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862808-01-3

862808-01-3 Structure

862808-01-3 Structure
IdentificationBack Directory
[Name]

3-(4-bromophenyl)-6-((4-(4-methoxyphenyl)piperazin-1-yl)methyl)thiazolo[2,3-c][1,2,4]triazole
[CAS]

862808-01-3
[Synonyms]

3-(4-bromophenyl)-6-((4-(4-methoxyphenyl)piperazin-1-yl)methyl)thiazolo[2,3-c][1,2,4]triazole
[Molecular Formula]

C22H22BrN5OS
[MDL Number]

MFCD05897677
[MOL File]

862808-01-3.mol
[Molecular Weight]

484.41
Chemical PropertiesBack Directory
[density ]

1.52±0.1 g/cm3(Predicted)
[solubility ]

DMF: 1 mg/ml; DMSO: Slightly soluble
[form ]

A crystalline solid
[pka]

6.56±0.10(Predicted)
[color ]

Off-white to light yellow
Hazard InformationBack Directory
[Description]

FSEN1 is an inhibitor of ferroptosis suppressor protein 1 (FSP1; IC50 = 313 nM).1 It is selective for FSP1 over NAD(P)H:quinone acceptor oxidoreductase 1 (NQO1; IC50 = >100 μM). FSEN1 induces cell death in GPX4-/- H460 non-small cell lung cancer (NSCLC) cells (EC50 = 69.36 nM) but not control H460 cells expressing Cas9 (H460Cas9). It sensitizes A549, Huh7, HCC1143, U2OS, SU-DHL-5, and T98G cancer cells to ferroptosis induced by (1S,3R)-RSL3 when used at concentrations ranging from 10 to 1,000 nM. FSEN1 also sensitizes H460Cas9 cells, but not FSP1-/- H460 cells, to cell death induced by the ferroptosis inhibitors dihydroartemisinin or FINO2 .
[Uses]

FSEN1 is a potent and non-competitive FSP1 inhibitor with an IC50 value of 313 nM. FSEN1 triggers iron death in cancer cells by inhibiting FSP1. FSEN1 can be used in research of cancer[1].
[References]

1. Hendricks, J.M., Doubravsky, C., Wehri, E., et al. Identification of structurally diverse FSP1 inhibitors that sensitize cancer cells to ferroptosis bioRxiv ,(2022).
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