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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- CAS No.: 175521-95-6
- 화학식: C10H19N
- 분자량:153.26
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Biological Activity
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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.
Chemical Information
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CAS No. 175521-95-6
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분자량 153.26
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화학식 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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Synonyms
(+)-BRD4780 free base
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AGN 192403 Related Classifications
HY-101374 Related Classifications
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