Endothelial lipase inhibitor-1 is a potent endothelial lipase inhibitor with an IC50 of 49 nM.

Nitric Oxide Synthase (599-613) Blocking Peptide, Bovine Endothelial Cell (Ac-Pro-Tyr-Asn-Ser-Ser-Pro-Arg-Pro-Glu-Gln-His-Lys-Ser-Tyr-Lys-Cys) is a peptide that inhibits the function of NOSs as a result it blocks the production of NO. Because of the invol

Imeglimin hydrochloride (EMD 387008 hydrochloride) prevents human endothelial cell death by inhibiting mitochondrial permeability transition without inhibiting mitochondrial respiration.

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

Sorafenib (Bay 43-9006) is a multikinase inhibitor that inhibits Raf-1, B-Raf, VEGFR2, VEGFR3, VEGFR4, PDGFRβ, FLT3, c-Kit, and others (IC50=6/22/90/15/20/20/57/58 nM) with oral activity. Sorafenib has antitumor activity and can induce autophagy and apoptosis as well as agonistic iron death.

BMS-309403 is an effective, selective and cell-permeable inhibitor of fatty acid binding protein 4 (FABP4) with a Ki of less than 2 nM.

Tesevatinib (XL-647) is an orally available, multi-target tyrosine kinase inhibitor (IC50s: 0.3, 16, 1.5, 8.7, and 1.4 nM for EGFR, ErbB2, KDR, Flt4, and EphB4).

Lenvatinib (E7080) is a multi-target receptor tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, KIT, PDGFR, and RET, and has oral activity. Lenvatinib has the strongest inhibitory activity on VEGFR2 and VEGFR3 (IC50=4/5.2 nM). Lenvatinib has strong anti-tumor activity.

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.

Blebbistatin ((±)-Blebbistatin) is a selective non-muscle myosin II (NMII) inhibitor. It promotes directional migration of corneal endothelial cells (CECs) and accelerates wound healing. Furthermore it preserves cell junctional integrity and barrier function.Blebbistatin is an inhibitor of MYH9.

Vardenafil (Vivanza) is an oral therapy for the treatment of erectile dysfunction. It is a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5). Penile erection is a hemodynamic process initiated by the relaxation of smooth muscle in the corpus cavernosum and its associated arterioles. During sexual stimulation, nitric oxide is released from nerve endings and endothelial cells in the corpus cavernosum. Nitric oxide activates the enzyme guanylate cyclase resulting in increased synthesis of cyclic guanosine monophosphate (cGMP) in the smooth muscle cells of the corpus cavernosum. The cGMP in turn triggers smooth muscle relaxation, allowing increased blood flow into the penis, resulting in erection. The tissue concentration of cGMP is regulated by both the rates of synthesis and degradation via phosphodiesterases (PDEs). The most abundant PDE in the human corpus cavernosum is the cGMPspecific phosphodiesterase type 5 (PDE5); therefore, the inhibition of PDE5 enhances erectile function by increasing the amount of cGMP.

YT 146 is a selective adenosine receptor A2 agonist with cardioprotective and vasodilatory effects that inhibits neointimal thickening after endothelial injury in rat femoral arteries.

Pazopanib (GW786034), a small molecule inhibitor, inhibits multiple protein tyrosine kinases with potential antineoplastic activity. Pazopanib selectively inhibits VEGFR-1, -2 and -3, c-kit and PDGF-R, which may result in inhibition of angiogenesis in tumors in which these receptors are upregulated.

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.

Tanshinone IIA (Tanshinone B)(Tanshinone B) is the diterpene quinone in Danshen, which is utilized in the treatment of cardiovascular and inflammatory.

2-Methoxyestradiol (2-ME2) is an orally bioavailable estradiol metabolite with potential antineoplastic activity. 2-Methoxyestradiol inhibits angiogenesis by reducing endothelial cell proliferation and inducing endothelial cell apoptosis. This agent also inhibits tumor cell growth by binding to tubulin, resulting in antimitotic activity, and by inducing caspase activation, resulting in cell cycle arrest in the G2 phase, DNA fragmentation, and apoptosis.

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

1. Farrerol has antioxidative activity.2. Farrerol modulates TAP and BNBD5 gene expression in mammary gland, enhances bMEC defense against S. aureus infection and could be useful in protection against bovine mastitis. 3. Farrerol inactivates KEAP-1 or act

AVE-9488 is a novel endothelial NO synthase (eNOS) enhancer that upregulates eNOS expression, induces NO production, and may ameliorate portal hypertension.

