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CAS No.: 243966-09-8

TCS 401 Catalog No. CSN19100

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

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技术信息

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].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.2603 mL
- 16.3014 mL
- 32.6027 mL
- 5 mM
- 0.6521 mL
- 3.2603 mL
- 6.5205 mL
- 10 mM
- 0.3260 mL
- 1.6301 mL
- 3.2603 mL

技术信息

CAS号

243966-09-8

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C10H11ClN2O5S

运输

蓝冰

分子量

306.72

别名

溶解度

DMSO	64.0 mg/mL (208.7 mM)
Water	insoluble

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