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193527-91-2

193527-91-2 structure
193527-91-2 structure
  • Name: IPAG
  • Chemical Name: 1-(4-iodophenyl)-3-(2-adamantyl)guanidine
  • CAS Number: 193527-91-2
  • Molecular Formula: C17H22IN3
  • Molecular Weight: 395.28
  • Catalog: Signaling Pathways GPCR/G Protein Sigma Receptor
  • Create Date: 2016-01-14 13:25:18
  • Modify Date: 2024-01-09 13:58:52
  • IPAG is a potent sigma-1 receptor antagonist with a pKi of 4.3[1]. IPAG induces apoptosis[2].

Name 1-(4-iodophenyl)-3-(2-adamantyl)guanidine
Synonyms ipag
Description IPAG is a potent sigma-1 receptor antagonist with a pKi of 4.3[1]. IPAG induces apoptosis[2].
Related Catalog
In Vitro Sigma1 inhibition by IPAG causes the autolysosomal degradation of PD-L1 in PC3 (hormone-insensitive prostate cancer) and MDA-MB-231 (triple-negative breast cancer) cell lines and reduces the levels of functional PD-L1 on the surface of the cells[2]. IPAG treatment produces a mean of 100±8 μg per 106 cells. IPAG can inhibit cell proliferation. Treatment with IPAG decreases cell mass[3]. IPAG treatment suppresses phosphorylation of translational regulator proteins p70S6K, S6, and 4E-BP1[3]. Cell Viability Assay[3] Cell Line: T47D cells Concentration: 10 μM Incubation Time: 24 hours Result: The mean forward scatter height (FSC-H) of DMSO (control) measured 412±5, whereas the mean FSC-H of IPAG treated cells was 390±4. Western Blot Analysis[3] Cell Line: T47D cells Concentration: 10 μM Incubation Time: Result: Decreased levels of phospho-threonine 389-p70S6Kinase (P-S6K), phospho-serine 235/236-ribosomal S6 (P-S6), and phospho-serine 65-4E-BP1 (P-4E-BP1).
References

[1]. James M Brimson, et al. Simple ammonium salts acting on sigma-1 receptors yield potential treatments for cancer and depression. Sci Rep. 2020 Jun 8;10(1):9251.

[2]. Halley M Oyer, et al.Small-Molecule Modulators of Sigma1 and Sigma2/TMEM97 in the Context of Cancer: Foundational Concepts and Emerging Themes. Front Pharmacol. 2019 Oct 21;10:1141.

[3]. Felix J Kim, et al. Inhibition of tumor cell growth by Sigma1 ligand mediated translational repression. Biochem Biophys Res Commun. 2012 Sep 21;426(2):177-82.

Molecular Formula C17H22IN3
Molecular Weight 395.28
Exact Mass 395.08600
PSA 47.91000
LogP 4.61580
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