AGN 193109

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Cat.No. 5758 - AGN 193109 | C28H24O2 | CAS No. 171746-21-7
Description: High affinity pan-RAR antagonist
Chemical Name: 4-[2-[5,6-Dihydro-5,5-dimethyl-8-(4-methylphenyl)-2-naphthalenyl]ethynyl]benzoic acid
Purity: ≥98% (HPLC)
Citations (3)
Reviews (1)
Literature (3)

Biological Activity for AGN 193109

AGN 193109 is a high affinity pan-retinoic acid receptor (RAR) antagonist (Kd values are 2, 2 and 3 nM at RARα, RARβ and RARγ, respectively). Exhibits no significant affinity for retinoic X receptors.

AGN 193109 synthesized to Ancillary Material Grade also available.

Technical Data for AGN 193109

M. Wt 392.49
Formula C28H24O2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 171746-21-7
PubChem ID 177238
Smiles CC(CC=C1C2=CC=C(C)C=C2)(C)C(C1=C3)=CC=C3C#CC4=CC=C(C(O)=O)C=C4

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for AGN 193109

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 1.96 5 with gentle warming

Preparing Stock Solutions for AGN 193109

The following data is based on the product molecular weight 392.49. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.05 mM 50.96 mL 254.78 mL 509.57 mL
0.25 mM 10.19 mL 50.96 mL 101.91 mL
0.5 mM 5.1 mL 25.48 mL 50.96 mL
2.5 mM 1.02 mL 5.1 mL 10.19 mL

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Product Datasheets for AGN 193109

Certificate of Analysis / Product Datasheet
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References for AGN 193109

References are publications that support the biological activity of the product.

Agarwal et al (1996) AGN193109 is a highly effective antagonist of retinoid action in human ectocervical epithelial cells. J.Biol.Chem. 271 12209 PMID: 8647816

Levi et al (2015) Saturated fatty acids regulate retinoic acid signalling and suppress tumorigenesis by targeting fatty acid-binding protein 5 Nat.Commun. 6 8794 PMID: 26592976

Jaurena et al (2015) Zic1 controls placode progenitor formation non-cell autonomously by regulating retinoic acid production and transport. Nat.Commun. 6 7476 PMID: 26101153

If you know of a relevant reference for AGN 193109, please let us know.

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Keywords: AGN 193109, AGN 193109 supplier, AGN193109, high, affinity, selective, retinoic, acid, receptors, RAR, antagonists, antagonisms, Retinoic, Acid, Receptors, 5758, Tocris Bioscience

3 Citations for AGN 193109

Citations are publications that use Tocris products. Selected citations for AGN 193109 include:

Moreau et al (2019) Timed Collinear Activation of Hox Genes during Gastrulation Controls the Avian Forelimb Position. Curr Biol 29 35 PMID: 30554902

Blixt et al (2018) Zinc finger gene nolz1 regulates the formation of retinal progenitor cells and suppresses the Lim3/Lhx3 phenotype of retinal bipolar cells in chicken retina. Dev Dyn 247 630 PMID: 29139167

Jian et al (2018) Glycemic Variability Promotes Both Local Invasion and Metastatic Colonization by Pancreatic Ductal Adenocarcinoma. Cell Mol Gastroenterol Hepatol 6 429 PMID: 30258965

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Near complete ablation of RA-induced transcription in MCF7 cells.
By Anonymous on 11/02/2019
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: MCF7

AGN193109 was dissolved to a concentration of 20 mM in DMSO with no solubility issues. Retinoic acid (10 uM), DMSO, or RA + AGN193109 (1 uM) was added to MCF7 cells for 5 hours following by qPCR analysis of a reporter gene normalized to GAPDH levels. There was no apoptosis in MCF7 cells at 1 uM inhibitor for up to 9 hours even though this has been reported elsewhere. 1 uM of inhibitor almost completely ablated RA induced gene transcription by qPCR. HX531 performed slightly better in our analysis, but the experiment was only performed once.

No obvious apoptosis in cell lines treated with this inhibitor.

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