HUVEC cells

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

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.

Allopurinol Sodium is a xanthine oxidase inhibitor with an IC50 of 7.82±0.12 μM.

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.

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

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.

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.

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.

D-myo-Inositol-1,3,4,5,6-pentaphosphate (ammonium salt) [Ins(1,3,4,5,6)P5 (ammonium salt)] is an isomer of inositol phosphate that functions as a small, soluble second messenger in cellular signaling. It can bind to the PH domain of Grp1 with a dissociation constant (Kd) of 590 nM. This compound inhibits the phosphorylation and kinase activity of Akt/PKB, leading to apoptosis in ovarian, lung, and breast cancer cells. Additionally, it exhibits anti-angiogenic activity in vitro, blocking capillary formation by HUVECs, and demonstrates antitumor effects in cancer xenograft models in nude mice.

PROTACBcl-xL degrader-4 (Compound 2-38-III) is a Bcl-xL PROTAC degrader with significant antitumor activity against HepG2 and HUVEC cells. It induces apoptosis by reducing mitochondrial membrane potential and activating the MAPK signaling pathway. PROTACBcl-xL degrader-4 markedly inhibits tumor growth in xenograft mouse models.

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.

Salinazid (Salicylaldehyde isonicotinoyl hydrazone) is a potent Cu(II) ionophore which preferentially kills HepG2 cells over HUVEC cells, and is superior to clioquinol.

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.

18-Deoxyherboxidiene (RQN-18690A) is a potent inhibitor of angiogenesis that selectively acts on SF3b, a subcomplex of the U2 small nuclear ribonucleoprotein (snRNP) in the spliceosome. It inhibits migration and tube formation in human umbilical vein endothelial cells (HUVEC) without significant cytotoxicity and has potential for cancer research.

AT-533 is a potent inhibitor of Hsp90 and HSV. AT-533 blocks the HIF-1α/VEGF/VEGFR-2 signaling pathway, leading to suppress tumor growth and angiogenesis. AT-533 also inhibits the activation of the downstream pathways, including Erk1/2, FAK, Akt/mTOR/p70S6K,. AT-533 inhibits the cell migration, invasion, and the tube formation of human umbilical vein endothelial cells (HUVECs).

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.

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].

ELA-32(human) TFA is a potent apelin receptor agonist with high affinity, demonstrating an IC50 of 0.27 nM and a Kd of 0.51 nM. This compound does not bind to GPR15 or GPR25. It activates the PI3K/AKT signaling pathway, facilitating self-renewal of human embryonic stem cells (hESCs) through cell-cycle progression and protein synthesis. Additionally, ELA-32(human) TFA enhances the TGFβ pathway, predisposing hESCs towards an endoderm lineage, and promotes angiogenesis in HUVEC cells.

3-Hydroxyxanthone (3-Hydroxy-xanthen-9-one), a xanthone derivative, inhibits NADPH-catalyzed lipid peroxidation in human umbilical vein endothelial cells (HUVECs) and suppresses TNF-alpha-induced ICAM-1 expression [1].