anti-angiogenic

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.

Specnuezhenide (Nuezhenide) significantly protects human neuroblastoma SH-SY5Y cells from 6-hydroxydopamine-induced neurotoxicity.Nuezhenide is the main inhibitory compound of fruits, it shows a clear inhibitory effect to the seeds of wheat and Chinese cabbage.

Matairesinol has radical and superoxide scavenging activities,; it also has anti-angiogenic activity by suppressing mROS signaling , can decrease hypoxia-inducible factor-1α± in hypoxic HeLa cells.

Benzyl isothiocyanate (Benzoylthiocarbimide) (BITC) is an isothiocyanate originally found in cruciferous vegetables. It shows immunomodulatory, anti-parasitic, antibiotic, antioxidative, anti-atherosclerotic, anti-angiogenic, anti-metastatic, anticancer chemotherapeutic, and chemopreventive activities.

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

4-Hydroxybenzyl alcohol (P-Methylolphenol) exhibits beneficial effects in cerebral ischemic injury, has neuroprotective effect through upregulation of Nrf2, Prdx6, and PDI expression via the PI3K/Akt pathway. 4-Hydroxybenzyl alcohol inhibit the development of new blood vessels by targeting multiple mechanisms of the angiogenic process, may as a promising candidate for the establishment of anti-angiogenic treatment strategies in cancer therapy.

Oltipraz (RP 35972) is a synthetic dithiolethione with potential chemopreventive and anti-angiogenic properties. Oltipraz induces phase II detoxification enzymes, such as glutathione S transferase (GST) and NAD(P)H: quinone oxidoreductase 1 (NQO1). The induction of detoxification enzymes enhances the detoxification of certain cancer-causing agents, thereby enhancing their elimination and preventing carcinogen-induced DNA damages. Although the exact mechanism through which the anti-angiogenesis effect remains to be fully elucidated, oltipraz maybe able to modulate the expression of a number of angiogenic factors, thereby blocking the sustained and focal neovascularization in multiple tumor cell types.

Rofecoxib (MK 966) binds to and inhibits the enzyme cyclooxygenase-2 (COX-2), resulting in an inhibition of the conversion of arachidonic acid to prostaglandins. Rofecoxib is a synthetic, nonsteroidal derivative of phenyl-furanone with anti-inflammatory, antipyretic and analgesic properties and potential antineoplastic properties. COX-related metabolic pathways may represent key regulators of cell proliferation and neo-angiogenesis. Some epithelial tumor cell types overexpress pro-angiogenic COX-2.

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.

Purpurin (Verantin) was a reversible and competitive inhibitor of MAO-A with a Ki value of 0.422μM. it exhibits anti-angiogenic, antifungal, antibiotic, and antioxidative activities.

Bromelain is an anti-inflammatory drug derived from pineapple stem. It acts through down-regulation of plasma kininogen, degradation of advanced glycation end-product receptors, inhibition of Prostaglandin E2 expression, and regulation of angiogenic bioma

Pomalidomide (CC-4047) is an anti-angiogenic and immunomodulatory agent. Pomalidomide is a ligand for the ubiquitin E3 ligase cereblon (CRBN) and is commonly used in the synthesis of PROTAC products.

Vanillyl Alcohol (3-Methoxy-4-hydroxybenzyl alcohol) possesses anti-angiogenic, anticonvulsive, anti-inflammatory, anti-oxidant, neuroprotective, and anti-nociceptive activities. Vanillyl alcohol can effectively inhibit the cytotoxicity and improved cell viability in 1-methyl-4-phenylpyridinium (MPP+)-induced MN9D dopaminergic cells, it also can attenuate the elevation of reactive oxygen species (ROS) levels, decrease in the Bax/Bcl-2 ratio and poly (ADP-ribose) polymerase proteolysis.

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

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.

Syringic acid (3,5-dimethoxy-4-hydroxy Benzoic Acid) (SYRA) is a potential antioxidant used in traditional Chinese medicine and is an emerging nutraceutical. It has potential anti-angiogenic, anti-glycating, anti-hyperglycaemic, neuroprotective, and memory-enhancing properties.

Thalidomide (Thalomid) is a synthetic derivative of glutamic acid (alpha-phthalimido-glutarimide) with teratogenic, immunomodulatory, anti-inflammatory and anti-angiogenic properties.

