TCS 401
Names
[ CAS No. ]:
243966-09-8
[ Name ]:
TCS 401
[Synonym ]:
Thieno[2,3-c]pyridine-3-carboxylic acid, 2-[(carboxycarbonyl)amino]-4,5,6,7-tetrahydro-, hydrochloride (1:1)
2-[(Carboxycarbonyl)amino]-4,5,6,7-tetrahydrothieno[2,3-c]pyridine-3-carboxylic acid hydrochloride (1:1)
Biological Activity
[Description]:
TCS 401 is a selective inhibitor of protein tyrosine phosphatase 1B (PTP1B).
[Related Catalog]:
[In Vitro]
TCS-401 (0.5, 1, 2 μM) significantly increases the proliferation of RPE cells. TCS-401 significantly increases the expression of cyclin A and cyclin D1 at the concentrations of 1 and 2 μM in a concentration-dependent manner. TCS-401 at concentrations of 0.5, 1, and 2 μM significantly increases phosphorylation of Erk and Akt compared to the control group. The activation of Erk and Akt by TCS-401 is blocked by pretreatment with PD98059 and LY294002, respectively. CS-401 treatment activates the MEK/Erk and PI3K/Akt signaling pathways and induces proliferation, differentiation, and migration in RPE cells[1]. CS-401 dose dependently inhibits the RPTC-Sup-induced reduction of fibronectin and α-SMA. At 1 μM, TCS-401 reverses the levels of fibronectin and α-SMA about onefold and at a dose of 2 μM, TCS-401 brings back fibronectin and α-SMA expression to near normal levels[2].
[Cell Assay]
Cell proliferation are examined using MTT assay. The 5×103 cells grown in a 96-well plate for 24 h are partially starved in DMEM/F12 supplemented with 1% FBS for 12 h, and then stimulated with various concentrations of TCS-401 for an additional 24 h. MTT are added to the culture medium, and the cells are incubated for an additional 4 h. The formazan crystals formed are then dissolved by adding dimethyl sulfoxide (100 μL per well). Absorbance at 490 nm are measured using a microplate reader.
[References]
[Related Small Molecules]
Chemical & Physical Properties
[ Molecular Formula ]:
C10H11ClN2O5S
[ Molecular Weight ]:
306.723
[ Exact Mass ]:
306.007721
[ Storage condition ]:
2-8℃