|Solubility||Soluble in DMSO.|
|Declaration||Manufactured by SynKinase.|
|Other Product Data||
Target: VEGFR2/YES/MLKL | Kinase Group: RTK | Substrate: Tyrosine
Click here for Original Manufacturer Product Datasheet
Our product description may differ slightly from the original manufacturers product datasheet.
|Shipping and Handling|
|Short Term Storage||+4°C|
|Long Term Storage||-20°C|
|Use/Stability||Stable for at least 2 years after receipt when stored at -20°C.|
|Product Specification Sheet|
Potent protein kinase VEGFR2 inhibitor (2nm range). Binds to the pseudokinase domain of MLKL and blocks cell death by necroptosis, as well. With regards to its role in necroptosis, it is an ATP-mimetic that was shown to bind recombinant mouse MLKL pseudokinase domain, which showed inhibited TSQ-induced death of mouse dermal fibroblasts by delaying MLKL translocation to the membrane. Appears therefore to be a valuable reagent to inhibit necroptosis. It also provides an important proof-of-principle that targeting catalytically-dead pseudoenzymes represents a feasible, emerging therapeutic avenue.
- Discovery of a novel and potent series of dianilinopyrimidineurea and urea isostere inhibitors of VEGFR2 tyrosine kinase: D.M. Sammond, et al.; Bioorg. Med. Chem Lett. 15, 3519 (2005)
- Activation of the pseudokinase MLKL unleashes the four-helix bundle domain to induce membrane localization and necroptotic cell death: J.M. Hildebrand, et al.; PNAS 111, 15072 (2014)
- Identification and structure-function analysis of subfamily selective G protein-coupled receptor kinase inhibitors: K.T. Homan, et al.; ACS Chem. Biol. 10, 310 (2015)
- Neutrophil necroptosis is triggered by ligation of adhesion molecules following GM-CSF priming: X. Wang, et al.; J. Immunol. 197, 4090 (2016)