TIE-2 VEGFR-2 kinase-IN-5 (TIE-2 and VEGFR-2 tyrosine kinase receptor inhibitor) is a potent agent with anti-angiogenic activity, commonly used in biomedical research focused on angiogenesis.

LCKLSL acetate is a competitive annexin A2 (AnxA2) inhibitor. LCKLSL acetate potently inhibits the binding of tissue plasminogen activator (tPA) to AnxA2 and the generation of plasmin. LCKLSL acetate has anti-angiogenic roles.

Tafetinib (SIM-010603) is a novel potent and orally available tyrosine kinase inhibitor with anti-angiogenic and anti-tumour activity.

Givinostat hydrochloride (ITF2357 hydrochloride) is an inhibitor of HDAC with IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively. Givinostat hydrochloride exhibits anti-inflammatory, anti-angiogenic, and antineoplastic activities.

SM27 is a fibroblast growth factor 2 (FGF2) inhibitor with anti-angiogenic activity and can be used to study tumours.

BPHA (MMP-2 MMP-9 Inhibitor II) is a potent, selective and orally active inhibitor of MMP-2, MMP-9 and MMP-14 with IC50s of 12 nM, 16 nM and 17 nM, respectively.BPHA does not inhibit MMP-1, -3 and -7 (IC50s of 974, >1000 and 795 nM, respectively).BPHA has anti-angiogenic and BPHA has anti-angiogenic and anti-tumor activities.

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.

A-176120 is a potent farnesyl pyrophosphate (FPP) analogues, it selectively inhibits farnesyltransferase. It has anti-angiogenic potential and may reduce H-ras NIH3T3 tumour growth.

Thiolutin (Acetopyrrothin) is an inhibitor of endothelial cell adhesion and produced by Streptomyces. Thiolutin shows antibiotic and anti-angiogenic properties. Thiolutin induces the phosphorylation of Hsp27 rapidly.

(S)-Thalidomide ((S)-(-)-Thalidomide) is the S-isomer of Thalidomide with immunomodulatory, anti-inflammatory, anticancer, anti-angiogenic, and pro-apoptotic activities, used in studying leprosy erythema nodosum and myeloma.

AZ10606120 dihydrochloride is a selectable, potent, high-affinity receptor antagonist with K D values of 1.4 and 19 nM at human and rat P2X 7 receptors, respectively. AZ10606120 dihydrochloride inhibits tumor growth and has anti-angiogenic activity. AZ 10606120 acts as a negative allosteric modulator when bound to a site coupled to the ATP binding site.

Burixafor hydrobromide (TG-0054 hydrobromide) is an orally bioavailable and potent CXCR4 antagonist with anti-angiogenic properties, potentially valuable in treating choroid neovascularization.

SU11652 is a potent cell-permeable pyrrole-indolinone compound. SU11652 acts as an ATP-competitive tyrosine kinase receptor and angiogenic inhibitor with greater selectivity for PDGFR-β (PDGFRβ, IC50 = 3 nM), Flk-1 (VEGFR2, IC50 = 27 nM), FGFR1 (IC50= 170

EG01377 2HCl is a potent, bioavailable and selective inhibitor of neuropilin-1 (NRP1) with a Kd value of 1.32 μM and an IC50 value of 609 nM for both EG01377 2HCl against NRP1-a1 and NRP1-b1.EG01377 exhibits anti-angiogenic, antimigratory and antitumor activities.

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.

Polyphyllin D induces apoptosis via the mitochondrial apoptotic pathway as evidenced by decreased Bcl-2 expression levels, disruption of MMP and increased Bax, cytochrome C, and cleaved-caspase-3 levels. Polyphyllin D has an anti-angiogenic effect. Polyphyllin D has toxicity in human RBCs as well as its underlying mechanism for the hemolysis and eryptosis/erythroptosis. Polyphyllin D has strong anticancer activity, can overcome drug resistance in R-HepG2 cells and elicit programmed cell death via mitochondrial dysfunction.

Bacopaside II is a potential anti-angiogenic agent, it can reduce endothelial cell migration and tubulogenesis and induce apoptosis.

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.

5alpha-Hydroxycostic acid possesses anti-angiogenic ability by interfering the VEGF- and Ang2-related pathways, and it may be a good drug candidate.

