PTP1B Inhibitor 抑制剂 CAS: 765317-72-4
MF: C26H19Br2N3O7S3
MW: 741.5

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).

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 :
n20D 1.73
IC50 :
PTP1B403: IC50 = 4 µM; PTP1B298: IC50 = 8 µM
pK值 :
pKa: 4.47 (Predicted), pKb: 1.70 (Predicted)
仅供科研使用。不可用于诊断或治疗。
PubChem CID :
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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PMID: # 27016479  Chiba, T. et al. 2016. Biochemical and biophysical research communications. 473: 323-8.

PMID: # 27095436  Song, GJ. et al. 2016. J Neuroinflammation. 13: 86.

PMID: # 26453921  Zhang, H. et al. 2015. Free radical biology & medicine. 89: 701-7.

PMID: # 24519936  Shi, L. et al. 2014. The Journal of biological chemistry. 289: 8432-41.

PMID: # 22903352  Vota, DM. et al. 2013. Cell biochemistry and biophysics. 65: 145-57.

PMID: # 23951017  Zhang, J. et al. 2013. PloS one. 8: e70828.

PMID: # 29742155  PLoS Pathog. e1007054.

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