SCR7

SKU: orb1226138

Description

SCR7 is a specific inhibitor of nonhomologous end-joining (NHEJ), blocks Ligase IV-mediated joining by interfering with its DNA binding but not that of T4 DNA Ligase or Ligase I; inhibits NHEJ in a Ligase IV-dependent manner within cells, causes accumulation of double-strand breaks (DSBs), and activates the intrinsic apoptotic pathway; decreases cell proliferation of MCF7, A549, and HeLa with IC50 of 40, 34, and 44 uM, respectively; increases the efficacy of DSB-inducing therapeutic modalities in mouse xenografts; increases the efficiency of precise genome editing with CRISPR-Cas9 in mammalian cell lines and in mice.

Key Properties

• CAS Number: 1533426-72-0
• MW: 334.395
• Purity: >98% (HPLC)
• Formula: C₁₈H₁₄N₄OS
• SMILES: O=C(C(/N=C/C1=CC=CC=C1)=C(/N=C/C2=CC=CC=C2)N3)NC3=S
• Target: DNA/RNA Synthesis
• Solubility: DMSO: ≥ 45 mg/mL

Bioactivity

• In Vivo:
  SCR7 (SCR7 pyrazine; 10 mg/kg; intraperitoneal injection; six doses; BALB/c mice) treatment significantly reduces breast adenocarcinoma-induced tumor and increases lifespan. 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.
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• In Vitro:
  SCR7 (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 IC50 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. Western blot analysis. Cell 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.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SCR-7

Quick Database Links

Gene Symbol

DNA/RNA Synthesis