Angiogenesis Inhibitors

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A1477 Angiostatin K1-3 human ≥90% (SDS-PAGE), recombinant, expressed in Pichia pastoris (without N-linked glycosylation) A proteolytic fragment of plasminogen containing the first three kringle structures. A specific inhibitor of endothelial cell growth and angiogenesis. More active relative to kringles 1-4. Studies with recombinant angiostatin show that the tumor inhibitory activity resides in a fragment of K1-3.
D193 DL-α-Difluoromethylornithine hydrochloride hydrate solid, ≥97% (NMR) Difluoromethylornithine (Eflornithine) inhibits polyamine biosynthesis by the selective, irreversible inhibition of ornithine decarboxylase (ODC). A chemoprotective agent that blocks angiogenesis.
SRP3031 Endostatin human recombinant, expressed in E. coli, ≥98% (SDS-PAGE), ≥98% (HPLC), cell culture tested Endostatin inhibits the proliferation and migration of endothelial cells. It blocks apoptosis of cells and G1 to S phase transition in the cell cycle. It inhibits angiogenesis by blocking the pro-angiogenic activities of VEGF and FGF-basic. Mutations in this gene lead to Knobloch Syndrome (KS), a rare autosomal recessive disorder.
E8279 Endostatin murine recombinant, expressed in Pichia pastoris, ≥95% (SDS-PAGE) Endostatin is a potent inhibitor of angiogenesis and tumor growth in vitro and in vivo; specifcally inhibits endothelial cell proliferation. Recombinant Endosatin expressed in yeast causes G1 arrest of endothelial cells, and endostatin treatment results in apoptosis of HUVE and HMVE cells.
Endostatin is an endogenous inhibitor of angiogenesis, and in vitro inhibits the migration of endothelial cells. Collagen XVIII is cleaved to form endostatin, and this system might act as the negative control of angiogenesis. During wound healing, endostatin decreases the amount of blood vessels that function normally, along with the matrix density in granulation tissue. However, it does not have an overall impact on wound healing. As it is a potent inhibitor of angiogenesis, it also strongly suppresses tumor growth.
F6771 Fumagillin from Aspergillus fumigatus ≥90%, powder Methionine aminopeptidase-2 (MetAP-2) inhibitor; inhibits endothelial cell proliferation and angiogenesis.
G6649 Genistein synthetic, ≥98% (HPLC), powder Genistein is essential for plant-microbe interaction. It acts as a natural chemoprotectant and helps in preventing tumor progression and heart disorders. Genistein functionally shares estrogen′s action. It is useful in evaluating nutraceuticals and functional foods. Genistein exhibits antimicrobial action and can serve as a phytoalexin and phytoanticipin.
Inhibitor of tyrosine protein kinase; competitive inhibitor of ATP in other protein kinase reactions. Antiangiogenic agent, down-regulates the transcription of genes involved in controlling angiogenesis.
G6776 Genistein from Glycine max (soybean), ~98% (HPLC) Inhibitor of tyrosine protein kinase; competitive inhibitor of ATP in other protein kinase reactions. Antiangiogenic agent, down-regulates the transcription of genes involved in controlling angiogenesis.
M6383 2-Methoxyestradiol powder 2-Methoxyestradiol (2-ME) is a potent inhibitor of endothelial cell proliferation and angiogenesis. A major estradiol metabolite, it has little affinity for classical estrogen receptors.
M9511 Minocycline hydrochloride powder Minocycline is a broad spectrum antibiotic with bacteriostatic function. Minocycline has anti-inflammatory properties. Minocycline inhibits lipopolysaccharide mediated inflammatory cytokine tumour necrosis factor (TNF-α) secretion by macrophages. Minocycline inhibits macrophage proliferation in a dose dependent manner. Minocycline inhibits neuroinflammation in pre-plaque of Alzheimer′s disease-like amyloid pathology through inhibition of key inflammatory enzymes like inducible nitric oxide synthase (iNOS), matrix metalloproteinase 9 (MMP-9) and 5-lipoxygenase. Minocycline inhibits endothelial cell proliferation and angiogenesis. Minocycline exhibits anti-tumor activity in glioma by inhibiting membrane type 1 matrix metalloproteinase (MT1-MMP). Minocycline increases cognition and neuronal differentiation. zMinocycline effectively reduces neuropathic pain by increasing the functions of nociceptin/orphanin FQ.
S0417 Silibinin ≥98% (HPLC) Silibinin function as a hepatoprotectant in patients with acute and chronic liver injury. This flavonoid fights against various cancer cells including, prostate, skin, breast, colon, lung, bladder and hepatocellular carcinoma (HCC). Silibinin exhibits its efficacy as an anti-cancer agent by blocking the secretion of proangiogenic factors from tumor cells, and by hindering growth and inducing apoptotic death of endothelial cells. In addition, it also interrupts capillary tube formation on Matrigel. Silibinin might be a good candidate for chemoprevention of prostate cancer (PC). It might be used as a potential therapeutic regimen for the treatment of endometriosis in vitro and in vivo.
S0292 Silymarin flavonolignans Silymarin is originally known to protect liver from various toxic agents and is used in treating hepatitis and cirrhosis. Silymarin possesses many biological actions such as antifibrotic, anti-lipid peroxidative, anti-inflammatory, immunomodulatory and membrane stabilizing. Silymarin also aids in liver regeneration.
Silymarin provides cardioprotective activity against ischemia-reperfusion induced myocardial infarction in rats.
Silymarin was shown to protect the liver from the cytotoxic effects of anti-tuberculosis drugs by decreasing serum alanine aminotransferase (ALT), aspartate aminotransferase (AST) and alkaline phosphatase (ALP) levels. This effect was related to the anti-oxidant effects of silymarin.
S6942 Staurosporine solution from Streptomyces sp. Ready Made Solution, 1 mM in DMSO (100 μg/214 μL), 0.2 μm filtered Potent cell-permeable inhibitor of protein kinase C. Induces apoptosis in Jurkat cells.
Potent inhibitor of phospholipid/calcium-dependent protein kinase. Inhibits the upregulation of VEGF expression in tumor cells.
S8442 SU 5416 ≥98% (HPLC) SU 516 inhibits the activity of neuronal nitric oxide synthase and protects the neuronal cells from nitric oxide-mediated neurotoxicity.1 It also acts an agonist of aryl hydrocarbon receptor and is an effective clinical agent for treating autoimmune diseases and transplant rejection.2
SU 5416 is a vascular endothelial growth factor (VEGF) receptor protein tyrosine kinase 1/2 inhibitor.
T144 (±)-Thalidomide ≥98%, powder (±)-Thalidomide selectively inhibits biosynthesis of tumor necrosis factor α (TNF-α). It also functions as an inhibitor of angiogenesis, an immunosuppressive agent, a sedative and a teratogen. Furthermore, thalidomide is known to exhibit antitumor functions in refractory multiple myeloma.
W4394 Withaferin A ≥95% (HPLC) Steroidal lactone that exhibits cytotoxicity towards tumor cells. Protective effects attributed to anti-lipid peroxidative, antioxidant and detoxifying functionality.
Withaferin A is a steroidal lactone that is isolated from the plant Withania somnifera. It has potent anti-inflammatory properties as it inhibits the activation of NF-κ B signaling pathway. The anti-tumor activity of Withaferin A is due to its ability to alter cytoskeletal architecture by binding annexin II and disrupting F actin cross-links. Withaferin A also inhibits angiogenesis by binding to vimentin and F-actin.