| Identification | Back Directory | [Name]
4-Imidazolidinone, 5-[(7-chloro-1H-indol-3-yl)methyl]-3-methyl-2-thioxo- | [CAS]
862377-51-3 | [Synonyms]
4-Imidazolidinone, 5-[(7-chloro-1H-indol-3-yl)methyl]-3-methyl-2-thioxo- | [Molecular Formula]
C13H12ClN3OS | [MOL File]
862377-51-3.mol | [Molecular Weight]
293.77 |
| Chemical Properties | Back Directory | [storage temp. ]
-20°C | [solubility ]
DMF: 20 mg/ml,DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml,DMSO: 14 mg/ml,Ethanol: 3 mg/ml | [form ]
A crystalline solid |
| Hazard Information | Back Directory | [Biological Activity]
Cl-Necrostatin-1 is an inhibitor of receptor-interacting protein kinase 1 (RIPK1).1 It inhibits RIPK1 activity when used at concentrations of 0.3, 3, and 30 μM. It also inhibits TNF-α-induced necroptosis in Jurkat cells deficient in Fas-associated death domain protein (FADD; EC50 = 180 nM), a modification that prevents caspase activation in response to death-domain receptor signaling.2,3 Cl-Necrostatin-1 (2 μl of a 4 mM solution, i.c.v.) reduces infarct size when administered pre- and post-occlusion, or post-occlusion only, in a mouse model of middle cerebral artery occlusion (MCAO). | [References]
1.Degterev, A., Hitomi, J., Germscheid, M., et al.Identification of RIP1 kinase as a specific cellular target of necrostatinsNat. Chem. Biol.4(5)313-321(2008)
2.Teng, X., Degterev, A., Jagtap, P., et al.Structure-activity relationship study of novel necroptosis inhibitorsBioorg. Med. Chem. Lett.15(22)5039-5044(2005)
3.Degterev, A., Huang, Z., Boyce, M., et al.Chemical inhibitor of nonapoptotic cell death with therapeutic potential for ischemic brain injuryNat. Chem. Biol.1(2)112-119(2005)
|
|
|