1. Apoptosis Autophagy
  2. RIP kinase Autophagy Apoptosis Beclin1 Necroptosis
  3. Apostatin-1

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.

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Apostatin-1 Chemical Structure

Apostatin-1 Chemical Structure

CAS No. : 2559703-06-7

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Description

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].

IC50 & Target

RIPK1

 

In Vitro

Apostatin-1 inhibits Velcade (Bortezomib, HY-134050)-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].

MedChemExpress (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].

MedChemExpress (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.
Molecular Weight

345.50

Formula

C19H27N3OS

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1CCCCCC1)C(SC2=NCCN2C)C3=CC=CC=C3

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
In Vitro: 

DMSO : 83.33 mg/mL (241.19 mM; ultrasonic and warming and adjust pH to 4 with HCl and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8944 mL 14.4718 mL 28.9436 mL 72.3589 mL
5 mM 0.5789 mL 2.8944 mL 5.7887 mL 14.4718 mL
10 mM 0.2894 mL 1.4472 mL 2.8944 mL 7.2359 mL
15 mM 0.1930 mL 0.9648 mL 1.9296 mL 4.8239 mL
20 mM 0.1447 mL 0.7236 mL 1.4472 mL 3.6179 mL
25 mM 0.1158 mL 0.5789 mL 1.1577 mL 2.8944 mL
30 mM 0.0965 mL 0.4824 mL 0.9648 mL 2.4120 mL
40 mM 0.0724 mL 0.3618 mL 0.7236 mL 1.8090 mL
50 mM 0.0579 mL 0.2894 mL 0.5789 mL 1.4472 mL
60 mM 0.0482 mL 0.2412 mL 0.4824 mL 1.2060 mL
80 mM 0.0362 mL 0.1809 mL 0.3618 mL 0.9045 mL
100 mM 0.0289 mL 0.1447 mL 0.2894 mL 0.7236 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Apostatin-1
Cat. No.:
HY-134050
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