GW806742X 是一种混合谱系激酶结构域样蛋白 (MLKL) 抑制剂,结合 MLKL 假激酶域的 Kd 值为 9.3 μM,并具有抗坏死活性。GW806742X 也具有抗 VEGFR2 的活性。
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GW806742X is a Mixed Lineage Kinase Domain-Like protein (MLKL) inhibitor which binds the MLKL pseudokinase domain with a Kd value of 9.3 μM and has anti-necroptosis activity. GW806742X has activity against VEGFR2[1][2]. Kd: 9.3 μM (MLKL)[1]
[1]. Hildebrand JM, et al. Activation of the pseudokinase MLKL unleashes the four-helix bundle domain to induce membrane localization and necroptotic cell death. Proc Natl Acad Sci U S A. 2014 Oct 21;111(42):15072-7. [2]. Yan B, et al. Discovery of a new class of highly potent necroptosis inhibitors targeting the mixed lineagekinase domain-like protein. Chem Commun (Camb). 2017 Mar 28;53(26):3637-3640.
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