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

Available Options

Size :PriceQuantity 
25 mg$205.00
5 mg$60.00

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

 

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:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

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