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14892-97-8

14892-97-8 structure
14892-97-8 structure
  • Name: SCR7 pyrazine
  • Chemical Name: 6,7-diphenyl-2-sulfanylidene-1H-pteridin-4-one
  • CAS Number: 14892-97-8
  • Molecular Formula: C18H12N4OS
  • Molecular Weight: 332.37900
  • Catalog: Signaling Pathways Apoptosis Apoptosis
  • Create Date: 2016-12-17 08:23:07
  • Modify Date: 2024-01-18 08:05:59
  • 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 activity[1][2].

Name 6,7-diphenyl-2-sulfanylidene-1H-pteridin-4-one
Synonyms 4-Oxo-6,7-diphenyl-2-thioxotetrahydropteridin
6,7-diphenyl-2-thiolumazine
2-Thioxo-4-oxo-6,7-diphenyl-1H,3H-pteridin
6,7-diphenyl-2-thioxo-2,3-dihydro-1H-pteridin-4-one
6,7-Diphenyl-2-thioxo-2,3-dihydro-1H-pteridin-4-on
SCR7 pyrazine
Description 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 activity[1][2].
Related Catalog
Target

DNA Ligase IV[1] CRISPR/Cas9[2]

In Vitro SCR7 pyrazine (20-100 μM; 24 hours; MCF7 cells) treatment interferes with NHEJ in cells, leading to accumulation of unrepaired double-strand breaks (DSBs)[1]. 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[1]. In MCF7 cells, 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[1]. Western Blot Analysis[1] 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.
In Vivo SCR7 pyrazine (10 mg/kg; intraperitoneal injection; six doses; BALB/c mice) treatment significantly reduces breast adenocarcinoma-induced tumor and increases lifespan[1]. Animal Model: BALB/c mice injected with breast adenocarcinoma cells[1] 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.
References

[1]. Srivastava M, et al. An inhibitor of nonhomologous end-joining abrogates double-strand break repair and impedes cancer progression. Cell. 2012 Dec 21;151(7):1474-87.

[2]. Lin C, et al. Increasing the Efficiency of CRISPR/Cas9-mediated Precise Genome Editing of HSV-1 Virus in Human Cells. Sci Rep. 2016 Oct 7;6:34531.

Melting Point 209 °C
Molecular Formula C18H12N4OS
Molecular Weight 332.37900
Exact Mass 332.07300
PSA 110.59000
LogP 3.74810
Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302
Precautionary Statements P301 + P312 + P330
RIDADR NONH for all modes of transport