AGN 193109
Based on 10 publication(s) in Google Scholar
AGN 193109 is a retinoid analog, and acts as a specific and highly effective antagonist of retinoic acid receptors (RARs), with Kds of 2 nM, 2 nM, and 3 nM for RARα, RARβ, and RARγ, respectively. AGN 193109 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. AGN 193109 is the antidote for retinoic acidosis, that ameliorates the skin and mucosal toxicity.
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- Pureté: 99.80%
- CAS No.: 171746-21-7
- Formule: C28H24O2
- Masse moléculaire:392.49
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
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Publications Citing Use of MedChemExpress (MCE) AGN 193109
More- Cancer Res. 2023 Jul 14;83(14):2387-2404. [Abstract]
- Nat Commun. 2026 May 11. [Abstract]
- Redox Biol. 2024 Nov:77:103361. [Abstract]
- Cell Rep Med. 2026 Apr 21;7(4):102698. [Abstract]
- Sci Adv. 2020 Nov 4;6(45):eaaz1410. [Abstract]
- Cell Commun Signal. 2025 Mar 29;23(1):156. [Abstract]
- Allergy. 2022 Feb;77(2):483-498. [Abstract]
- Front Pharmacol. 2025 Apr 24:16:1562244. [Abstract]
- bioRxiv. 2024 Oct 23:2024.10.20.619300. [Abstract]
- Research Square Preprint. 2023 Nov 17.
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Cell Proliferation/Viability Assay
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Flow Cytometry
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In Vivo Imaging
Activité biologique
Kd: 2 nM (RARα), 2 nM (RARβ), 3 nM (RARγ)[1]
AGN 193109 is a highly effective antagonist of retinoic acid receptors, with Kds of 2 nM, 2 nM, and 3 nM for RARα, RARβ, and RARγ, respectively. AGN 193109 is completely RAR specific, because it does not bind to or transactivate through any of the RXRs[1]. AGN 193109 (100 nM) inhibits the TTNPB (a retinoic acid receptor agonist)-dependent morphological change in ECE16-1 cells. AGN193109 half-reverses retinoid-dependent growth suppression at 10 nM, and completely shows this effect at 100 nM in ECE16-1 cells. AGN193109 (100 nM) also eliminates TTNPB-induced decrease in levels of K5, K6, K14, K16, and K17 and increase in levels of K7, K8, and K19[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 171746-21-7
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Appearance Solid
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Masse moléculaire 392.49
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Formule C28H24O2
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Color White to light yellow
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SMILES
O=C(O)C1=CC=C(C#CC2=CC=C3C(C)(C)CC=C(C4=CC=C(C)C=C4)C3=C2)C=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 2 years -20°C 1 year
Publications (10)
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Journal Impact Factor
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Most Recent
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Cancer Res
Retinol saturase mediates retinoid metabolism to impair a ferroptosis defense system in cancer cells. [Abstract]2023 Jul 14;83(14):2387-2404. PMID: 37184371 -
Nat Commun
All-trans retinoic acid destabilizes ADAR1 protein through retinoylation-mediated USP7 dissociation and improves immunotherapy in pancreatic cancer. [Abstract]2026 May 11. PMID: 42115161 -
Redox Biol
2024 Nov:77:103361. PMID: 39317105
AGN 193109 purchased from MedChemExpress. Usage Cited in: Redox Biol. 2024 Nov:77:103361. [Abstract]
Relative viability shows retinoic acid receptor α (RARA) resisted KRAS G12C mutant cells to ferroptosis caused by RSL3, IKE, Sotorasib and Adagtasib (IC50), demonstrated by medications with RARA inhibitor AGN193109 (1000 nM; 72 h) for 72 h.
