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

Thienopyridone 

Cat. No.: HY-128153 Purity: 98.04%
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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5 mg USD 300 In-stock
Estimated Time of Arrival: December 31
10 mg USD 480 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1350 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1950 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 5 mg/mL (20.64 mM; ultrasonic and warming and adjust pH to 5 with HCl and heat to 80°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.1271 mL 20.6356 mL 41.2712 mL
5 mM 0.8254 mL 4.1271 mL 8.2542 mL
10 mM 0.4127 mL 2.0636 mL 4.1271 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (8.58 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

ThienopyridonePhosphataseApoptosisPRLoncogenicphosphatasesp130CascleavageapoptosisanticancerFAKPARPcaspase-8Inhibitorinhibitorinhibit

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Product Name:
Thienopyridone
Cat. No.:
HY-128153
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