Angiogenesis

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.

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.

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.

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

Silymarin (Silybin B) (Silybin B) is a polyphenolic flavonoid that extracts from the milk thistle or seeds of Silybum marianum. It is used in the prevention and treatment of liver diseases.

HA 155 (Autotaxin Inhibitor IV) is a boronic acid-based compound, inhibiting ATX with IC50 of 5.7 nM by selectively binding to its catalytic threonine.

PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC50 of 39.9 nM and a Ki of 42 nM. It also inhibits the PDGFR, EGFR, and c-Src tyrosine kinases with IC50 values of 310 nM, 240 nM, and 44 nM, respectively.

Isoliquiritin apioside, isolated from Glycyrrhizae radix rhizome, significantly decreases PMA-induced increases in MMP9 activities and suppresses PMA-induced activation of MAPK and NF-κB. Isoliquiritin apioside auppresseses invasiveness and angiogenesis o

(Rac)-Arnebin 1 (beta, beta-dimethylacrylshikonin) has anti-tumor, anti-inflammatory, anti-immune deficiency and protecting liver.

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).

MGCD-265 analog (Glesatinib) is an orally bioavailable multitargeted tyrosine kinase inhibitor with potential antineoplastic activity with IC50 of 29 nM and 10 nM for c-Met and VEGFR2, respectively.

Ibuprofen Lysine (Neoprofen) is a non-steroidal anti-inflammatory drug.

Angiogenesis inhibitor BT2 is a novel inhibitor of angiogenesis and vascular permeability, inhibiting ERK phosphorylation and the expression of FosB ΔFosB, VCAM-1, and many genes involved in proliferation, migration, angiogenesis, and inflammation, interacting with MEK1, suppressing retinal CD31, pERK, VCAM-1, and VEGF-A165 expression.

Angiogenesis Agent 1 (Compound C-31), a glycoside analogue derived from salidroside, acts as an activator of the HIF-1α pathway and shows potential in diabetic hind limb ischemia research [1].

Angiogenesis Inhibitor 3 (Compound 8) is a potent substance that effectively inhibits the growth of HUVEC and HCT-15 cells, demonstrating IC50 values of 1.00 and 0.71 μM, respectively. It not only induces apoptosis in these cells but also exhibits significant anticancer activity by suppressing cancer cell invasion. Furthermore, this compound successfully inhibits angiogenesis in zebrafish embryos [1].

Angiogenesis Inhibitor 4 is a potent agent for inhibiting angiogenesis, with potential applications in cancer research [1].

Penicillamine (Artamine), possessing antineoplastic properties, induces apoptosis by a p53-mediated mechanism and inhibits angiogenesis by chelating with copper, a cofactor for angiogenesis. Artamine is a beta dimethyl analog of the amino acid cysteine. As a degradation product of penicillin antibiotics, Artamine chelates with heavy metals and increases their urinary excretion.

Nintedanib (Intedanib) is a triple vascular kinase inhibitor that inhibits VEGFR1, VEGFR2, and VEGFR3 (IC50=34 13 13 nM), FGFR1, FGFR2, and FGFR3 (IC50=69 37 108 nM), PDGFRα, and PDGFRβ (IC50=59 65 nM). Nintedanib has antitumor activity and inhibits tumor growth by inhibiting angiogenesis.

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.

R1498 is an inhibitor of cyclin-dependent kinase 2. It also acts by targeting angiogenesis and mitosis pathways. It is well-tolerated and orally active for hepatocellular carcinoma and gastric cancer treatment.

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.