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squarunkin A

Names

[ CAS No. ]:
2101958-02-3

[ Name ]:
squarunkin A

Biological Activity

[Description]:

Squarunkin A is a potent and selective UNC119-cargo interaction inhibitor, interrupting the UNC119A-myristoylated Src N-terminal peptide interaction (IC50=10 nM). Squarunkin A interferes with the activation of Src kinase in cells[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Src

[Target]

IC50: 10 nM (UNC119A-myristoylated Src N-terminal peptide interaction)[1]


[In Vitro]

Squarunkin A (2.5 μM, 0.625 μM, 0.078 μM 和 0.01 μM) 浓度依赖性地抑制 Src 磷酸化[1]。 Squarunkin A 不靶向其他脂蛋白伴侣的脂蛋白结合位点，如结合 s-戊烯化蛋白的 PDE6d, AIPL1 和 RhoGDI。Squarunkin A 在细胞裂解液中与 UNC119 结合并干扰 Src 激活[1]。

[References]

[1]. Tom Mejuch, et al. Small-Molecule Inhibition of the UNC119-Cargo Interaction. Angew Chem Int Ed Engl. 2017 May 22;56(22):6181-6186.  

Chemical & Physical Properties

[ Molecular Formula ]:
C25H32F3N5O4

[ Molecular Weight ]:
523.55

Related Compounds