| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
RIPK1
Apostatin-1 targets TRADD, an adaptor protein that is a key mediator of TNFR1 (Tumor Necrosis Factor Receptor 1) signaling. TRADD regulates both cell survival and cell death pathways through its interactions with TRAF2, RIPK1, and other signaling molecules. Apostatin-1 binds to the N-terminal TRAF2-binding domain of TRADD (TRADD-N) with a KD of 2.17 μM, and disrupts the binding of TRADD to TRAF2. By inhibiting TRADD, Apostatin-1 blocks the recruitment of TRAF2 and the downstream activation of NF-κB and MAPK pathways. The compound also affects the ubiquitination of RIPK1 and beclin 1, modulating both apoptosis and autophagy. |
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| ln Vitro |
Apostatin-1 (Apt-1) is a TRADD inhibitor that affects the ubiquitination of RIPK1 and beclin 1 by interacting with the pocket on the N-terminal TRAF2 binding domain of TRADD (TRADD-N). In vitro, apostatin-1 successfully prevents bortezomib- and RIPK1-dependent apoptosis (RDA).[1]
In vitro, Apostatin-1 inhibits bortezomib-induced apoptosis and RIPK1-dependent apoptosis (RDA) with an IC50 of approximately 1 μM. The compound also inhibits TRADD-mediated signaling pathways, including the activation of NF-κB and MAPK pathways. Apostatin-1 affects the ubiquitination of RIPK1 and beclin 1, modulating both apoptosis and autophagy. The compound demonstrates cellular activity at micromolar concentrations, making it a useful tool for studying TRADD function in various cell types. Apostatin-1's ability to inhibit both apoptosis and autophagy highlights the complex role of TRADD in regulating cell fate decisions. |
| ln Vivo |
Apostatin-1 (Apt-1) (20 mg/kg, IP, once) prolongs the survival of mice with systemic inflammation by inhibiting inflammatory responses.
In vivo data for Apostatin-1 is limited in the available literature. The compound is primarily used as a research tool for in vitro studies of TRADD function. TRADD inhibition has been shown to affect cellular homeostasis and apoptosis in various experimental systems. The in vivo effects of Apostatin-1, including its pharmacokinetic properties and therapeutic potential, have not been extensively characterized. Apostatin-1's mechanism of action suggests potential applications in diseases where TRADD signaling is dysregulated, including cancer and inflammatory disorders. |
| Enzyme Assay |
Apostatin-1's binding to TRADD is assessed using biochemical binding assays. Surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC) are used to measure the binding affinity (KD) of Apostatin-1 for TRADD-N. Competition binding assays using labeled ligands may also be employed. These assays provide quantitative information on the interaction between Apostatin-1 and its target protein.
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| Cell Assay |
Velcade (50 nM) and Apt-1 (10 μM) were used to induce RIPK1-dependent apoptosis (RDA) in Jurkat cells, and the effects on cell viability were assessed after the treatment for 24 hours.MEFs were treated with mTNF (1 ng/mL) and 5Z-7- Oxozeaenol (0.5 μM), and Apt-1 was added at various concentrations for 8 hours.
In vitro, Apostatin-1 is tested on cultured cells to assess its effects on apoptosis and autophagy. Cells are treated with varying concentrations of Apostatin-1, with or without apoptotic stimuli such as bortezomib or TNFα. Apoptosis is assessed by flow cytometry using Annexin V staining, caspase activity assays, or PARP cleavage by Western blot. Autophagy is assessed by measuring LC3-II conversion, p62 levels, and autophagosome formation. Ubiquitination of RIPK1 and beclin 1 is assessed by immunoprecipitation followed by Western blot. These cell-based assays provide mechanistic insights into the activity of Apostatin-1. |
| Animal Protocol |
Animal studies for Apostatin-1 are limited in the available literature. The compound has not been extensively evaluated in vivo, and specific animal models, dosing regimens, and efficacy endpoints have not been reported. Apostatin-1 is primarily used as a research tool for in vitro studies. Further studies are needed to characterize the in vivo activity and therapeutic potential of Apostatin-1.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Apostatin-1 is not available in the literature. As a small molecule inhibitor, Apostatin-1 is expected to have properties suitable for cellular penetration, but its absorption, distribution, metabolism, and excretion have not been characterized. The compound is primarily used in research settings for in vitro studies.
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| Toxicity/Toxicokinetics |
Toxicological data for Apostatin-1 is not available in the literature. The compound is used in research settings and has not been evaluated for clinical safety. As a TRADD inhibitor, Apostatin-1 may affect cell survival and death pathways, and its toxicity profile would need to be characterized in future studies.
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| References | |
| Additional Infomation |
Apostatin-1 (Apt-1) is a novel TRADD inhibitor used as a research tool for studying apoptosis, autophagy, and cell survival pathways. TRADD is an adaptor protein that plays a critical role in TNFR1 signaling, regulating both cell survival and cell death. Apostatin-1 binds to the TRAF2-binding domain of TRADD, inhibiting its interaction with TRAF2 and downstream signaling. The compound inhibits bortezomib-induced apoptosis and RIPK1-dependent apoptosis, highlighting its potential as a tool for studying cell death mechanisms. Apostatin-1 is not approved as a therapeutic agent and is used for research purposes only. The compound's unique mechanism of action makes it a valuable tool for studying the role of TRADD in health and disease.
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| Molecular Formula |
C19H27N3OS
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| Molecular Weight |
345.5022
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| Exact Mass |
345.187
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| CAS # |
2559703-06-7
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| Related CAS # |
2559703-06-7
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| PubChem CID |
154824620
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| Appearance |
White to off-white solid
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| Density |
1.2±0.1 g/cm3
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| Index of Refraction |
1.630
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| LogP |
3.63
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
24
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| Complexity |
440
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C1=NC([H])([H])C([H])([H])N1C([H])([H])[H])C([H])(C1C([H])=C([H])C([H])=C([H])C=1[H])C(N([H])C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H])=O
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| InChi Key |
OXBMBNASDMMXSA-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
N-cycloheptyl-2-[(1-methyl-4,5-dihydroimidazol-2-yl)sulfanyl]-2-phenylacetamide
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| Synonyms |
Apt-1; Apostatin-1
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 69~83.3mg/mL (~199.7~241.2 mM)
Ethanol: ~9 mg/mL (~26.1 mM) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05954286 | Not yet recruiting | Drug: Upamostat Drug: Placebo (PO) |
SARS-CoV-2 | Henry M. Jackson Foundation for the Advancement of Military Medicine |
September 2023 | Phase 2 |
Products are for research use only; We do not sell to patients
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