1. Metabolic Enzyme/Protease
    Apoptosis
  2. Phosphatase
    Apoptosis
  3. Thienopyridone

Thienopyridone 

Cat. No.: HY-128153
Handling Instructions

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.

For research use only. We do not sell to patients.

Thienopyridone Chemical Structure

Thienopyridone Chemical Structure

CAS No. : 1018454-97-1

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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].

IC50 & 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

242.30

Formula

C₁₃H₁₀N₂OS

CAS No.

1018454-97-1

SMILES

O=C1C(C=C(C2=CC=CC=C2)S3)=C3C(N)=CN1

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

ThienopyridonePhosphataseApoptosisPRLoncogenicphosphatasesp130CascleavageapoptosisanticancerFAKPARPcaspase-8Inhibitorinhibitorinhibit

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Thienopyridone
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