endothelial cells

Yoda 1 is an agonist of the Piezo1 channel that agonizes human- and mouse-derived Piezo1 (EC50=17.1 26.6 μM). Yoda 1 is also an inhibitor of glycine transporter protein 2 (GlyT2).

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

Dimethyl sulfoxide (DMSO) is a commonly used solvent to dissolve polar and non-polar compounds. Dimethyl sulfoxide has been widely used for masterbatch preparation of compounds in biological experiments. Dimethyl sulfoxide has bacteriostatic activity.

Lipopolysaccharides (LPS) derived from Escherichia coli 055:B5, are a unique component of the cell wall of Gram-negative bacteria. They are composed of three regions: lipid A, oligosaccharide core, and O-specific polysaccharide (O-antigen). Lipopolysaccharides help maintain the integrity of the cell outer membrane and protect bacteria from damage by bile salts and lipid antibiotics. Lipopolysaccharides are highly immunogenic antigens that can enhance immune responses and can be used to construct inflammatory models.

Ranirestat (AS-3201) is an orally active and potent aldose reductase (AR) inhibitor with neuroprotective properties that ameliorates peripheral nerve dysfunction in rats with advanced diabetic polyneuropathy.Ranirestat inhibits the inflammatory response of high glucose-exposed endothelial cells and may be useful for the study of diabetic sensory-motor polyneuropathy.

SB 216641 hydrochloride (SB-216641A) is a selective 5-HT1B D receptor antagonist with anxiolytic properties that antagonizes the vasoconstrictor response mediated by sumatriptan. 10-O-Methylprotosapphosporin is an HbF inducer that can be used in the study of metabolic disorders and diabetes.

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

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.

VEGFR-3-IN-1 is a novel, potent, and selective VEGFR3 inhibitor with an IC50 of 110.4 nM. It exhibits 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.

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.

Azilsartan (TAK-536) is an Angiotensin 2 Receptor Blocker that acts as an Angiotensin 2 Type 1 Receptor Antagonist, leading to a physiologic effect of decreased blood pressure.

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.

Addition of the Rhamnose (6-Deoxy-L-mannose)-rich polysaccharide, RROP-1, to normal human dermal fibroblasts (NHDFs) and human endothelial cells produced a dose-dependent stimulation of the calcium-signaling pathway, inducing fast and transient increases in Ca2 influx and intracellular free Ca2 level.

Calcium dobesilate(CaD) has angioprotective properties and protects endothelial cells partly by ameliorating HG induced inflammation.

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.

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.

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.

ATN-224 (Bis(choline)tetrathiomolybdate) inhibits SOD1 activity in endothelial cells, an effect that is dose dependent with an IC50 of 17.5±3.7 nM. ATN-224 is an oral Cu2+ Zn2+-superoxide dismutase 1 (SOD1) inhibitor.

Isorhamnetin (3-methylquercetin) is the methylated metabolite of quercetin. Quercetin is an important dietary flavonoid with in vitro antioxidant activity. Isorhamnetin prevents endothelial cell injuries from oxidized LDL via inhibition of lectin-like ox-LDL receptor-1 upregulation, interference of ox-LDL-mediated intracellular signaling pathway (p38MAPK activation, NF-kappaB nuclear translocation, eNOS expression) and the antioxidant activity of isorhamnetin. Isorhamnetin prevents endothelial dysfunction, superoxide production, and overexpression of p47phox induced by angiotensin II. Isorhamnetin appears to be a potent drug against esophageal cancer due to it's in vitro potential to not only inhibit proliferation but also induce apoptosis of Eca-109 cells.

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

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.

Morroniside would act as a regulator of hepatic inflammatory reactions and lipid metabolism in db db mice. It exhibits protective effects against diabetic renal damage and human umbilical vein endothelial cells, by inhibiting hyperglycemia and oxidative s

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

Erianin is a nature product extracted from Dendrobium chrysotoxum, has notable antitumour activity , can cause extensive tumour necrosis, growth delay. Erianin has antiangiogenic action by inhibiting endothelial metabolism in a JNK SAPK-dependent manner a