MK-0533 is a novel PPARγ partial agonist for the prevention of vascular endothelial dysfunction (VED) and VED-related cardiovascular disease.

NoxA1ds acetate is a potent and selective NADPH oxidase 1 (NOX1) inhibitor (IC50 : 20 nM). Exhibits selectivity for NOX1 over NOX2, NOX4, NOX5 and xanthine oxidase. Inhibits NOX1-derived O2- production in HT-29 human colon cancer cells. Attenuates VEGF-induced human pulmonary artery endothelial cell migration under hypoxic conditions in vitro.

Elsibucol (AGI 1096) is a VCAM1 inhibitor for the study of organ transplant rejection.Elsibucol is a metabolically stable propanol derivative with antioxidant, anti-inflammatory and anti-proliferative properties. It lowers blood cholesterol levels and reduces oxidative stress and inflammatory responses in injured arteries, thereby inhibiting atherosclerosis and protecting endothelial healing after arterial injury.

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).

Naphazoline (Naphcon-a) is a sympathomimetic compound with marked alpha adrenergic activity. Naphazoline can be used as a vasoconstrictor with a rapid action in reducing swelling when applied to mucous membrane.

LCB 03-0110 (3-(2-(3-(Morpholinomethyl)phenyl)thieno[3,2-b]pyridin-7-ylamino)phenol) is a potent inhibitor of discoidin domain receptor family tyrosine kinases and strongly inhibits several tyrosine kinases, including the c-Src family, spleen tyrosine kinase, Bruton's tyrosine kinase, and vascular endothelial growth factor receptor 2, which are important for immune cell signaling and inflammatory reactions.

AP23846 is a novel and potent Src family kinase inhibitor that reduces vascular endothelial growth factor and interleukin-8 expression and abrogates downstream angiogenic processes in human solid tumor cell lines.

TB500 acetate(885340-08-9 free base) (Frag17-23 Acetate) is a synthetic version of an active region of thymosin β4. It promote endothelial cell differentiation, angiogenesis in dermal tissues, keratinocyte migration, collagen deposition and decrease inflammation.

LXW7 is an octamer disulfide cyclic peptide and αvβ3 integrin ligand, acts as a potent and specific endothelial progenitor cells (EPCs) and endothelial cells (ECs) targeting ligand. LXW7 is a disulfide cyclic octa-peptide (cGRGDdvc) containing unnatural amino acids flanking both sides of the main functional motif.

NM-3 is an orally available anti-angiogenic inhibitor with anti-tumour activity.NM-3 is used as a radiation modulator in vitro and in vivo.NM-3 inhibits vascular endothelial growth factor (VEGF), thereby inhibiting the proliferation of endothelial cells. This inhibits the proliferation of endothelial cells. NM-3 is associated with a mechanism of apoptosis induction by reactive oxygen species.

C-Type Natriuretic Peptide (CNP) (1-22), human acetate is an agonist of natriuretic peptide receptor B (NPR-B), an endothelial-derived relaxant and growth inhibitory factor. C-Type Natriuretic Peptide (CNP) (1-22), human acetate inhibits cAMP synthesis stimulated by histamine and 5-HT or directly by Forskolin.

(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.

Thiolutin (Acetopyrrothin) is an inhibitor of endothelial cell adhesion and produced by Streptomyces. Thiolutin shows antibiotic and anti-angiogenic properties. Thiolutin induces the phosphorylation of Hsp27 rapidly.

Giripladib (PLA695)(PLX-695) is a cPLA2-specific inhibitor that inhibits the radiation-induced increase of phosphorylated ERK and phosphorylated Akt in endothelial cells.

T-1840383 is an inhibitor of VEGF-induced VEGFR-2 phosphorylation and HGF-induced c-Met phosphorylation in vascular endothelial cells and cancer epithelial cells.

nor-NOHA acetate (Nω-Hydroxy-nor-L-arginine acetate) is a reversible inhibitor of arginase, with anti-leukemic activity, effective in endothelial dysfunction, immunosuppression, and metabolism.

Ombrabulin hydrochloride is a synthetic, selective CA-4 phosphate ester or derivative of Ombrabulin to disrupt the tubulin cytoskeleton of endothelial cells and has antivascular effects. Ombrabulin is a tubulin polymerizing inhibitor, a member of the combretastatin A-4 compound class, which is a water-soluble tubulin depolymerizing tumor vascularizing compound.

