anti-angiogenesis

Takeda-6d, a novel, potent DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor, inhibits B-RAF and VEGFR2 with IC50 of 7.0nM and 2.2nM.

Oglufanide (H-Glu-Trp-OH) is a naturally occurring thymic immunomodulator that inhibits vascular endothelial growth factor (VEGF).

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.

SC144 is an orally active small-molecule gp130 inhibitor.

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.

(±)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.

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.

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.

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

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

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.

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.

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.

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

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.

beta-Escin is a natural mixture of triterpenoid saponins isolated from horse chestnut (Aesculus hippocastanum) seeds, can be used as a vasoprotective anti-inflammatory, anti-edematous and anti-nociceptive agent.

Chlorahololide D is a natural lindane-type sesquiterpene dimer and selective potassium channel blocker that stimulates reactive oxygen species ROS levels to cause cell cycle arrest in the G2 phase, modulates Bcl-2 and Bax and FAK, thereby inhibiting MCF-7 cell growth and triggering apoptosis. Chlorahololide D inhibits tumor proliferation, migration and angiogenesis in in vivo experiments and has anti-breast cancer potential.

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.

3'- O- Acetylhamaudol, isolated from the roots of Angelica japonica, exhibits anti-tumor activity through dual actions, anti-angiogenesis and intestinal intraepithelial lymphocyte activation.

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.

FAK inhibitor 2, antitumor and anti-angiogenesis activitiesis ,is a potent focal adhesion kinase (FAK) inhibitor with an IC50 of 0.07 nM .

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.

HS-345, a TrkA/Akt inhibitor, exhibits potent anti-pancreatic cancer properties. This compound inhibits the growth and proliferation of pancreatic cancer cells by blocking the TrkA/Akt signaling pathway and induces cell apoptosis (Apoptosis). Additionally, HS-345 inhibits angiogenesis by reducing the expression of HIF-1α and VEGF. It holds promise for use in pancreatic cancer research.