Bioactivity | 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]. | ||||||||||||
Target | IC50: 10 nM (UNC119A-myristoylated Src N-terminal peptide interaction) | ||||||||||||
Invitro | 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]。 | ||||||||||||
Name | Squarunkin A | ||||||||||||
CAS | 2101958-02-3 | ||||||||||||
Formula | C25H32F3N5O4 | ||||||||||||
Molar Mass | 523.55 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [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. |