Description
SCR7 is an unstable form that can be autocyclized into a stable form SCR7 pyrazine. SCR7 pyrazine is a DNA ligase IV inhibitor that blocks nonhomologous end-joining (NHEJ) in a ligase IV-dependent manner. SCR7 pyrazine is also a CRISPR/Cas9 enhancer which increases the efficiency of Cas9-mediated homology-directed repair (HDR). SCR7 pyrazine induces cell apoptosis and has anticancer activityIn VitroSCR7 (SCR7 pyrazine; 20-100 µM; 24 hours; MCF7 cells) treatment interferes with NHEJ in cells, leading to accumulation of unrepaired double-strand breaks (DSBs). SCR7 (SCR7 pyrazine) treatment shows a dose-dependent decrease in cell proliferation with IC 50 values of 40 µM, 34 µM, 44 µM, 8.5 µM, 120 µM, 10 µM and 50 µM for MCF7, A549, HeLa, T47D, A2780, HT1080 and Nalm6 cells, respectively. In MCF7 cells, SCR7 (SCR7 pyrazine; 20, 40 µM) treatment increases phosphorylation of ATM and activates p53, decreases MDM2, BCL2, resulting in activation of proapoptotic proteins, PUMA and BAX. And the shorter fragments of MCL1, PARP1, Caspase 3, and Caspase 9 cleavage are upregulated in a dose-dependent manner. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: MCF7 cells Concentration: 20 µM, 40 µM, 100 µM Incubation Time: 24 hours Result: Showed an increase in levels of gH2AX foci and protein.In VivoSCR7 (SCR7 pyrazine; 10 mg/kg; intraperitoneal injection; six doses; BALB/c mice) treatment significantly reduces breast adenocarcinoma-induced tumor and increases lifespan. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: BALB/c mice injected with breast adenocarcinoma cells Dosage: 10 mg/kg Administration: Intraperitoneal injection; on alternate days (0, 2, 4, 6, 8, and 10) Result: Significantly reduced breast adenocarcinoma-induced tumor and increased lifespan.Form:SolidIC50& Target:DNA Ligase IV CRISPR/Cas9