PTP1B Inhibitor 抑制剤 (CAS 765317-72-4)

5.0(1)

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

アプリケーション： PTP1B Inhibitor is a cell-permeable allosteric inhibitor of the PTP1B (protein tyrosine phosphatase 1B) enzyme.

CAS 番号: 765317-72-4

Purity: ≥95%

Molecular Weight: 741.5

Molecular Formula: C₂₆H₁₉Br₂N₃O₇S₃

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* Refer to Certificate of Analysis for lot specific data (including water content).

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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

Physical State :

Solid

Solubility :

Soluble in DMSO, and ethanol.

保存方法 :

Store at -20° C

Boiling Point :

855° C at 760 mmHg

Density :

1.81 g/cm³

Refractive Index :

n²⁰_D 1.73

IC50 :

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

pK Values :

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

試験・研究用以外には使用しないでください。臨床及び体外診断には使用できません。

PubChem CID :

448662

MDL Number :

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

Download SDS (MSDS)

分析表

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