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ChemicalBook--->CAS DataBase List--->2559703-06-7

2559703-06-7

2559703-06-7 Structure

2559703-06-7 Structure
IdentificationBack Directory
[Name]

Benzeneacetamide, N-cycloheptyl-α-[(4,5-dihydro-1-methyl-1H-imidazol-2-yl)thio]-
[CAS]

2559703-06-7
[Synonyms]

Benzeneacetamide, N-cycloheptyl-α-[(4,5-dihydro-1-methyl-1H-imidazol-2-yl)thio]-
N-Cycloheptyl-2-[(1-methyl-4,5-dihydro-1H-imidazol-2-yl)sulfanyl]-2-phenylacetamide
[Molecular Formula]

C19H27N3OS
[MDL Number]

MFCD32899498
[MOL File]

2559703-06-7.mol
[Molecular Weight]

345.51
Chemical PropertiesBack Directory
[density ]

1.21±0.1 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

DMSO : 83.33 mg/mL (241.19 mM; ultrasonic and warming and adjust pH to 4 with HCl and heat to 80°C)
[form ]

Solid
[pka]

13.99±0.20(Predicted)
[color ]

White to off-white
Hazard InformationBack Directory
[Uses]

Apostatin-1 (Apt-1) is a potent TRADD inhibitor. Apostatin-1 can bind with TRADD-N (KD=2.17 μM), disrupting its binding to both TRADD-C and TRAF2. Apostatin-1 modulates the ubiquitination of RIPK1 and beclin 1. Apostatin-1 blocks apoptosis and restores cellular homeostasis by activating autophagy in cells with accumulated mutant tau, α-synuclein, or huntingtin[1].
[Biological Activity]

Apostatin-1 (Apt-1) is a potent TRADD inhibitor. Apostatin-1 can bind with TRADD-N (KD=2.17 μM), disrupting its binding to both TRADD-C and TRAF2. Apostatin-1 modulates the ubiquitination of RIPK1 and beclin 1. Apostatin-1 blocks apoptosis and restores cellular homeostasis by activating autophagy in cells with accumulated mutant tau, α-synuclein, or huntingtin[1]. Apostatin-1 inhibits Velcade (Bortezomib, 0)-induced apoptosis and RIPK1-dependent apoptosis (RDA) and necroptosis, with an IC50 of 0.97 μM[1].Apostatin-1 (10 μM, 6 h) effectively induces autophagy and the degradation of long-lived proteins[1]. Apostatin-1 (20 mg/kg, IP, once) inhibits inflammatory responses, and increases survival of systemic inflammation mouse model[1].
[in vivo]

Apostatin-1 (20 mg/kg, IP, once) inhibits inflammatory responses, and increases survival of systemic inflammation mouse model[1].

Animal Model:Wild-type mice (n = 10, male, 8 weeks of age, systemic inflammation mouse model)[1]
Dosage:20 mg/kg
Administration:IP, once
Result:Reduced expression of the TNF-induced inflammatory target gene products, NOS and COXII27, and of inflammatory cytokines in cells stimulated with pathogen-associated molecular patterns, including interferon γ (IFNγ), lipopolysaccharide (LPS), Pam3CSK4 (a synthetic bacterial lipopeptide), and muramyl dipeptide (MDP). Showed increased survival following intravenous delivery of TNF, a mouse model of systemic inflammation.
[IC 50]

RIPK1
[References]

[1]. Xu D, et al. Modulating TRADD to restore cellular homeostasis and inhibit apoptosis. Nature. 2020 Nov;587(7832):133-138.
Spectrum DetailBack Directory
[Spectrum Detail]

Benzeneacetamide, N-cycloheptyl-α-[(4,5-dihydro-1-methyl-1H-imidazol-2-yl)thio]-(2559703-06-7)1HNMR
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