VEGFR-3-IN-1 is a novel potent and selective VEGFR3 inhibitor with an IC50 of 110.4 nM.VEGFR-3-IN-1 possesses antitumor activity, inactivates the VEGFR3 signaling pathway, and inhibits the proliferation and migration of VEGF-C-induced human dermal lymphatic endothelial cells (HDLEC), MDA-MB-231 and MDA-MB-436 cells. MB-436 cells and inhibited the proliferation and migration of human dermal lymphatic endothelial cells (HDLEC), MDA-MB-231 and MDA-MB-436 cells.

INCA-6 (Triptycene-1,4-quinone) is a cell-permeable NFAT inhibitor. INCA-6 inhibits of CN-NFAT signaling by targeting of NFAT(P) substrate to the calcineurin (CN) phosphatase site.

4SC-203 is a multikinase inhibitor with potential antineoplastic activity. 4SC-203 selectively inhibits FMS-related tyrosine kinase 3 (FLT3/STK1), FLT3 mutated forms, and vascular endothelial growth factor receptors (VEGFRs).

TG 100572 Hydrochloride is a inhibitor of multi-targeted kinase which inhibits receptor tyrosine kinases and Src kinases(IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively).

ZM323881 hydrochloride (ZM 323881 HCl) is a potent and selective VEGFR2 inhibitor.

Norepinephrine (Levophed) can stimulate apoptosis in adult rat ventricular myocytes by activation of the β-adrenergic pathway. It can up-regulate the expression of vascular endothelial growth factor, matrix metalloproteinase (MMP)-2, and MMP-9 in nasopharyngeal carcinoma tumour cells.

Desmopressin acetate (16679-58-6 free base) (DDAVP) is the synthetic analog of the antidiuretic hormone arginine vasopressin. Vasopressin Receptor The antidiuretic properties of desmopressin have led to its use in polyuric conditions including primary nocturnal enuresis, nocturia, and diabetes insipidus. Desmopressin acetate (16679-58-6 free base) works by limiting the amount of water that is eliminated in the urine. Desmopressin acetate (16679-58-6 free base) binds to V2 receptors in renal collecting ducts, increasing water reabsorption. It also stimulates the release of von Willebrand factor from endothelial cells by acting on the V2 receptor.

Axitinib (AG-013736) is an orally bioavailable tyrosine kinase inhibitor with IC50s of 0.1, 0.2, 0.1-0.3, 1.7, 1.6 nM for VEGFR1, VEGFR2, VEGFR3, c-kit, and PDGFRβ, respectively.

Terrestrosin D can induce apoptotic cell death and inhibit angiogenesis in xenograft tumor cells, cell cycle arrest and induction of apoptosis in cancer cells and endothelial cells might be plausible mechanisms of actions for the observed antitumor and an

(Z)-Guggulsterone inhibits the growth of human prostate cancer cells by causing apoptosis. Z-guggulsterone inhibits angiogenesis by suppressing the VEGF–VEGF-R2–Akt signaling axis.

Vandetanib (ZD6474) is a potent inhibitor of VEGFR2 (IC50: 40 nM). It also inhibits VEGFR3 and EGFR.

Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that inhibits VEGFR2 and PDGFRβ (IC50=80/2 nM). Sunitinib has antitumor activity and can be used for the treatment of kidney cancer and gastrointestinal tumors.

Semaxinib (SU5416) is a potent and selective VEGFR2 inhibitor (IC50: 1.23 μM), 20-fold more selective for VEGFR than PDGFRβ, lack of activity against InsR, EGFR, and FGFR. Semaxanib reversibly inhibits ATP binding to the tyrosine kinase domain of vascular endothelial growth factor receptor 2 (VEGFR2), which may inhibit VEGF-stimulated endothelial cell migration and proliferation and reduce the tumor microvasculature.

Calycosin (Cyclosin) acts as a selective estrogen receptor modulator. Calycosin induces apoptosis in human ovarian cancer SKOV3 cells by activating caspases and Bcl-2 family proteins. Calycosin suppresses breast cancer cell growth via ERβ-dependent regulation of IGF-1R, p38 MAPK and PI3K/Akt pathways. Calycosin has antineoplastic effects against osteosarcoma through inducing apoptosis showing in vitro and in vivo investigations. Calycosin was shown to induce angiogenesis in human umbilical vein endothelial cell cultures (HUVEC) in vitro. Calycosin may be an effective skin-lightening agent that regulates the expression of melanogenic enzymes. Calycosin exhibited tyrosinase inhibitory activity with an IC(50) value of 38.4 microM.