792957-74-5
792957-74-5 structure
- Name: ER-000444793
- Chemical Name: ER-000444793
- CAS Number: 792957-74-5
- Molecular Formula: C23H18N2O2
- Molecular Weight: 354.4
- Catalog: Signaling Pathways Metabolic Enzyme/Protease Mitochondrial Metabolism
- Create Date: 2018-03-23 17:41:22
- Modify Date: 2024-01-29 14:10:17
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ER-000444793 is a potent inhibitor of mitochondrial permeability transition pore (mPTP) opening. ER-000444793 inhibits mPTP with an IC50 of 2.8 μM.
| Name | ER-000444793 |
|---|
| Description | ER-000444793 is a potent inhibitor of mitochondrial permeability transition pore (mPTP) opening. ER-000444793 inhibits mPTP with an IC50 of 2.8 μM. |
|---|---|
| Related Catalog | |
| Target |
IC50: 2.8 μM (mPTP)[1] |
| In Vitro | ER-000444793 is a small molecule, non-toxic mPTP inhibitor with a mechanism of action independent of CypD inhibition. ER-000444793 potently and dose-dependently inhibits Ca2+-induced mPT. ER-000444793 binds CypD, a CsA/CypD homogenous time-resolved fluorescence (HTRF) assay is used to study compound binding. Both CsA and SfA dose-dependently decrease HTRF signal, suggesting displacement of labelled CsA from rhCypD protein (CsA IC50=23 nM and SfA IC50= 5 nM). In contrast, ER-000444793 has no effect up to a concentration of 50 μM, indicating lack of displacement of labelled-CsA from rhCypD protein. Together, these data suggest the mechanism of ER-000444793 in delaying mPT is independent of CypD functional inhibition[1]. |
| Cell Assay | NFAT-RE-luc2 Jurkat cells are collected, centrifuged at 300 g for 5 minutes and re-suspended in serum-free RPMI-1640 media, plus supplements without antibiotic. Cell suspension (15,000 cells/20 μL) is added to each well of a solid black 384 well plate and incubated in the presence of compound for 20 hours at 37 °C. Alamar Blue is used and is added to each well at 2x concentration in media and reaction allowed to proceed for 4 hours at 37 °C. Fluorescence (ex. 540 nm/em. 590 nm) is recorded using Pherastar FS[1]. |
| References |
| Molecular Formula | C23H18N2O2 |
|---|---|
| Molecular Weight | 354.4 |
| Storage condition | 2-8℃ |