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Braco-19 trihydrochloride

CAS No. : 1177798-88-7

MCE 站：Braco-19 trihydrochloride

产品活性：Braco-19 trihydrochloride 是一种有效的端粒酶/端粒 (telomerase/telomere) 抑制剂，可防止端粒酶的催化作用。Braco-19 trihydrochloride 作为四联体 (GQ) 结合配体，稳定 GQ 四联体在 3V 端粒 DNA 处的形成，并可以导致快速衰老或选择性细胞死亡。Braco-19 trihydrochloride 也是一种HAdV病毒复制抑制剂。

研究领域：Cell Cycle/DNA Damage  |  Anti-infection

作用靶点：DNA/RNA Synthesis  |  CMV

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.
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.
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.
BRACO-19 trihydrochloride (0-40 μM; 24 hours) decreases the AdV virus growth in a dose-dependent manner in eGFP-transinfected HEK 293 cells.
BRACO-19 trihydrochloride (0-150 μM; 24 hours) shows a decrease in band intensity in an increasing concentration-dependent manner.

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.
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).

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