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Tirofiban hydrochloride monohydrate (MK-383 Hydrochloride) is a potent non-peptide, glycoprotein IIb IIIa (integrins alphaIIbbetaIII) antagonist.

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

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.

TASP 0277308 is a potent and selective sphingosine 1-phosphate 1 (S1P1) receptor antagonist (IC50 = 7.8 nM). TASP 0277308 inhibits S1P-induced chemotaxis (IC50 = 1.1-1.6 nM), HUVEC cell proliferation (IC50 = 3-3.6 nM) and suppresses angiogenesisin vivo. TASP 0277308 also blocks VEGF-induced tube-formation of HUVECsin vitroand reverses or impairs the development of arthritis or mechano-allodynia.

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.

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

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

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.

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

Damascenone is a mixture of E- and Z-isomer damascenones, characteristic compounds with anti-inflammatory properties derived from Epipremnum pinnatum.

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

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

22-(4′-py)-JA, a semisynthetic derivative of junamycin A isolated from the Thai blue sponge (Xestospongia sp.), exhibits antimetastatic properties by inhibiting the AKT/mTOR/p70S6K signaling pathway. It also impedes tumor cell invasion and angiogenesis in human umbilical vein endothelial cells (HUVEC), while suppressing the expression of metalloproteinases (MMP-2 and MMP-9), hypoxia-inducible factor 1α (HIF-1α), and vascular endothelial growth factor (VEGF). Its potent anticancer activity is particularly noted against non-small cell lung cancer (NSCLC) [1].

Nrf2 activator-9 (compound D-36) is an agent that mitigates oxidative stress by inhibiting the apoptosis of HUVEC cells induced by oxidized low-density lipoprotein (oxLDL) and high glucose (HG), also protecting vascular endothelial cells (VEC) from oxLDL and HG-induced injury, offering potential therapeutic benefits for atherosclerosis prevention and treatment [1].

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.

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

Bruceine B, a potent inhibitor of leukocyte-endothelial cell adhesion, may have anti-inflammatory activity, it can inhibit neutrophil adhesion to lipopolysaccharide-stimulated HUVEC and T cell adhesion to TNF-stimulated HUVEC.

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).

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

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.

BMP-22 is an inhibitor of autotaxin (IC50 = 170 nM). It is selective for autotaxin over the phosphodiesterases NPP6 and NPP7 at 10 μM. BMP-22 (0.1-1,000 nM) inhibits autotaxin-mediated production of lysophosphatidic acid (LPA) from lysophosphatidylcholine in vitro in a concentration-dependent manner. It inhibits LPC-dependent MM1 cell invasion of a human umbilical vein endothelial cell (HUVEC) monolayer. BMP-22 (0.5 mg/kg per day) decreases the number of lung metastatic foci in a B16/F10 syngeneic mouse melanoma model of lung metastasis.

Nephthenol shows antiproliferative activity against the cell lines HUVEC and K-562 and for cytotoxicity against the cell line HeLa.

Potent, high affinity apelin receptor agonist (IC50 = 0.27 nM; Kd = 0.51 nM). Exhibits no binding GPR15 and GPR25. Activates the PI3K/AKT pathway and promotes self-renewal of hESCs via cell-cycle progression and protein translation. Also potentiates the T

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.

VEGFR-2-IN-39 (PROTAC-5), a PROTAC that targets VEGFR-2 with an IC 50 of 208.6 nM, demonstrates low toxicity. It effectively inhibits the proliferation of EA.hy926, a type of HUVEC, in a concentration-dependent manner, achieving an IC 50 value of 38.65 µM [1].

Compound 3b, an antiangiogenic agent, inhibits Akt phosphorylation in both HFF and HUVEC cells and is utilized in cancer research [1].

Tubulin Inhibitor 31 is a potent compound with an inhibitory concentration (IC 50) of 4 µM, demonstrating significant anti-proliferative activity and the ability to inhibit HUVEC migration.

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].

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

Coronarin, A, B, C, and D are cytotoxic prinicples from the rhizomes of Hedychium coronarium, Zingiberaceae. Coronarin A exhibits good growth inhibition activities on HUVEC proliferation, it effectively suppresses the growth factor induced tube formation

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].

N-Arachidonoyl-L-serine (ARA-S), a recently isolated endocannabinoid with a distinct activity profile that diverges from typical endocannabinoids, does not interact with central cannabinoid (CB1), peripheral cannabinoid (CB2) receptors, or vanilloid receptor 1 (VR1). Unlike other compounds, ARA-S (5 mg/kg) counteracts the lowering of blood pressure induced by a 10 mg/kg intravenous bolus of abnormal cannabidiol (Abn-CBD) in anesthetized rat models. Additionally, akin to Abn-CBD, ARA-S induces relaxation in isolated rat mesenteric arteries and abdominal aorta and promotes phosphorylation of Akt and mitogen-activated protein kinase (MAPK) in human umbilical vein endothelial cells (HUVEC). The mechanisms through which ARA-S and Abn-CBD exert their effects on vascular systems show variations and merit deeper investigation.

DYB-03 is an orally active HIF-1α EZH2 inhibitor that inhibits migration, invasion, and angiogenesis of lung cancer cells and HUVECs in vitro and in vivo, and induces apoptosis in 2-ME2- and GSK126-resistant A549 and H460 cells [1].

VEGFR-2-IN-37 (compound 12), a VEGFR-2 inhibitor, demonstrates an inhibition rate of approximately 56.9 μM at 200 μM concentration and is identified as a potential inhibitor of human umbilical vein endothelial cell (HUVEC) proliferation [1].

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.

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.

1. Sauchinone is a useful adjunctive treatment for bacterial infection. 2. Sauchinone, an active lignan found in Saururus chinensis, to regulate the activation of HSCs, to prevent liver fibrosis, and to inhibit oxidative stress in vivo and in vitro. 3. Sa

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

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.

Taspine shows antitumor activity by modulating the EGFR signaling pathway of Erk1/2 and Akt in vitro and in vivo, it can inhibit growth and induce apoptosis of HUVEC in a dose-dependent manner, it has shown meaningful angiogenesis activity. Taspine exhibi

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.

SARS-CoV-2 Mpro-IN-22 (compound 4) is an effective inhibitor of the SARS-CoV-2 main protease (Mpro), with an IC50 of 1.2 µg mL. This hydrolyzable tannin exhibits no significant cytotoxic activity in A549 and HUVEC cell lines.

Fibulostatin 6.2, an anti-angiogenic peptide, inhibits the migration of human umbilical vein endothelial cells in vitro [1].

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.

Shizukaol B exerts anti-inflammatory effects in LPS-activated microglia partly by modulating JNK-AP-1 signaling pathway; it also shows significant anti-neuroinflammatory effects by inhibiting nitric-oxide (NO) production in lipopolysaccharide (LPS)-stimul

Cycloshizukaol A prevents monocyte adhesion to HUVEC through the inhibition of cell adhesion molecules expression stimulated by TNF-alpha, it inhibits PMA-induced homotypic aggregation of HL-60 cells without cytotoxicity with MIC values of 0.9 microM.

1. Brazilin (Braziletto) exhibits anti-hepatotoxic, antiplatelet effects. 2. Brazilin has cancer preventive effect, may inhibit T24 cell growth and trigger cell death through a c-Fos-mediated and tumor cell specific signaling pathway. 3. Brazilin has anti-inflammatory property, can suppress mastitis and high glucose-induced vascular inflammatory process related with the inhibition of oxidative stress, CAMs expression, and NF-κB activation in HUVEC; may be useful to treat chronic inflammatory disorders including rheumatoid arthritis.