Piperlongumine (Piplartine) is a natural alkaloid from Piper longum L. It selectively kills cancer cells and strengthens the level of reactive oxygen species (ROS).

MYLS22 is a first-in-class and selective inhibitor of optic atrophy 1 (OPA1) . MYLS22 can target endothelial OPA1 to curtail tumor growth and inhibits angiogenesis by impinging on NFkB activity and on angiogenic gene expression. It with anti-angiogenesis and anti-cancer activity.

Deoxypodophyllotoxin shows cytotoxic , antineoplastic, antitumor, insecticidal, anti-angiogenic, vascular disrupting, insecticidal, antiviral, and anti-inflammatory activities.

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

NSC-6038 (4-chloro-N,N-dipropylbenzamide) is a benzamide-based bioactive compound with a wide range of biological activities and has been shown to possess anti-inflammatory, antioxidant and anti-angiogenic activities, and has also been shown to be effective in the treatment of a wide range of diseases such as cancer, diabetes and cardiovascular diseases.

Bavachinin (Bavachinin A)(7-O-Methylbavachin) is a natural compound isolated from the Chinese herb Fructus Psoraleae with potent anti-angiogenic activity.

Fruquintinib (HMPL-013) is an orally available, small molecule inhibitor of vascular endothelial growth factor receptors (VEGFRs), with potential anti-angiogenic and antineoplastic activities.

LY2457546 is a potent and orally bioavailable inhibitor of multiple receptor tyrosine kinases involved in angiogenic and tumorigenic signalling. LY2457546 demonstrates potent activity against targets that include VEGFR2 (KDR), PDGFRβ, FLT-3, Tie-2 and members of the Eph family of receptors. In vivo, LY2457546 inhibited VEGF-driven autophosphorylation of lung KDR in the mouse and rat in a dose and concentration dependent manner. LY2457546 was well tolerated and exhibited efficacy in a 13762 syngeneic rat mammary tumor models. Additionally, LY2457546 caused complete regression of well-established tumors in an acute myelogenous leukemia (AML) FLT3-ITD mutant xenograft tumor model. The unique spectrum of target activity, potent in vivo anti-tumor efficacy in a variety of rodent and human solid tumor models, exquisite potency against a clinically relevant model of AML, and non-clinical safety profile justify the advancement of LY2457546 into clinical testing. (source: Invest New D......

possesses anticancer, anti-invasive, anti-metastasis, anti-angiogenic and pro-apoptosis properties with high safety.Frondoside A, a natural glycoside extracted from the sea cucumber, Cucumaria frondosa,

Fruquintinib-d3 is a deuterated compound of Fruquintinib. Fruquintinib has a CAS number of 1194506-26-7. Fruquintinib is an orally available, small molecule inhibitor of vascular endothelial growth factor receptors (VEGFRs), with potential anti-angiogenic and antineoplastic activities.

TID43, a CK2 inhibitor, exhibits potent inhibition with an IC50 value of 0.3 μM. It is applicable in anti-angiogenic research [1].

Tubulin inhibitor 14 is a potent inhibitor of NQO2 (quinone oxidoreductase 2) with an IC50 of 1.0 μM, which also inhibits tubulin polymerization and the formation of endothelial cell capillary-like tubes. As a microtubule destabilizer, Tubulin inhibitor 14 has potential tumor-selective, anti-angiogenic, and vascular-destructive properties [1].

PKRA83 is a potent prokineticin (PK2) antagonist that crosses the blood-brain barrier and competes for PK2 binding to its receptors PKR1 and PKR2. PKRA83 effectively inhibits PK2 receptors and acts on PKR1 (IC50: 5.0 nM) and PKR2 (IC50: 8.2 nM). PKRA83 exhibits anti-cancer and anti-angiogenic effects.

Coenzyme Q0 (CoQ0), a potent, orally active ubiquinone compound derived from Antrodia cinnamomea, induces apoptosis and autophagy. It suppresses HER-2/AKT/mTOR signaling, enhancing apoptosis and autophagy mechanisms. Additionally, Coenzyme Q0 regulates NFκB/AP-1 activation and promotes Nrf2 stabilization, contributing to the attenuation of inflammation and redox imbalance. It also exhibits anti-angiogenic activity by downregulating MMP-9/NF-κB and upregulating HO-1 signaling.