Braco-19 (trihydrochloride)

Braco-19 trihydrochloride is a potent telomerase/telomere inhibitor, preventing the capping and catalytic action of telomerase. Braco-19 acts as G-quadruplex (GQ) binding ligand, stabilizing G-quadruplexes formation at the 3V telomeric DNA overhang and produce rapid senescence or selective cell death. Braco-19 is also a HAdV virus replication inhibitor^[1][2]. IC50 & Target: IC50: telomerase^[1] In Vitro: Braco-19 trihydrochloride, as a well-known GQ binding ligand, interacts specifically with the HAdV GQs and increases their stability, and blocks the HAdV multiplication^[2].
BRACO-19 trihydrochloride (1.0-10 μM; 5 day) cause zero growth inhibition is found 1 μM, the IC₅₀ for BRACO-19 in UXF1138L cells is 2.5 μM, the IC₁₀₀ is 5 μM^[1].
BRACO-19 trihydrochloride (1 μM; 24 hours) shows dramatically reduced nuclear hTERT expression. However, residual cytoplasmic hTERT staining is observed accompanied by the occurrence of atypical mitoses^[1].
BRACO-19 trihydrochloride (0-40 μM; 24 hours) decreases the AdV virus growth in a dose-dependent manner in eGFP-transinfected HEK 293 cells^[2].
BRACO-19 trihydrochloride (0-150 μM; 24 hours) shows a decrease in band intensity in an increasing concentration-dependent manner^[2].
In Vivo: BRACO-19 trihydrochloride (oral administration or intraperitoneal injection; 2 or 5 mg/kg; 3 weeks) oral dosing regimen are always inactive and the animals have to be sacrificed due to high tumor burden before overall termination of the study, Chronic, i.p. BRACO-19 administration, qdx5 is efficient in inhibiting tumor growth in earlystage xenografts but not advanced-stage xenografts^[1].
BRACO-19 trihydrochloride (intraperitoneal injection; 2 mg/kg; 3 weeks; starting 6 days after transplantation of UXF1138LX fragments) inhibits tumor growth significantly and under these conditions, marked single-agent antitumor activity is observed, with some animals in the group showing complete regressions (5 of 12 tumors)^[1].