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Submit ReviewAGN 193109
说明： High affinity pan-RAR antagonist
化学名： 4-[2-[5,6-Dihydro-5,5-dimethyl-8-(4-methylphenyl)-2-naphthalenyl]ethynyl]benzoic acid
纯度： ≥98% (HPLC)
生物活性 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 promotes the differentiation from mouse embryonic stem cells into paraxial mesoderm. AGN 193109 suppresses primary human cardiovascular smooth muscle cell calcification.
AGN 193109 synthesized to Ancillary Material Grade also available.
化合物库 for AGN 193109
AGN 193109 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for AGN 193109
| 分子量 | 392.49 |
| 公式 | C28H24O2 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 171746-21-7 |
| PubChem ID | 177238 |
| InChI Key | NCEQLLNVRRTCKJ-UHFFFAOYSA-N |
| Smiles | CC(CC=C1C2=CC=C(C)C=C2)(C)C(C1=C3)=CC=C3C#CC4=CC=C(C(O)=O)C=C4 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for AGN 193109
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 3.92 | 10 温和加热 |
制备储备液 for AGN 193109
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 25.48 mL | 127.39 mL | 254.78 mL |
| 0.5 mM | 5.1 mL | 25.48 mL | 50.96 mL |
| 1 mM | 2.55 mL | 12.74 mL | 25.48 mL |
| 5 mM | 0.51 mL | 2.55 mL | 5.1 mL |
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产品说明书 for AGN 193109
参考文献 for AGN 193109
参考文献是支持产品生物活性的出版物。
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
Russell et al (2018) Inverse agonism of retinoic acid receptors directs epiblast cells into the paraxial mesoderm lineage. Stem Cell Res. 30 85 PMID: 29807258
Rogers et al (2020) Retinoids repress human cardiovascular cell calcification with evidence for distinct selective retinoid modulator effects. Arterioscler.Thromb.Vasc.Biol. 40 656 PMID: 31852220
If you know of a relevant reference for AGN 193109, please let us know.
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关键词: AGN 193109, AGN 193109 supplier, AGN193109, high, affinity, selective, retinoic, acid, receptors, RAR, antagonists, antagonisms, differentiation, stem, cells, Retinoic, Acid, Receptors, Other, Differentiation, Products, Organoids, 5758, Tocris Bioscience
7 篇 AGN 193109 的引用文献
引用文献是使用了 Tocris 产品的出版物。 AGN 193109 的部分引用包括：
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
Chad A et al (2020) Fattening chips: hypertrophy, feeding, and fasting of human white adipocytes in vitro. Lab Chip 20 4152-4165 PMID: 33034335
Seungwoon et al (2020) CD137 Signaling Regulates Acute Colitis via RALDH2-Expressing CD11b-CD103+ DCs. Cell Rep 30 4124-4136.e5 PMID: 32209473
Gabriel et al (2021) Regulation of prefrontal patterning and connectivity by retinoic acid. Nature 598 483-488 PMID: 34599305
Marina et al (2019) ALDH3A1 Overexpression in Melanoma and Lung Tumors Drives Cancer Stem Cell Expansion, Impairing Immune Surveillance through Enhanced PD-L1 Output. Cancers (Basel) 11 PMID: 31817719
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
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AGN 193109 的评论
平均评分: 5 (Based on 1 Review.)
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Near complete ablation of RA-induced transcription in MCF7 cells.
By
Anonymous on 11/02/2019
分析类型： In Vitro
种属： Human
细胞系/组织： 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.
该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
Retinoid Receptors Scientific Review
Written by Alexander Moise, this review summarizes the nature of retinoid receptors, their isotype and isoform variants and modulation of retinoid signaling. Compounds available from Tocris are listed.