Cucurbit[8]uril

Cucurbit[8]uril is a potent, low toxicity and orally active supramolecular inducer of protein heterodimerization. Cucurbit[8]uril induces heterodimerization of methylviologen and naphthalene functionalized proteins. Cucurbit[8]uril can induce energy transfer ^[1][2]. IC50 & Target: Protein Heterodimerization^[1] In Vitro: Cucurbit[8]uril (0~20 μM; 48 hours; CHO-K1 cells) makes the relative cell viability dropped marginally to 86%^[2].
Cucurbit[8]uril indeed selectively induces the heterodimerization of MV–eYFP with Np–eCFP. Cucurbit[8]uril-induced high energy transfer between the proteins is only observed in the presence of all three supramolecular components, allowing the formation of the ternary complex. In the presence of Cucurbit[8]uril, the unspecific protein assembly induced by the methylviologen is inhibited. The ternary system of Cucurbit[8]uril with methylviologen (MV) and naphthalene (NP) can also be successfully used for the formation of selective protein heterodimers of more hydrophobic proteins. The presence of Cucurbit[8]uril as a host molecule is required to prevent MV induced unspecific dimerization with hydrophobic protein surfaces^[1]. In Vivo: Cucurbit[8]uril shows a very low toxicity of the in vivo intravenous injection, as well as oral administration studies on mice^[2].