243966-09-8

243966-09-8 - Names and Identifiers

Name	2-(Oxaloamino)-4,5,6,7-tetrahydrothieno[2,3-c]pyridine-3-carboxylic acid hydrochloride
Synonyms	TCS401 TCS-401 TCS 401 TCS 401 HCl TCS-401 Hydrochloride 2-(Oxaloamino)-4,5,6,7-tetrahydrothieno[2,3-c]pyridine-3-carboxylic acid hydrochloride
CAS	243966-09-8

243966-09-8 - Physico-chemical Properties

Molecular Formula	C10H11ClN2O5S
Molar Mass	306.72
Solubility	DMSO: 5 mg/mL mother liquor preservation: sub-packing and freezing to avoid repeated freezing and thawing;-20 ℃,1 month;-80 ℃,6 months (after dilution, the solution temperature is low and storage may precipitate, as far as possible to use the present) Mother liquor preservation: sub-packing and freezing to avoid repeated freezing and thawing;-20 ℃,1 month;-80 ℃,6 months (after dilution, the solution temperature is low and storage may precipitate, and try to use it now) Cell experiment: Dissolve with DMSO first: dilute with culture medium, and the dilution process is recommended to be carried out in sections to avoid excessive concentration changes leading to compound precipitation. If the compound is precipitated during the dilution process, it can be redissolved by ultrasound. During dilution, ensure that the final concentration of DMSO in the working fluid should be below 0.1% as far as possible, and the maximum should not exceed 0.5%, and set up a DMSO control group with correspond
Storage Condition	under inert gas (nitrogen or Argon) at 2-8°C
Use	TCS-401 (HCI) is a selective inhibitor of protein-tyrosine phosphatase 1B (PTP1B; Ki = 0.29 µM). It inhibits the protein phosphatases CD45 D1D2, PTPβ, PTPε D1, SHP-1, PTPα D1, and LAR D1D2 at much higher concentrations (Kis = 59, 560, 1,100, >2,000, >2,000, and >2,000 μM, respectively).1 Several PTPs have been proposed to act as negative regulators of insulin signaling, thus this enzyme is a potential drug target in diabetes.
In vitro study	TCS-401 (0.5, 1, 2μM) 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. 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.

243966-09-8 - Reference

Reference

1: Du ZD, Hu LT, Zhao GQ, Li Y, Ma ZZ. Protein tyrosine phosphatase 1B regulates the activity of retinal pigment epithelial cells. Mol Vis. 2015 May 1;21:523-31. eCollection 2015. PubMed PMID: 25999679; PubMed Central PMCID: PMC4431406.
2: Ponnusamy M, Ma L, Zhuang S. 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. doi: 10.1152/ajprenal.00564.2012. Epub 2013 Jan 2. PubMed PMID: 23283996; PubMed Central PMCID: PMC3602703.

243966-09-8 - Preparation solution concentration reference

	1mg	5mg	10mg
1 mM	3.26 ml	16.301 ml	32.603 ml
5 mM	0.652 ml	3.26 ml	6.521 ml
10 mM	0.326 ml	1.63 ml	3.26 ml
5 mM	0.065 ml	0.326 ml	0.652 ml

Last Update：2024-01-02 23:10:35

243966-09-8 - Cell Experiment

From the cultured RPE cells treated with TCS 401, cell proliferation was assessed using a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetracolium bromide assay, and the protein expression levels of cyclin A and cyclin D1 were determined. The effect of TCS 401 on cell differentiation was confirmed by immunostaining for α-smooth muscle actin and by western blot. Cell migration activity and PTP1B signaling mechanism were determined. Migration Assay was used to evaluate cell migration activity. PTP1B signaling mechanism was determined by use of PD98059 and LY294002.

Last Update：2023-08-16 21:32:38

243966-09-8 - Reference Information

biological activity

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

in vitro study

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. 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.

Last Update：2024-04-10 22:29:15