Benzeneacetamide, N-cycloheptyl-α-[(4,5-dihydro-1-methyl-1H-imidazol-2-yl)thio]-
- Product Name
- Benzeneacetamide, N-cycloheptyl-α-[(4,5-dihydro-1-methyl-1H-imidazol-2-yl)thio]-
- CAS No.
- 2559703-06-7
- Chemical Name
- Benzeneacetamide, N-cycloheptyl-α-[(4,5-dihydro-1-methyl-1H-imidazol-2-yl)thio]-
- Synonyms
- Apostain-1;Apostatin-1 ，S9705;Apostatin-1, 10 mM in DMSO;N-Cycloheptyl-2-((1-methyl-4,5-dihydro-1H-imidazol-2-yl)thio)-2-phenylacetamide;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;Apostatin 1,TRADD,Apostatin-1,Beclin1,RIPK,Autophagy,SH-SY5Y,Receptor-interacting protein kinases,Apoptosis,Apostatin1,HT-29,Jurkat cells,RIP kinase,inhibit,beclin 1,Inhibitor,Atg6,Apt1,Apt 1,Necroptosis,inflammatory responses,HeLa,RIPK1
- CBNumber
- CB39815026
- Molecular Formula
- C19H27N3OS
- Formula Weight
- 345.51
- MOL File
- 2559703-06-7.mol
Benzeneacetamide, N-cycloheptyl-α-[(4,5-dihydro-1-methyl-1H-imidazol-2-yl)thio]- Property
- 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)
- pka
- 13.99±0.20(Predicted)
- form
- Solid
- color
- White to off-white
- InChI
- InChI=1S/C19H27N3OS/c1-22-14-13-20-19(22)24-17(15-9-5-4-6-10-15)18(23)21-16-11-7-2-3-8-12-16/h4-6,9-10,16-17H,2-3,7-8,11-14H2,1H3,(H,21,23)
- InChIKey
- OXBMBNASDMMXSA-UHFFFAOYSA-N
- SMILES
- C(C1C=CC=CC=1)(C(=O)NC1CCCCCC1)SC1=NCCN1C
Safety
- WGK Germany
- WGK 3
- Storage Class
- 11 - Combustible Solids
N-Bromosuccinimide Price
- Product number
- SML3028
- Product name
- Apostatin-1
- Purity
- ≥98% (HPLC)
- Packaging
- 5 mg
- Price
- $111
- Updated
- 2026/03/19
- Product number
- SML3028
- Product name
- Apostatin-1
- Purity
- ≥98% (HPLC)
- Packaging
- 25 mg
- Price
- $356
- Updated
- 2026/03/19
Benzeneacetamide, N-cycloheptyl-α-[(4,5-dihydro-1-methyl-1H-imidazol-2-yl)thio]- Chemical Properties,Usage,Production
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.
Benzeneacetamide, N-cycloheptyl-α-[(4,5-dihydro-1-methyl-1H-imidazol-2-yl)thio]- Preparation Products And Raw materials
Raw materials
Preparation Products
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