[CAS NO. 2559703-06-7] Apostatin-1
PRODUCTS SPECIFICATIONS [2559703-06-7]
DESCRIPTION [2559703-06-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 345.50 |
| Molecular Formula | C19H27N3OS |
| SMILES | O=C(NC1CCCCCC1)C(SC2=NCCN2C)C3=CC=CC=C3 |
Summary
Apostatin-1 (Apt-1) is a potent TRADD inhibitor. Apostatin-1 can bind with TRADD-N ( K D =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] .
In Vitro
Apostatin-1 inhibits Velcade (
Bortezomib
, HY-134050)-induced apoptosis and RIPK1-dependent apoptosis (RDA) and necroptosis, with an IC
50
of 0.97 μM
[1]
.
Apostatin-1 (10 μM, 6 h) effectively induces autophagy and the degradation of long-lived proteins
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis [1]
| Cell Line: | SH-SY5Y, HeLa, HT-29, and Jurkat cells |
| Concentration: | 10 μM |
| Incubation Time: | 6 h |
| Result: | Effectively induced autophagy by LC3 II induction and p62 reduction. |
In Vivo
Apostatin-1 (20 mg/kg, IP, once) inhibits inflammatory responses, and increases survival of systemic inflammation mouse model [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 83.33 mg/mL ( 241.19 mM ; ultrasonic and warming and adjust pH to 4 with HCl and heat to 80°C)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.8944 mL | 14.4718 mL | 28.9436 mL |
| 5 mM | 0.5789 mL | 2.8944 mL | 5.7887 mL |
| 10 mM | 0.2894 mL | 1.4472 mL | 2.8944 mL |