PTP1B Inhibitor 抑制剂 (CAS 765317-72-4)

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备用名: PTP1B Inhibitor is also known as Protein Tyrosine Phosphatase 1B Inhibitor.

应用； PTP1B Inhibitor is a cell-permeable allosteric inhibitor of the PTP1B (protein tyrosine phosphatase 1B) enzyme.

CAS号码: 765317-72-4

纯度: ≥95%

分子量: 741.5

分子式: C₂₆H₁₉Br₂N₃O₇S₃

仅供科研使用。不可用于诊断或治疗。

* 参考分析证明大量特定数据 (包括水含量).

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PTP1B Inhibitor blocks the activity of the Protein Tyrosine Phosphatase 1B, which is a key factor in the negative regulation of insulin and leptin signaling pathway. Molecular dynamic studies have shown that PTP1B Inhibitor has strong binding and high selectivity due to the hydrogen bonding networks formed around the active sites. Cytotoxicity and low revival rates throughout clone generation and maintence result if PTP1B is over-expressed in CHO and HEK293 stable cell clones. Studies have shown that PTP1B Inhibitor could dramatically magnify the membrane translocation of the key glucose transporter Glut4 in PTP1B-overexpressed CHO cells. PTP1B Inhibitor selectively increases the phosphorylation of the insulin receptor, insulin receptor substrate 1, and Akt, mimicking the action of insulin. PTP1B Inhibitor is also known as Protein Tyrosine Phosphatase 1B Inhibitor, and 3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethyl-N-[4-[(2-thiazolylamino)sulfonyl]phenyl]-6-benzofuransulfonamide.

参考文献

1. Sun, T., et al. 2007. Chembiochem. 8: 187-193. PMID: 17183521

2. Wang, J.F., et al. 2009. Protein Eng. Des. Sel. 22: 349-355. PMID: 19380334

3. Xu, J.Q., et al. 2010. Bioorg. Med. Chem. 18: 3934-3939. PMID: 20472439

4. Sundaram, S., et al. 2010. Mol. Biol. 44: 535-540. PMID: 20608179

5. Hughes, S.K. et al. 2015. Mol. Biol. Cell. 26(21): 3867-3878. PMID: 26337385

物理状态 :

Solid

溶解度 :

Soluble in DMSO, and ethanol.

保存 :

Store at -20° C

沸点 :

855° C at 760 mmHg

密度 :

1.81 g/cm³

折射率 :

n²⁰_D 1.73

IC50 :

PTP1B403: IC₅₀ = 4 µM; PTP1B298: IC₅₀ = 8 µM

pK值 :

pK_a: 4.47 (Predicted), pK_b: 1.70 (Predicted)

仅供科研使用。不可用于诊断或治疗。

PubChem CID :

448662

MDL 号码 :

MFCD09037556

SMILES :

CCC1=C(C2=C(O1)C=C(C=C2)S(=O)(=O)NC3=CC=C(C=C3)S(=O)(=O)NC4=NC=CS4)C(=O)C5=CC(=C(C(=C5)Br)O)Br

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