoxib binds to and inhibits the enzyme cyclooxygenase-2 (COX-2), thereby inhibiting the conversion of arachidonic acid into prostaglandins. Apricoxib-mediated inhibition of COX-2 may induce tumor cell apoptosis and inhibit tumor cell proliferation and tumor angiogenesis. COX-related metabolic pathways may represent crucial regulators of cellular proliferation and angiogenesis.