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TCS 401

Katalog-Nr.GC12020

A selective PTP1B inhibitor

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TCS 401 Chemische Struktur

Cas No.: 243966-09-8

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5mg
90,00 $
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10mg
144,00 $
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25mg
288,00 $
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50mg
432,00 $
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Sample solution is provided at 25 µL, 10mM.

Description of TCS 401

TCS 401 is a selective inhibitor of protein tyrosine phosphatase 1B (PTP1B).

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].

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.

Protocol of TCS 401

Cell experiment:

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.

Chemical Properties of TCS 401

Cas No. 243966-09-8 SDF
Chemical Name 2-(carboxyformamido)-4,5,6,7-tetrahydrothieno[2,3-c]pyridine-3-carboxylic acid hydrochloride
Canonical SMILES O=C(C(O)=O)NC1=C(C(O)=O)C2=C(S1)CNCC2.Cl
Formula C10H10N2O5S.HCl M.Wt 306.72
Löslichkeit 0.1 M NaOH: 5 mg/ml Storage Desiccate at RT
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of TCS 401

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 3.2603 mL 16.3015 mL 32.603 mL
5 mM 0.6521 mL 3.2603 mL 6.5206 mL
10 mM 0.326 mL 1.6302 mL 3.2603 mL
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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