For research use only. Not for therapeutic Use.
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].
Squarunkin A (2.5 μM, 0.625 μM, 0.078 μM, and 0.01 μM) treatment leads to a concentration-dependent reduction of Src phosphorylation[1].
Squarunkin A does not target the lipoprotein-binding sites of other lipoprotein chaperones, such as PDE6d, AIPL1, and RhoGDI, which bind S-prenylated proteins. Squarunkin A binds to UNC119 in cell lysate and interferes with Src activation[1].
| Catalog Number | I042020 |
| CAS Number | 2101958-02-3 |
| Synonyms | ethyl 4-[[3,4-dioxo-2-[2-[4-[3-(trifluoromethyl)phenyl]piperazin-1-yl]ethylamino]cyclobuten-1-yl]amino]piperidine-1-carboxylate |
| Molecular Formula | C25H32F3N5O4 |
| Purity | ≥95% |
| InChI | InChI=1S/C25H32F3N5O4/c1-2-37-24(36)33-9-6-18(7-10-33)30-21-20(22(34)23(21)35)29-8-11-31-12-14-32(15-13-31)19-5-3-4-17(16-19)25(26,27)28/h3-5,16,18,29-30H,2,6-15H2,1H3 |
| InChIKey | ZKITWOVRRSBKFG-UHFFFAOYSA-N |
| SMILES | CCOC(=O)N1CCC(CC1)NC2=C(C(=O)C2=O)NCCN3CCN(CC3)C4=CC=CC(=C4)C(F)(F)F |
| 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. |
