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7-Cl-O-Nec1 | RIP1 inhibitor

CAS:
852391-15-2
Catalog Number:
10-4544
Activity:
RIP1 inhibitor
Alternate Names:
Nec-1s
Chemical Name:
5-((7-Chloro-1H-indol-3-yl)methyl)-3-methylimidazolidine-2,4-dione
Molecular Weight:
277.71
Molecular Formula:
C13H12ClN3O2
Solubility:
Soluble in DMSO (up to 25 mg/ml).
Physical Properties:
Off-white solid
Purity:
>98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
Shipping Code:
RT

7-Cl-O-Nec1 (852391-15-2) is a necrostatin-1 (Cat.# 10-1162) analogue with superior potency (IC50 = 206nM vs 494nM), selectivity and metabolic stability in blocking RIP1.1,2 7-Cl-O-Nec1 shows no off-target inhibition of indolamine-2,3-deoxygenase (IDO) in contrast to Necrostatin-1 (Nec-1).3,4 7-Cl-O-Nec1 showed higher activity in inhibiting necroptosis in Jurkat cells than Necrostatin-1 (EC50 = 210 nM vs. EC50 = 490 nM), no non-specific cytotoxicity at high concentrations (100 μM) and reasonable pharmacokinetic characteristics when used in mice.2 7-Cl-O-Nec1 is recommended for cellular and in vivo use over Necrostatin-1.5

References/Citations:

1) Degterev et al. (2005) Chemical inhibitor of nonapoptotic cell death with therapeutic potential for ischemic brain injury; Nat. Chem. Biol., 1 112
2) Teng et al. (2005) Structure-activity relationship of novel necroptosis inhibitors; Bioorg. Med. Chem. Lett., 15 5039
3) Degterev et al. (2012) Activity and specificity of necrostatin-1, small-molecule inhibitor of RIP1 kinase; Cell Death Differ., 20 366
4) Takahashi et al. (2012) Necrostatin-1 analogues: critical issues on the specificity, activity and in vivo use in experimental disease models; Cell Death Dis., 3 e437
5) Degterev et al. (2013) Addendum: Chemical inhibitor of nonapoptotic cell death with therapeutic potential for ischemic brain injury; Nat. Chem. Biol., 9 192

 

7-Cl-O-Nec1 | RIP1 inhibitor is also available in the Cellular Metabolism Library.
CAS:
852391-15-2
Catalog Number:
10-4544
Activity:
RIP1 inhibitor
Alternate Names:
Nec-1s
Chemical Name:
5-((7-Chloro-1H-indol-3-yl)methyl)-3-methylimidazolidine-2,4-dione
Molecular Weight:
277.71
Molecular Formula:
C13H12ClN3O2
Solubility:
Soluble in DMSO (up to 25 mg/ml).
Physical Properties:
Off-white solid
Purity:
>98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

Product Data Sheet:

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