MW 439.5 Da, Purity >99%. Potent, reversible and selective ATP-binding site-targeting Tie2 kinase inhibitor (IC50 = 250 nM). Anti- angiogenesis agent. Active in vivo and in vivo. Cell-permeable.
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- EMBO molecular medicine 14:e143642022Angpt2/Tie2 autostimulatory loop controls tumorigenesis.Applications:Unspecified applicationReactive species:Unspecified reactive speciesNinelia Minaskan Karabid,Tobias Wiedemann,Sebastian Gulde,Hermine Mohr,Renu Chandra Segaran,Julia Geppert,Maria Rohm,Giovanni Vitale,Germano Gaudenzi,Alessandra Dicitore,Donna Pauler Ankerst,Yiyao Chen,Rickmer Braren,Georg Kaissis,Franz Schilling,Mathias Schillmaier,Graeme Eisenhofer,Stephan Herzig,Federico Roncaroli,Jürgen B Honegger,Natalia S PellegataPubMed 35266635
- Molecular therapy. Nucleic acids 17:49-622019miR-15a/-16 Inhibit Angiogenesis by Targeting the Tie2 Coding Sequence: Therapeutic Potential of a miR-15a/16 Decoy System in Limb Ischemia.Applications:Unspecified applicationReactive species:Unspecified reactive speciesMarie Besnier et. al.PubMed 31220779
Key facts
- CAS number
- 948557-43-5
- Purity
- > 99%
- Form
- Solid
- Molecular weight
- 439.5 Da
- Molecular formula
- C26H21N3O2S
- PubChem identifier
- 23625762
- Nature
- Synthetic
Alternative names
Angiopoietin-1 receptor, CD202b, CD202b antigen, Endothelial tyrosine kinase, Endothelium specific receptor tyrosine kinase 2, Hyk, Soluble TIE2 variant 1, Soluble TIE2 variant 2, TEK tyrosine kinase endothelial, TIE2_HUMAN, Tek, Tunica interna endothelial cell kinase, Tyrosine kinase with Ig and EGF homology domains-2, Tyrosine-protein kinase receptor TEK, Tyrosine-protein kinase receptor TIE-2, VMCM, VMCM 1, Venous malformations multiple cutaneous and mucosal, hTIE 2, p140 TEK, tek tyrosine kinase
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MW 439.5 Da, Purity >99%. Potent, reversible and selective ATP-binding site-targeting Tie2 kinase inhibitor (IC50 = 250 nM). Anti- angiogenesis agent. Active in vivo and in vivo. Cell-permeable.
Key facts
- CAS number
- 948557-43-5
- Purity
- > 99%
- Form
- Solid
- Molecular weight
- 439.5 Da
- Molecular formula
- C26H21N3O2S
- PubChem identifier
- 23625762
- Nature
- Synthetic
- Solubility
Soluble in DMSO to 50 mM.
- Biochemical name
- 4-[4-(6-methoxy-2-naphthalenyl)-2-(4-methylsulfinylphenyl)-1H-imidazol-5-yl]pyridine
- Biological description
Potent, reversible and selective ATP-binding site-targeting Tie2 kinase inhibitor (IC50 = 250 nM). Anti- angiogenesis agent. Active in vivo and in vivo. Cell-permeable.
- Canonical SMILES
- COC1=CC2=C(C=C1)C=C(C=C2)C3=C(NC(=N3)C4=CC=C(C=C4)S(=O)C)C5=CC=NC=C5
- InChI
- InChI=1S/C26H21N3O2S/c1-31-22-8-5-19-15-21(4-3-20(19)16-22)25-24(17-11-13-27-14-12-17)28-26(29-25)18-6-9-23(10-7-18)32(2)30/h3-16H,1-2H3,(H,28,29)
- InChIKey
- SINQIEAULQKUPD-UHFFFAOYSA-N
- IUPAC name
- 4-[4-(6-methoxynaphthalen-2-yl)-2-(4-methylsulfinylphenyl)-1H-imidazol-5-yl]pyridine
Storage
- Shipped at conditions
- Ambient - Can Ship with Ice
- Appropriate short-term storage conditions
- +4°C
- Appropriate long-term storage conditions
- +4°C
- Storage information
- The product can be stored for up to 12 months
Supplementary info
- This supplementary information is collated from multiple sources and compiled automatically.
- Activity summary
TIE2 also known as TEK or CD202B is a receptor tyrosine kinase with a mass of approximately 145 kDa. It plays an important role in vascular development and maintenance. TIE2 is mainly expressed in endothelial cells which line the interior surface of blood vessels. It binds angiopoietins predominantly Angiopoietin-1 (Angpt1) influencing vascular stability and permeability. Researchers use TIE2 antibodies including anti-TIE and anti-clone to study its role and functions across various contexts.
- Biological function summary
TIE2 plays a central role in angiogenesis and blood vessel maturation. It forms a receptor complex with other components to mediate its effects. This interaction mainly involves Angpt1 which binds to TIE2 stabilizing blood vessels and preserving their integrity. TIE2 also participates in cell survival and migration processes necessary for normal vascular function. Researchers often perform Angpt1 ELISA in bulk to quantify interactions involving TIE2 in experiments.
- Pathways
TIE2 is important in the angiopoietin-TIE signaling pathway regulating vascular development. TIE2 is related to proteins such as Angpt1 which are centrally involved in this pathway. It also interacts with various signaling molecules including phosphatidylinositol-3-kinase (PI3K) which contributes to cell survival pathways. Alterations in the TIE2 signaling cascade can lead to aberrant angiogenesis and related pathologies.
- Associated diseases and disorders
TIE2 is implicated in several vascular diseases and cancer. Mutations or dysregulation of TIE2 can result in venous malformations and further compromise blood vessel integrity. In cancer TIE2 expression can influence tumor angiogenesis enhancing tumor growth and metastasis. TIE2 interacts with proteins like vascular endothelial growth factor (VEGF) which are involved in neovascularization and cancer progression. Understanding these interactions helps target therapeutic strategies in relevant diseases.
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Chemical Structure - Tie2 kinase inhibitor, ATP-binding site-targeting Tie2 kinase inhibitor. Cell-permeable. (ab141270)
2D chemical structure image of ab141270, Tie2 kinase inhibitor, ATP-binding site-targeting Tie2 kinase inhibitor. Cell-permeable.
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