Tie-2

MGCD265 is a multitargeted tyrosine kinase inhibitor that binds to and inhibits the phosphorylation of several RTKs, including the c-Met receptor (HGFR); the Tek/Tie-2 receptor; VEGFR types 1, 2, and 3; and MST1R.

Pexmetinib is a potent inhibitor of cytokine synthesis, via the dual inhibition of p38 mitogen-activated protein kinase (MAPK), and Tie2/Tek receptor tyrosine kinase.

Tie2 kinase inhibitor is a potent and selective Tie2 inhibitor with IC50 of 0.25 μM.

XL184 free base (Cabozantinib) is a small molecule designed to inhibit multiple receptor tyrosine kinases, specifically MET and VEGFR2.

AMG-Tie2-1 is a highly potent, non-selective inhibitor of Tie-2 (IC50 <1 nM).

Altiratinib is a novel c-MET/TIE-2/VEGFR inhibitor; effectively reduce tumor burden in vivo and block c-MET pTyr(1349)-mediated signaling, cell growth and migration as compared with a HGF antagonist in vitro.

Sodium succinate dibasic is an inhibitor of multiple receptor tyrosine kinases. Sodium succinate dibasic is known to be a potent inhibitor of Met, Flt-1 (VEGFR1), Flk-1 (VEGFR2), Flt-3 (VEGFR3), Ron, and Tie-2. Sodium succinate dibasic has been observed to inhibit Met (c-Met)-driven tumor cell and non-c-Met driven tumor cell (HCT116 and MDA-MB-231) proliferation. This product has also been observed to effectively inhibit c-Met phosphorylation and its downstream signaling pathways in serum starved MKN45 cells, as well as inducing apoptosis in these cells.

CE-245677 is a potent reversible inhibitor of Tie2 and TrkA/B kinases with a cellular IC50s of 4.7 and 1 nM.

TIE-2/VEGFR-2 kinase-IN-2 is a potent dual inhibitor of the Vascular Endothelial Growth Factor Receptor 2 (VEGFR2) and the Tyrosine kinase with immunoglobulin-like and EGF-like domains 2 (Tie-2), exhibiting pIC50 values of 8.61 and 8.56, respectively. This compound serves as an effective anti-angiogenic agent, making it a valuable tool for cancer research. Its ability to inhibit both targets can provide insights into tumor vascularization and growth.

GW768505A free base is a potent dual inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR2) and Tie-2, exhibiting a pIC50 of 7.81 for VEGFR2. This compound demonstrates significant anti-angiogenic activity, making it valuable for research applications in cancer biology and therapeutic angiogenesis. It can be utilized in studies aimed at elucidating the roles of VEGFR2 and Tie-2 in various pathological conditions.

TIE-2/VEGFR-2 kinase-IN-1 is a potent inhibitor targeting the TIE-2 and VEGFR-2 kinases, which are critical regulators of angiogenesis. This compound is instrumental in researching diseases characterized by abnormal blood vessel formation, including various cancers and diabetic retinopathy. Its application facilitates the exploration of therapeutic strategies aimed at modulating angiogenic processes and offers insights into the underlying mechanisms of angiogenesis-related pathologies.

RK-20448 is an ATP-competitive inhibitor targeting Lck, Src, KDR/VEGF2R, and Tie-2, demonstrating IC50 values of 0.24, 1.19, 10.74, and 5.85 µM, respectively. Additionally, it inhibits BLK, Csk, Fyn, and Lyn, with IC50 values of 0.37, 4.27, 2.03, and 0.43 µM, respectively. This compound is valuable for research involving signal transduction pathways mediated by receptor tyrosine kinases and may contribute to studies on cancer and vascular biology.

TIE-2/VEGFR-2 kinase-IN-5 is a selective inhibitor of TIE-2 and VEGFR-2 receptor tyrosine kinases, with reported pIC50 values of 7.78 nM and 8.11 nM, respectively. This compound exhibits strong anti-angiogenic properties, making it valuable for studies investigating angiogenesis and associated therapeutic strategies. Its ability to effectively disrupt signaling pathways involved in blood vessel formation positions TIE-2/VEGFR-2 kinase-IN-5 as a critical tool for research in vascular biology and cancer therapeutics.

