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IPAG

  Cat. No.:  DC11545   Featured
Chemical Structure
193527-91-2
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More than 5000 active chemicals with high quality for research!
Field of application
IPAG is a prototypic selective inhibitor of sigma1 receptor that engages the unfolded protein response and induces autophagy in cancer cells.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 193527-91-2
Chemical Name: 1-(4-Iodophenyl)-3-(2-adamantyl)guanidine
SMILES: N(C1=CC=C(I)C=C1)C(=N)NC1C2CC3CC1CC(C3)C2
Formula: C17H22In3
M.Wt: 395.29
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: [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.
Description: IPAG is a prototypic selective inhibitor of sigma1 receptor that engages the unfolded protein response and induces autophagy in cancer cells.
In Vivo: 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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC73507 WLB-89462 WLB-89462 (WLB89462) is a potent, highly selective sigma-2 receptor (σ2R) ligand with Ki of 13 nM, >100-fold selective over σ1R (Ki=1777 nM).
DC73504 JR1-157 JR1-157 is a potent selective sigma 2 receptor (σ2R) ligand with Ki value of 47 nM, >10-fold selectivity over σ1R.
DC48913 CM398 CM398 is a highly selective, orally active sigma-2 receptor ligand (Ki=0.43 nM), with high sigma-1/sigma-2 selectivity rato (1000-fold). CM398 shows notable affinity for dopamine (Ki=32.90 nM) and serotonin transporters (Ki=244.2 nM). CM398 shows promising anti-inflammatory analgesic effects in the formalin model of inflammatory pain in mice.
DC46854 BMY-14802 hydrochloride BMY-14802 hydrochloride (BMY-14802-1) is a selective and orally active sigma receptor antagonist with an IC50 of 112 nM. BMY-14802 hydrochloride is also a 5-HT1A and adrenergic α1 receptors agonist. BMY-14802 hydrochloride has antipsychotic effects.
DC42317 EST64454 hydrochloride EST64454 hydrochloride is a selective and orally active sigma-1 receptor antagonist with a Ki of 22 nM. EST64454 hydrochloride has the potential for the research of the pain.
DC11545 IPAG IPAG is a prototypic selective inhibitor of sigma1 receptor that engages the unfolded protein response and induces autophagy in cancer cells.
DC11758 PB 28 dihydrochloride A potent, mixed sigma2 agonist and sigma1 antagonist with Ki of 0.28 and 13.0 nM, respectively.
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