TCS 401
Cat. No.: DC23216
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Chemical Structure
243966-09-8
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Field of application
TCS 401 is a potent, selective inhibitor of protein-tyrosine phosphatase 1B (PTP1B) with Ki of 0.29 uM, weakly inhibits the protein phosphatases CD45 D1D2, PTPβ, PTPε D1, SHP-1, PTPα D1, and LAR D1D2 with Ki of 59, 560, 1,100, >2,000, >2,000, and >2,000 u
| Cas No.: |
243966-09-8 |
| Chemical Name: |
Thieno[2,3-c]pyridine-3-carboxylic acid, 2-[(carboxycarbonyl)amino]-4,5,6,7-tetrahydro-, hydrochloride (1:1) |
| Synonyms: |
TCS-401;TCS401 |
| SMILES: |
O=C(O)C1C2CCNCC=2SC=1NC(=O)C(=O)O.[H]Cl |
| Formula: |
C10H11ClN2O5S |
| M.Wt: |
306.7227 |
| Purity: |
>98% |
| Sotrage: |
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: |
TCS 401 is a selective inhibitor of protein tyrosine phosphatase 1B (PTP1B). |
| 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: |
[1]. Du ZD, et al. Protein tyrosine phosphatase 1B regulates the activity of retinal pigment epithelial cells. Mol Vis. 2015 May 1;21:523-31.
[2]. Ponnusamy M, et al. Necrotic renal epithelial cell inhibits renal interstitial fibroblast activation: role of protein tyrosine phosphatase 1B. Am J Physiol Renal Physiol. 2013 Mar 15;304(6):F698-709. |
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