Date published: 2026-3-18

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PTP1B Inhibitor (CAS 765317-72-4)

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Alternate Names:
PTP1B Inhibitor is also known as Protein Tyrosine Phosphatase 1B Inhibitor.
Application:
PTP1B Inhibitor is a cell-permeable allosteric inhibitor of the PTP1B (protein tyrosine phosphatase 1B) enzyme.
CAS Number:
765317-72-4
Purity:
≥95%
Molecular Weight:
741.5
Molecular Formula:
C26H19Br2N3O7S3
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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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. 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. 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.


PTP1B Inhibitor (CAS 765317-72-4) References

  1. Acquisition of a specific and potent PTP1B inhibitor from a novel combinatorial library and screening procedure.  |  Shen, K., et al. 2001. J Biol Chem. 276: 47311-9. PMID: 11584002
  2. Hyrtiosal, a PTP1B inhibitor from the marine sponge Hyrtios erectus, shows extensive cellular effects on PI3K/AKT activation, glucose transport, and TGFbeta/Smad2 signaling.  |  Sun, T., et al. 2007. Chembiochem. 8: 187-93. PMID: 17183521
  3. PTP1B as a drug target: recent developments in PTP1B inhibitor discovery.  |  Zhang, S. and Zhang, ZY. 2007. Drug Discov Today. 12: 373-81. PMID: 17467573
  4. Discovery of a novel competitive inhibitor of PTP1B by high-throughput screening.  |  Shi, L., et al. 2008. Acta Pharmacol Sin. 29: 278-84. PMID: 18215359
  5. Molecular dynamics studies on the interactions of PTP1B with inhibitors: from the first phosphate-binding site to the second one.  |  Wang, JF., et al. 2009. Protein Eng Des Sel. 22: 349-55. PMID: 19380334
  6. Dammaranes from Gynostemma pentaphyllum and synthesis of their derivatives as inhibitors of protein tyrosine phosphatase 1B.  |  Xu, JQ., et al. 2010. Bioorg Med Chem. 18: 3934-9. PMID: 20472439
  7. Baculovirus expression system: an alternative for producing catalytically active human PTP-1B.  |  Sundaram, S., et al. 2010. Mol Biol (Mosk). 44: 535-40. PMID: 20608179
  8. Rhododendric acid A, a new ursane-type PTP1B inhibitor from the endangered plant Rhododendron brachycarpum G. Don.  |  Choi, YH., et al. 2012. Bioorg Med Chem Lett. 22: 6116-9. PMID: 22940448
  9. Unprecedented diterpenoids as a PTP1B inhibitor from the Hainan soft coral Sarcophyton trocheliophorum Marenzeller.  |  Liang, LF., et al. 2013. Org Lett. 15: 274-7. PMID: 23273218
  10. PTP1B-dependent regulation of receptor tyrosine kinase signaling by the actin-binding protein Mena.  |  Hughes, SK., et al. 2015. Mol Biol Cell. 26: 3867-78. PMID: 26337385
  11. PTP1B inhibitor promotes endothelial cell motility by activating the DOCK180/Rac1 pathway.  |  Wang, Y., et al. 2016. Sci Rep. 6: 24111. PMID: 27052191
  12. A novel PTP1B inhibitor extracted from Ganoderma lucidum ameliorates insulin resistance by regulating IRS1-GLUT4 cascades in the insulin signaling pathway.  |  Yang, Z., et al. 2018. Food Funct. 9: 397-406. PMID: 29215104
  13. PTP1B Inhibitor Claramine Rescues Diabetes-Induced Spatial Learning and Memory Impairment in Mice.  |  Wu, M., et al. 2023. Mol Neurobiol. 60: 524-544. PMID: 36319905

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

PTP1B Inhibitor, 5 mg

sc-222227
5 mg
$231.00

PTP1B Inhibitor, 25 mg

sc-222227A
25 mg
$936.00

What is the IC50 of this product? The website has two different numbers and I am not sure what they designate.

Asked by: SCchem16
Thank you for your question. This chemical, PTP1B Inhibitor: sc-222227, is a non-competitive allosteric inhibitor of PTP1B (IC50 = 4 µM and 8 µM for PTP1B403 and PTP1B298, respectively). There are two IC50 values because the inhibitory concentration was measured at two different (assumed) amino acids.
Answered by: Chemical Support 2
Date published: 2017-03-10

What is the half-life period of sc-222227?

Asked by: SCchem16
Thank you for your question. This chemical, PTP1B Inhibitor (CAS 765317-72-4), has a half-life of > 3 years if storage conditions are kept.
Answered by: Chemical Support 2
Date published: 2017-03-10
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Rated 5 out of 5 by from Inibitore allosterico della PTP1BIl prodotto è stato consegnato rapidamente; la confezione era integra e il prodotto ben conservato. In fase di prove sperimentali, il prodotto è risultato attivo e conforme alle aspettative.
Date published: 2023-02-06
Rated 5 out of 5 by from HughesHughes, SK. et al. (PubMed 26337385) report that Mena associates constitutively with the tyrosine phosphatase PTP1B and mediates a novel negative feedback mechanism that attenuates receptor tyrosine kinase signaling. They also found that disruption of this attenuation by MenaINV sensitizes tumor cells to low growth factor concentrations, thereby increasing the migration and invasion responses that contribute to aggressive, malignant cell phenotypes. -SCBT Publication Review
Date published: 2015-05-26
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PTP1B Inhibitor is rated 5.0 out of 5 by 2.
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