Target nature :
not known
CAS n° :
2243462-48-6
Mecanism of action :
disruption of the endoplasmic reticulum protein quality control requiring ERAD stress response independently of the canonical unfolded protein response (UPR)
Physico-chemical properties :
Molecular weight: 283.11 g.mol
Experimental solubility: PBS pH7.4: 1.0 ± 0.2 µM; PBS pH7.4 10% DMSO: 5.6 ± 0.7 µM; NaCl 9/1000 with 10% cremophor EL: 284 ± 5 µM; NaCl 9/1000 with 10% solutol HS15: 939 ± 5 µM;
Probe availability :
upon request
Princeps reference :
Raj, S et al. (2016) Antimicrobial Agents and Chemotherapy, 60 (3), 1438-1449, DOI:10.1128/AAC.02239-15
More bibliography :
NA
Other available information on the probe :
Compound identified through a chemical library screening for toxicity against Aspergillus fumigatus. The initial hit was a mixture of two isomers: isomer alpha (sr7575 or (E) 1-(2,4-Dichlorophenyl)-2-(2-nitrovinyl)-1H-pyrrole) and isomer ß ((E) 1-(2,4-Dichlorophenyl)-3-(2-nitrovinyl)-1H-pyrrole). The latter was found to have lost the ability to block the fungal growth.
Metabolic stability of sr7575 on human liver microsomes at 37°C: t1/2 = 37 ± 1 min
Other information on the target :
NA
Selectivity profile :
KINOMEscan (DiscoveRx) @ 10µM: 14 hits out of 451 kinases tested (S-score(35) = 0.03)
In vivo data :
Not evaluated
In vitro data :
Growth inhibitor of various fungi (A. fumigatus, A. flavus, Candida albicans, Cryptococcus neoformans and Saccharomyces cerevisiae) on plates and liquid media at concentrations ranging from 0.6 to 10 µg/mL.
Fungistatic effect.
Toxicity :
- CiToxLAB study report
Under the experimental conditions of this study, the test item, sr7575 did not show any mutagenic activity in the bacterial reverse mutation test with Salmonella typhimurium, in the absence or the presence of a rat metabolising system.
- No lethality observed after intraperitoneally injection of sr7575 (dose 100 mg/kg) in mice
Chaine SMILES :
O=N(=O)/C=C/c1cccn1c2ccc(Cl)cc2Cl
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