antiangiogenic

Amifostine (Ethyol) anhydrous is a cytoprotective agent, acts as a free radical scavenging activity.

AKB-6899 is an inhibitor of prolyl hydroxylase domain 3 (PHD3) and increases the soluble form of the VEGF receptor (sVEGFR-1) production from GM-CSF-treated macrophages. AKB-6899 leads to stabilization of HIF-2α which induces sVEGFR-1 production from tumor-associated macrophages and decreases tumor growth.

Itraconazole (R51211) is a triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes necessary for ERGOSTEROL synthesis.

Mycophenolic acid (Mycophenolate) is an inosine monophosphate dehydrogenase(IMPDH) inhibitor with anti-proliferative activity.

Regorafenib (BAY 73-4506) is an orally active, multi-targeted receptor tyrosine kinase inhibitor that inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ, exhibiting both antitumor and anti-angiogenic activity.

Regorafenib Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, KIT, RET, RAF-1, B-RAF and B-RAF(V600E) respectively.

Cabozantinib (XL184) is a multi-targeted tyrosine kinase receptor inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt3 (IC50=0.035/1.3/4.6/7/11.3 nM). Cabozantinib exhibits both antitumor and antiangiogenic activity.

Bucillamine (DE019) protects against Ischemia/reperfusion injury in high-risk organ transplants and inhibits the production of VEGF. Bucillamine is an orally active sulfhydryl donor and antioxidant with antirheumatic and antiangiogenic properties. Bucillamine can be used for studies about choroidal neovascularization and rheumatoid arthritis.

AAL-993 is a potent VEGFR inhibitor with IC50s of 130 nM, 23 nM and 18 nM for VEGFR1, VEGFR2 and VEGFR3, respectively. AAL993 has a weak inhibitory effect on other tyrosine kinases. AAL993 also shows potent antiangiogenic and antitumor activities.

Rhapontigenin (Protigenin) is a mechanism-based, selective inactivator of cytochrome P450 1A1 (IC50: 400 nM), an aryl hydrocarbon hydroxylase which activates polycyclic aromatic hydrocarbons that act as procarcinogens. Rhapontigenin is a natural analog of resveratrol with antioxidant and anti-cancer activity. At higher concentrations, rhapontigenin inhibits the proliferation of HL-60R and HepG2 cancer cell lines (IC50: 48 μM).

KG5 is a dual allosteric inhibitor of PDGFRβ and B-Raf with a Kd of 520 nM and 300 nM for PDGFRβ and PDGFRα. KG5 inhibits FLT3, KIT, and c-Raf with anticancer and antiangiogenic activities.

Cabozantinib hydrochloride (XL184) is a potent pan-tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt4 (IC50s: 0.035, 1.3, 4.6, 7 and 6 nM).

Delanzomib (CEP-18770) is an orally active inhibitor of the chymotrypsin-like activity of proteasome (IC50: 3.8 nM). It only marginally inhibits the tryptic and peptidylglutamyl activities of the proteosome.

Morellic acid has anti-cancer activity, it strongly inhibited the migration of HUVEC at a low concentration of 0.5 μM in HUVEC cell migration assay in vitro. Morellic acid also has antiangiogenic activity.

Antiangiogenic agent 6 (Pt-1) effectively inhibits angiogenesis and induces necroptosis in tumor cells.

Antiangiogenic agent 7 (Compound 1) induces apoptosis, elevates Reactive Oxygen Species (Reactive Oxygen Species), and inhibits the intracellular enzyme thioredoxin reductase. It exhibits anticancer activity with IC50 values ranging from 0.08 to 3.5 μM against cervical cancer cells (HeLa), prostate cancer cells (PC-3), and non-small cell lung cancer cells (A549). Additionally, Antiangiogenic agent 7 suppresses tumor growth in a mouse xenograft model.

Antiangiogenic agent 8 (Compound 3m) functions as both an antibacterial agent and an antiangiogenic compound. It shows minimum inhibitory concentrations (MIC) of 16, 8, 4, 16, and 8 μg/mL against E. coli, P. aeruginosa, B. subtilis, S. aureus, and C. glabrata, respectively, with minimum bactericidal concentrations (MBC) ranging from 32 to 64 μg/mL. This compound holds potential for applications in infection control and cardiovascular disease research.

Antiangiogenic agent 2 (compound 3b) is a potent thymidine phosphorylase inhibitor (IC50: 39.71 μM) with demonstrated anti-angiogenic effects.

Antiangiogenic agent 3 is a potent inhibitor of human umbilical vein endothelial cells (HUVEC), effectively blocking HUVEC migration and chemotactic motilities. Additionally, it suppresses the gene expression of Src, cdc42, and MAPK, manifesting its strong antiangiogenic properties.

Compound 3b, an antiangiogenic agent, inhibits Akt phosphorylation in both HFF and HUVEC cells and is utilized in cancer research [1].

Antiangiogenic Agent 5 (Compound 17) exhibits potent anti-angiogenic activity by inhibiting SRPK 1 with an IC50 of 1.3 nM [1].

Suramin Sodium Salt (BAY-205) is a sodium salt form of suramin, a polysulphonated naphthylurea with potential antineoplastic activity. Suramin blocks the binding of various growth factors, including insulin-like growth factor I (IGF-I), epidermal growth factor (EGF), platelet-derived growth factor (PDGF), and tumor growth factor-beta (TGF-beta), to their receptors, thereby inhibiting endothelial cell proliferation and migration. This agent also inhibits vascular endothelial growth factor (VEGF)- and basic fibroblast growth factor (bFGF)-induced angiogenesis; retroviral reverse transcriptase; uncoupling of G-proteins from receptors; topoisomerases; cellular folate transport; and steroidogenesis.

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

Notoginsenoside R1 (Sanchinoside R1) has been shown to exhibit antioxidant, antiapoptotic, anti-inflammatory, and immune-stimulatory properties.