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ER000444793

  Cat. No.:  DC20997   Featured
Chemical Structure
792957-74-5
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More than 5000 active chemicals with high quality for research!
Field of application
ER-000444793 is a potent, cyclophilin D-independent inhibitor of mitochondrial permeability transition pore (mPTP) with with IC50 of 2.8 uM.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 792957-74-5
Chemical Name: 1,2-Dihydro-2-oxo-N-[2-(phenylmethyl)phenyl]-4-quinolinecarboxamide
Synonyms: ER000444793;ER 000444793;ER-000444793
SMILES: O=C(NC1=C(CC2=CC=CC=C2)C=CC=C1)C(C3=CC=CC=C3N4)=CC4=O
Formula: C23H18N2O2
M.Wt: 354.409
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
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.
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: [1]. Briston T, et al. Identification of ER-000444793, a Cyclophilin D-independent inhibitor of mitochondrial permeability transition, using a high-throughput screen in cryopreserved mitochondria. Sci Rep. 2016 Nov 25;6:37798.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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