1018454-97-1

1018454-97-1 structure
1018454-97-1 structure
  • Name: Thienopyridone
  • Chemical Name: Thienopyridone
  • CAS Number: 1018454-97-1
  • Molecular Formula: C13H10N2OS
  • Molecular Weight: 242.30
  • Catalog: Signaling Pathways Apoptosis Apoptosis
  • Create Date: 2020-06-01 19:15:28
  • Modify Date: 2024-01-10 19:29:45
  • Thienopyridone is a potent and selective phosphatase of regenerating liver (PRL) phosphatase inhibitor with IC50s of 173 nM, 277 nM and 128 nM for PRL-1, PRL-2, and PRL-3, respectively. Thienopyridone shows minimal effects on other phosphatases. Thienopyridone induces p130Cas cleavage and apoptosis and has anticancer effects[1].

Name Thienopyridone
Description Thienopyridone is a potent and selective phosphatase of regenerating liver (PRL) phosphatase inhibitor with IC50s of 173 nM, 277 nM and 128 nM for PRL-1, PRL-2, and PRL-3, respectively. Thienopyridone shows minimal effects on other phosphatases. Thienopyridone induces p130Cas cleavage and apoptosis and has anticancer effects[1].
Related Catalog
Target

IC50: 173 nM (PRL-1), 277 nM (PRL-2) and 128 nM (PRL-3)[1]

In Vitro Thienopyridone shows significant inhibition of tumor cell anchorage-independent growth in soft agar. The EC50 values of the Thienopyridone are 3.29 μM and 3.05 μM for RKO and HT-29 cells, respectively[1]. Thienopyridone (1-75 μM; 24 hours; HeLa cells) treatment shows a dose-dependent down-regulation of total p130Cas in HeLa cells. Thienopyridone induces p130Cas and FAK cleavage leads to caspase-mediated cell apoptosis. Thienopyridone induces the cleavage of PARP and caspase-8[1]. Thienopyridone (3.75-30 μM; 24 hours) significantly suppresses HUVEC migration but not proliferation[1]. Cell Viability Assay[1] Cell Line: RKO and HT-29 cells Concentration: 0.5 μM, 1.67 μM, 5 μM, 8.33 μM Incubation Time: 14 days Result: Exhibited a dose-dependent inhibition in cancer cell anchorage-independent growth as measured by either colony number or colony size. Western Blot Analysis[1] Cell Line: HeLa cells Concentration: 1 μM, 5 μM, 10 μM, 25 μM, 50 μM, 75 μM Incubation Time: 24 hours Result: A dose-dependent down-regulation of total p130Cas was observed.
References

[1]. Daouti S, et al. A selective phosphatase of regenerating liver phosphatase inhibitor suppresses tumor cell anchorage-independent growth by a novel mechanism involving p130Cas cleavage. Cancer Res. 2008 Feb 15;68(4):1162-9.

Molecular Formula C13H10N2OS
Molecular Weight 242.30
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