angiogenic

SPHINX31 is a potent inhibitor of serine/arginine-rich protein kinase 1 (SRPK1; IC50: 5.9 nM).

Suramin Sodium Salt (BAY-205) is a sodium salt form of suramin, a polysulphonated naphthylurea with potential antineoplastic activity. Suramin blocks the binding of various growth factors, including insulin-like growth factor I (IGF-I), epidermal growth factor (EGF), platelet-derived growth factor (PDGF), and tumor growth factor-beta (TGF-beta), to their receptors, thereby inhibiting endothelial cell proliferation and migration. This agent also inhibits vascular endothelial growth factor (VEGF)- and basic fibroblast growth factor (bFGF)-induced angiogenesis; retroviral reverse transcriptase; uncoupling of G-proteins from receptors; topoisomerases; cellular folate transport; and steroidogenesis.

DMOG (Dimethyloxalylglycine), an antagonist of the α-ketoglutarate cofactor, is an inhibitor for HIF prolyl hydroxylase.

beta-Escin is a natural mixture of triterpenoid saponins isolated from horse chestnut (Aesculus hippocastanum) seeds, can be used as a vasoprotective anti-inflammatory, anti-edematous and anti-nociceptive agent.

1. Sinapine, an alkaloid from seeds of the cruciferous species, can be used as an effective natural compound for chemo-resistance. 2. Sinapine has antioxidant and radio-protective activities.

Sinapine Thiocyanate, is a derivative of Sinapine (S486605), an alkaloidal amine found in black mustard seeds. It is the choline ester of Sinapic Acid (S486800). It is also a phenolic-chloine conjugates, acting as anti-oxidants and acetylcholinesterase inhibitors, that can be used for the treatment of Alzheimer's disease (AD).

Methylstat is a methyl ester prodrug of a Jumonji C domain-containing histone demethylase (JMJD) inhibitor that has favorable cell permeability. The free acid of methylstat inhibits JMJD2A, JMJD2C, JMJD2E, PHF8, and JMJD3 with IC50 values of approximately 4.3, 3.4, 5.9, 10, and 43 μM, respectively, in an in vitro assay. Methylstat inhibits growth of the JMJD2C-sensitive esophageal cancer cell line KYSE150 with a GI50 of 5.1 μM, whereas the free acid of methylstat did not inhibit cell growth up to 100 μM. Methylstat induces histone hypermethylation at multiple sites in a concentration-dependent manner (EC50 for H3K4me3 and H3K9me3 = 10.3 and 8.6 μM in KYSE150 cells and 6.7 ad 6.3 μM in MCF-7 cells, respectively).

Fasentin (N-[4-chloro-3-(trifluoromethyl)phenyl]-3-oxobutanamide) is an inhibitor of GluT1.

Formononetin (Flavosil) is an O-methylated isoflavone and a phytoestrogen from the root of Astragalus membranaceus.

Notoginsenoside R1 (Sanchinoside R1) has been shown to exhibit antioxidant, antiapoptotic, anti-inflammatory, and immune-stimulatory properties.

PTP inhibitor 1 is an inhibitor of cell-permeable protein tyrosine phosphatase (PTP) that covalently binds the catalytic domain of the Src homology region 2 domain-containing phosphatase (SHP-1(ΔSH2)),with Ki of128 μM.

Specnuezhenide (Nuezhenide) is isolated from the fruit of Ligustrum lucidum. It inhibits NF-κB and wnt/β-catenin signaling, thereby suppressing IL-1β-induced chondrocyte inflammation. It exerts anti-inflammatory effects in a rat model of osteoarthritis (OA).

Antiangiogenic agent 2 (compound 3b) is a potent thymidine phosphorylase inhibitor (IC50: 39.71 μM) with demonstrated anti-angiogenic effects.

Antiangiogenic Agent 5 (Compound 17) exhibits potent anti-angiogenic activity by inhibiting SRPK 1 with an IC50 of 1.3 nM [1].

Antiangiogenic agent 6 (Pt-1) effectively inhibits angiogenesis and induces necroptosis in tumor cells.

Antiangiogenic agent 7 (Compound 1) induces apoptosis, elevates Reactive Oxygen Species (Reactive Oxygen Species), and inhibits the intracellular enzyme thioredoxin reductase. It exhibits anticancer activity with IC50 values ranging from 0.08 to 3.5 μM against cervical cancer cells (HeLa), prostate cancer cells (PC-3), and non-small cell lung cancer cells (A549). Additionally, Antiangiogenic agent 7 suppresses tumor growth in a mouse xenograft model.

Antiangiogenic agent 8 (Compound 3m) functions as both an antibacterial agent and an antiangiogenic compound. It shows minimum inhibitory concentrations (MIC) of 16, 8, 4, 16, and 8 μg/mL against E. coli, P. aeruginosa, B. subtilis, S. aureus, and C. glabrata, respectively, with minimum bactericidal concentrations (MBC) ranging from 32 to 64 μg/mL. This compound holds potential for applications in infection control and cardiovascular disease research.

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.

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

Amifostine (Ethyol) anhydrous is a cytoprotective agent, acts as a free radical scavenging activity.

AKB-6899 is an inhibitor of prolyl hydroxylase domain 3 (PHD3) and increases the soluble form of the VEGF receptor (sVEGFR-1) production from GM-CSF-treated macrophages. AKB-6899 leads to stabilization of HIF-2α which induces sVEGFR-1 production from tumor-associated macrophages and decreases tumor growth.

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

Itraconazole (R51211) is a triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes necessary for ERGOSTEROL synthesis.

Mycophenolic acid (Mycophenolate) is an inosine monophosphate dehydrogenase(IMPDH) inhibitor with anti-proliferative activity.