tcsc0464 Daun02

Daun02 is converted by β-galactosidase to Daunorubicin, which is a topoisomerase inhibitor.

IC50 & Target: Topoisomerase^[1][2]

In Vitro: Daun02 is a prodrug, which is converted by β-galactosidase to Daunorubicin, which has been shown to reduce calcium ion (Ca²⁺)-dependent action potentials in neuroblastoma cells^[1]. Daunorubicin is a topoisomerase inhibitor^[2]. Daun02 is a good substrate for β-galactosidase (β-gal). The concentration of Daun02 producing 50% (EC₅₀) decrease in cell viability is 0.5 μM, 1.5 μM, and 3.5 μM for T47-D, Panc02, and MCF-7, respectively^[3].

In Vivo: Daun02 is a good substrate for β-gal with K_m and V_max values of 0.37 mM and 8.6 μmol/min/mg protein. At a concentration of 10^-5 M, Daun02 is 79% bound to plasma protein compares to 94% for Daunomycin^[3].