Squarunkin A 是一种有效的选择性 UNC119-内容物 (Cargo) 相互作用抑制剂,能够抑制 UNC119A 与肉豆蔻酰化的 Src N 末端肽相互作用 (IC50=10 nM)。Squarunkin A 会干扰细胞中 Src 激酶的活化。
生物活性
Squarunkin A is a potent and selective UNC119-cargo interaction inhibitor, interrupting the UNC119A-myristoylated Src N-terminal peptide interaction (IC 50 =10 nM). Squarunkin A interferes with the activation of Src kinase in cells.
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。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。 has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : 9.62 mg/mL (18.37 mM; ultrasonic and warming and heat to 60°C)配制储备液