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.
Product information
CAS Number: 1018454-97-1
Molecular Weight: 242.30
Formula: C13H10N2OS
Chemical Name: 7-amino-2-phenyl-4H, 5H-thieno[3, 2-c]pyridin-4-one
Smiles: NC1=CNC(=O)C2C=C(SC=21)C1C=CC=CC=1
InChiKey: FBVOPOZVLBHOHR-UHFFFAOYSA-N
InChi: InChI=1S/C13H10N2OS/c14-10-7-15-13(16)9-6-11(17-12(9)10)8-4-2-1-3-5-8/h1-7H,14H2,(H,15,16)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 5 mg/mL (20.64 mM; ultrasonic and warming and adjust pH to 5 with HCl and heat to 80°C)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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. 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. Thienopyridone (3.75-30 μM; 24 hours) significantly suppresses HUVEC migration but not proliferation.
References:
- 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.
Products are for research use only. Not for human use.
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