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TCS 401

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Chemical Structure| 243966-09-8 同义名 : -
CAS号 : 243966-09-8
货号 : A420041
分子式 : C10H11ClN2O5S
纯度 : 99%+
分子量 : 306.723
MDL号 : MFCD09971132
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

0.1 M NaOH: 6 mg/mL(19.56 mM)，配合低频超声，并调节pH至9
动物实验配方：
生物活性
描述 Protein tyrosine phosphatase-1B (PTP1B) is an important negative regulator of insulin receptor- and vascular endothelial growth factor receptor-dependent signalings in endothelial cells. Genetic or pharmacological inhibition of PTP1B has been shown to enhance endothelial cell proliferation and migration and increase nitric oxide production. In vivo, inhibiting PTP1B can reverse endothelial dysfunction, promote angiogenesis, and accelerate wound healing[3]. Upon activation of pattern recognition receptors, macrophages and plasmacytoid dendritic cells from PTP1B-knockout mice secrete lower amounts of type I interferon (IFN) than cells from wild-type mice. In contrast, secretion of the proinflammatory cytokines TNFα and IL6 was unaltered. While PTP1B deficiency did not affect Ifnb1 transcription, type I IFN accumulated in macrophages, suggesting a role for PTP1B in mediating secretion of type I IFN[4]. TCS 401 is a selective inhibitor of 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. TCS-401 treatment activates the MEK/Erk and PI3K/Akt signaling pathways and induces proliferation, differentiation, and migration in RPE cells[5]. TCS-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[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.26mL

0.65mL

0.33mL

16.30mL

3.26mL

1.63mL

32.60mL

6.52mL

3.26mL
参考文献

[1]Du ZD, Hu LT, et al. Protein tyrosine phosphatase 1B regulates the activity of retinal pigment epithelial cells. Mol Vis. 2015 May 1;21:523-31. eCollection 2015.

[2]Ponnusamy M, Ma L, 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.

[3]Yuan Wang,et al. Inhibiting Protein Tyrosine Phosphatase 1B to Improve Regenerative Functions of Endothelial Cells. J Cardiovasc Pharmacol. 2018 Feb;71(2):59-64.

[4]Elisa Reimer,et al. Protein tyrosine phosphatase 1B is involved in efficient type I interferon secretion upon viral infection. J Cell Sci. 2020 Apr 23;134(5):jcs246421.

[5] Du ZD, et al. Protein tyrosine phosphatase 1B regulates the activity of retinal pigment epithelial cells. Mol Vis. 2015 May 1;21:523-31.

[6] 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.