TIE-2/VEGFR-2 kinase-IN-3 is a benzimidazole compound that selectively inhibits TIE-2 and VEGFR-2 tyrosine kinase receptors, exhibiting IC50 values of 6.9 nM and 3.5 nM, respectively. This inhibitor is valuable for research focused on angiogenesis, providing insights into tumor growth and vascular development. Its potent activity makes it a significant tool for investigating therapeutic strategies targeting vascular-related diseases.

TIE-2/VEGFR-2 kinase-IN-4 is a benzimidazole compound that functions as a potent inhibitor of TIE-2 and VEGFR-2 tyrosine kinase receptors, with IC50 values of 5.2 nM and 5.1 nM, respectively. This inhibitor effectively modulates signaling pathways involved in angiogenesis, making it a valuable reagent for research focused on vascular development and tumor growth. Its specificity for both targets allows for detailed studies in cancer biology and therapeutic development.

TP-S1-68 is a potent TIE-2 inhibitor with an IC50 of 3.65 μM. This compound demonstrates significant antibacterial activity against a range of bacterial and fungal pathogens. TP-S1-68 serves as a valuable starting point for the development of novel TIE-2 inhibitors and is applicable in research focused on solid tumors, as well as bacterial and fungal infections.

SB-633825 is a potent ATP-competitive inhibitor targeting TIE2, LOK (STK10), and BRK, with IC50 values of 3.5 nM, 66 nM, and 150 nM, respectively. This compound effectively inhibits cancer cell proliferation and angiogenesis, making it a valuable tool for research on tumor growth and vascular development. Its selective inhibition profile supports studies aimed at understanding the roles of these kinases in cancer biology and therapeutic strategies.

BAY-826 is a selective and potent inhibitor of the TIE2 receptor, exhibiting a binding affinity (Kd) of 1.6 nM. This compound plays a significant role in studying angiogenesis and vascular biology by modulating TIE2 signaling pathways. Its application in research encompasses tumor microenvironment studies, vascular disorder investigations, and potential therapeutic strategies targeting vascular-related diseases.

6-Hydroxy-2,2′,4,4′-tetrabromodiphenyl ether is a selective inhibitor of Tie2 kinase, exhibiting an IC50 value of 2.1 μM. This compound interacts with the ATP binding site of Tie2, effectively inhibiting its kinase activity and thereby blocking tumor angiogenesis. It is a valuable tool for research focused on vascular biology and cancer therapeutics.

Vasculotide is a Tie-2 activator that mimics angiopoietin-1, inducing phosphorylation of the Tie-2 receptor. It exhibits anti-inflammatory properties and reduces vascular permeability, making it effective in ameliorating endotoxin-induced endothelial barrier dysfunction. Research applications include promoting angiogenesis in diabetic ulcer models and protecting against vascular leakage in murine abdominal sepsis, while also improving microcirculatory perfusion in rat models of hemorrhagic shock.

Trebananib is an Fc fusion peptibody that selectively neutralizes angiopoietin 1 (Ang1) and angiopoietin 2 (Ang2) by inhibiting their interaction with the TIE2 receptor. This mechanism leads to significant anti-angiogenic and anti-tumor effects, making Trebananib a valuable tool for research in cancer biology and vascular studies. Its ability to modulate angiogenesis provides important insights for therapeutic strategies targeting tumor vasculature.

Tie2 kinase inhibitor 2 is a selective inhibitor of the Tie2 kinase with an IC50 value of 1 μM. It effectively inhibits endothelial cell tube formation, making it a valuable tool for investigating Tie2-mediated angiogenic disorders. This compound is suitable for research focused on angiogenesis and related therapeutic applications.

Tie2 Kinase Inhibitor 3 is a potent inhibitor of the Tie-2 kinase, exhibiting an IC50 value of 30 nM. By competing with the ATP binding site of Tie-2, this compound effectively inhibits phosphorylation and signaling pathways associated with Tie-2, thereby influencing the stability and maturation of blood vessels. Its mechanisms provide valuable insights into tumor angiogenesis, making Tie2 kinase inhibitor 3 a significant tool for research focused on restricting tumor growth and modulating angiogenic processes.

BSF-466895 is a potent Tie2 inhibitor with an IC50 value of 5 nM, demonstrating significant inhibition of Tie1 as well. This compound is valuable for research applications focused on vascular biology and angiogenesis, as well as exploring the therapeutic potential in disorders related to angiogenic dysregulation. BSF-466895 serves as a useful tool for elucidating the role of the Tie2 signaling pathway in various biological contexts.