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Cell Rep Med
CAR-M2 immunotherapy resolves renal fibrosis via revascularization and apoptosis of profibrotic Cxcr2+ endothelial cells. [Abstract]2026 Apr 21;7(4):102698. PMID: 41887221 -
Sci Adv
Histone demethylase LSD1 is critical for endochondral ossification during bone fracture healing. [Abstract]2020 Nov 4;6(45):eaaz1410. PMID: 33148658
AGN 193109 purchased from MedChemExpress. Usage Cited in: Sci Adv. 2020 Nov 4;6(45):eaaz1410. [Abstract]
AGN 193109 (2 or 4 mg/kg; i.p.; every day, from 2 to 12 dpf). Reconstruction of μCT data reflects hard bony callus formation and Safranin O staining that shows cartilage formation of Lsd1Prx1 and control mice treated with AGN193109.
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Cell Commun Signal
Retinoic acid enhances γδ T cell cytotoxicity in nasopharyngeal carcinoma by reversing immune exhaustion. [Abstract]2025 Mar 29;23(1):156. PMID: 40158172 -
Allergy
The bile acid-activated retinoic acid response in dendritic cells is involved in food allergen sensitization. [Abstract]2022 Feb;77(2):483-498. PMID: 34365653 -
Front Pharmacol
Synergistic effects of retinol and retinyl palmitate in alleviating UVB-induced DNA damage and promoting the homologous recombination repair in keratinocytes. [Abstract]2025 Apr 24:16:1562244. PMID: 40343007 -
bioRxiv
All-trans retinoic acid-mediated ADAR1 degradation synergizes with PD-1 blockade to suppress pancreatic cancer. [Abstract]2024 Oct 23:2024.10.20.619300. PMID: 39484589 -
AGN 193109 purchased from MedChemExpress. Usage Cited in: Research Square Preprint. 2023 Nov 17.
BMDCs (5-7 days) cultured from RA reporter mice are exposed to SiO2 (100 μg/mL) and AM80 (20 μM) solely for 14 h, BMDCs are pretreated with AGN193109 (1 μM; 60 min) for 60 min, and then exposed to SiO2 (100 μg/mL) for 14 h and incubated with DDAOG (10 μM). DDAO fluorescence is analyzed by flow cytometry. Data are representative of three independent experiments.
Solvant et solubilité
DMSO : 2 mg/mL (5.10 mM; Need warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 5 mg/mL (12.74 mM); Suspended solution; Need ultrasonic
Add each solvent one by one: 15% Cremophor EL 85% Saline
Solubility: 12.5 mg/mL (31.85 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
Cells (10,000/cm2) are seeded in complete medium and allowed to attach overnight. The cells are then shifted to defined medium (DM), allowed to equilibrate for 24 h, and treatment is initiated by addition of fresh DM or DM containing epidermal growth factor (EGF) or retinoid. After 3 days of daily treatment with retinoid, the cells are harvested with 0.025% trypsin, 1 mM EDTA, fixed in isotonic buffer containing 4% formaldehyde, and counted using a counter[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice (n=6) are treated topically on the dorsal skin with vehicle (92.5% acetone/7.5% DMSO), 0.072 μmol/kg of TTNPB, 1.15 μmol/kg of AGN 193109, or 0.072 μmol/kg of TTNPB plus 0.072, 0.288, or 1.15 μmol/kg of AGN 193109 for 5 days. Mice are euthanized on Day 8[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (280 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Johnson AT, et al. Synthesis and characterization of a highly potent and effective antagonist of retinoic acid receptors. J Med Chem. 1995 Nov 24;38(24):4764-7. [Content Brief]
[2]. Agarwal C, et al. AGN193109 is a highly effective antagonist of retinoid action in human ectocervical epithelial cells. J Biol Chem. 1996 May 24;271(21):12209-12. [Content Brief]
[3]. Standeven AM, et al. Specific antagonist of retinoid toxicity in mice. Toxicol Appl Pharmacol. 1996 May;138(1):169-75. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5478 mL | 12.7392 mL | 25.4784 mL | 63.6959 mL |
| 5 mM | 0.5096 mL | 2.5478 mL | 5.0957 mL | 12.7392 mL |
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