AGN 192403
AGN 192403 (BRD4780) is a potent and selective imidazoline-1 receptor antagonist with a Ki value of 42 nM. AGN 192403 is also a TMED9 inhibitor. AGN 192403 shows protective effects on oxidative cytotoxicity and mitochondrial inhibitor-induced cytotoxicity in astrocytes. AGN 192403 mitigates the proliferation and migration of differentiated glioma tumor cells. AGN 192403 can be used for glioma tumor and neurological diseases research.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 175521-95-6
- 分子式: C10H19N
- 分子量:153.26
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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生物活性
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Caspase-9 |
imidazoline-1 receptor 42 nM (Ki) |
AGN 192403 (10-100 μM, 24 h) inhibits the former lysosomal destabilization and the subsequent decrease in mitochondrial potential in astrocytes exposed to Naphthazarin (HY-N7526)[1].
AGN 192403 (10-100 μM, 24 h) inhibits the Antimycin A- and Rotenone (HY-B1756)-induced decrease in mitochondrial potential, cytochrome c release, caspase-9 activation, and eventually LDH release in astrocytes[1].
AGN 192403 (4-25 μM, 14 days) exerts a remarkable inhibitory effect on glioma stem cells (GSC)s self-renewal, demonstrating almost complete inhibition of self-renewal at the highest concentration applied[2].
AGN 192403 (0-25 μM, 18-48 h) targets TMED9, reduces the stemness, reduces GSC migration, and inhibits GSC tumorigenic functions[2].
AGN 192403 (4-25 μM, 0-8 days) induces cell death in a dose dependent manner in patient-derived GSCs[2].
AGN 192403 (4-25 μM, 48 h-8 days) inhibits TMED9 and exerts anti-tumor effects in diffuse intrinsic pontine glioma (DIPG) cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:patient-derived GSCs
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Concentration:0, 4, 10, 25 μM
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Incubation Time:48 h
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Result:Decreased TMED9 expression in a dose-dependent manner in three different patient-derived GSCs.
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Cell Line:GSCs
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Concentration:10, 25 μM
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Incubation Time:48 h
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Result:Showed a marked and dose dependent reduction in SOX2 expression.
Markedly reduced YKL40 expression.
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Cell Line:GSCs
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Concentration:10, 25 μM
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Incubation Time:18-20 h
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Result:Dose-dependently reduced GSC migration.
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Cell Line:GSCs
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Concentration:4, 10, 25 μM
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Incubation Time:0, 1, 2, 3, 4, 5, 6, 7, 8 days
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Result:Resulted in a dose-dependent induction of cell death, at multiple points over the course of one week.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 175521-95-6
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分子量 153.26
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分子式 C10H19N
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SMILES
CC([C@H]1[C@@]2([H])C[C@@](CC2)([H])[C@@H]1N)C
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別名
(+)-BRD4780 free base
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Choi DH, et al. Protective effects of rilmenidine and AGN 192403 on oxidative cytotoxicity and mitochondrial inhibitor-induced cytotoxicity in astrocytes. Free Radic Biol Med. 2002 Nov 15;33(10):1321-33. [Content Brief]
[2]. Daoud Sarsour A, et al. Targeting the Cargo Receptor TMED9 as a Therapeutic Strategy Against Brain Tumors. Cells. 2025 May 23;14(11):772. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
AGN 192403 関連分類
HY-101374 関連分類
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