DKFZ-633

DKFZ-633 is a potent KLK6 inhibitor and KLK6-specific probe with an IC₅₀ of 250 nM against human KLK6. DKFZ-633 covalently labels active KLK6 in a specific manner, and successfully pulls down and captures endogenous active KLK6 from cell-conditioned media. DKFZ-633 serves as a critical tool for investigating the function of KLK6 and its regulatory mechanisms in head and neck cancer^[1]. In Vitro:DKFZ-633 (compound 44) (0.25 μM; 30 min) inhibits recombinant triple-mutant human KLK6, with an IC₅₀ of 0.25 μM after 30 min of pre-incubation at room temperature^[1].
DKFZ-633 (12-25 μM; 1 h; room temperature) pulls down active endogenous human KLK6 from FaDu cell-conditioned medium in a dose-dependent manner^[1].
DKFZ-633 (50 μM; 1 h; room temperature) pulls down active endogenous human KLK6 from the conditioned media of various human cancer cell lines, including two cell-dependent glycoforms^[1].