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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

GW806742X is an inhibitor of Mixed Lineage Kinase Domain-Like protein (MLKL) which binds the MLKL pseudokinase domain (Kd: 9.3 μM) with anti-necroptosis activity. GW806742X has activity against VEGFR2.

Vulpinic Acid (Pulvinic acid methyl ester) is a lichen metabolite with anti-inflammatory, antibacteria, properties, plant growth inhibitor.

E7820 (ER68203-00) is an angiogenesis inhibitor by suppressing integrin a2 (a cell adhesion molecule expressed on endothelial cells).

Tirofiban (L700462) (MK-383) is a selective palate GPIIb/IIIa antagonist which inhibits platelet aggregation with IC50 of 9 nM.

ODM-203, a Selective Inhibitor of FGFR and VEGFR, Shows Strong Antitumor Activity, and Induces Antitumor Immunity

VEGFR-2-IN-29 is a VEGFR2 inhibitor.

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.

Allopurinol (Zyloric) is a Xanthine Oxidase Inhibitor. The mechanism of action of allopurinol is as a Xanthine Oxidase Inhibitor.

4-Nitrothalidomide is a modified form of thalidomide that inhibits the growth and proliferation of HUVEC cells and is commonly used in the synthesis of pomalidomide, which has anticancer potential.

Cediranib (AZD2171) (AZD2171) is a highly potent (IC50 < 1 nmol/L) ATP-competitive inhibitor of recombinant KDR tyrosine kinase in vitro, also inhibits Flt1/4 (IC50: 5 nM/≤3 nM), similar activity against PDGFRβ and c-Kit, selective more for VEGFR than PDGFR-α (36-fold), CSF-1R (110-fold), and Flt3 (1000-fold) in HUVEC cells.

Carebastine, the active metabolite of Ebastine, is an antagonist of the histamine H1 receptor.

Dooku1 is an analog of Yoda1 and a selective antagonist of endogenous Piezo1 channels. Dooku1 inhibits Ca2+ entry induced by 2μMYoda1 with IC50 values of 1.3μM (in HEK 293 cells) and 1.5μM (in HUVEC). Dooku1 inhibits Yoda1-induced aortic relaxation.

CLZ-8 (Mcl1-IN-8) is an orally active inhibitor of Mcl-1-PUMA (p53 up-regulated mediator of apoptosis) with radioprotective properties.CLZ-8 ameliorates radiation-induced HUVEC cell damage and reduces apoptosis counts, and inhibits radiation-induced overexpression of PUMA.

VEGFR-2-IN-57 (compound 6n) exhibits significant cytotoxicity on HUVEC cells, with an IC50 value of 28.77 nM.

Azaspirene, a novel angiogenesis inhibitor, is based on the 1-oxa-7-azaspiro[4.4]non-2-ene-4,6-dione framework. Previous studies have shown that Azaspirene effectively inhibits VEGF-induced migration of human umbilical vein endothelial cells (HUVEC), demonstrating a potentially effective dosage. Moreover, azaspirene analogs may exhibit potential antitumor effects against uterine adenocarcinoma, possibly through significant anti-angiogenic activity.

p-F-HHSiD (p-Fluorohexahydrosiladifenidol) hydrochloride is a selective M3mAChR antagonist. It is capable of inhibiting acetylcholine-mediated vasodilation in human umbilical vein endothelial cells (HUVEC).

VEGFR PDGFR-IN-1 (Compound 1) is an inhibitor of VEGFR with an IC50 of 0.4 μM. It can inhibit angiogenesis in HUVEC cells and holds promise for impeding tumor growth and metastasis.

VEGFR-2-IN-65 (Compound 07) functions as a VEGFR-2 inhibitor. It forms hydrogen bonds with Cys180 and can inhibit tube formation in HUVECs.

SDX-7539 is a selective MetAP2 inhibitor that inhibits the proliferation of HUVEC, with an IC50 of 120 μM. It has demonstrated antitumor activity in xenografted NSCLC in athymic nude mice.

Anti-MRSA agent 10 (Compound 2d) is a cephalosporin derivative with antibacterial properties. It displays minimal resistance and shows low cytotoxicity in HUVEC and HBZY-1 cells.

D-01 is a dual-target inhibitor of HIF-1α and EZH2, with IC50 values of 4.86 μM and 0.99 μM, respectively. It suppresses the expression of the H3K27me3 protein and inhibits the migration, colony formation, and invasion of A549 cells, as well as lumen formation in HUVEC. D-01 is applicable in lung cancer research.

α2AR agonist 1 (compound S6a) is a morpholinopyrimidinone that serves as an agonist for the α2-adrenergic receptor (α2AR). This compound elicits a concentration-dependent relaxation in precontracted aortic rings induced by phenylephrine (pEC50=6.81). Additionally, α2AR agonist 1 elevates levels of NOx and NO in HUVEC.

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.