| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
STAMBP-IN-1 targets STAMBP (signal-transducing adaptor molecule-binding protein), a deubiquitinating enzyme. It interrupts the interaction between STAMBP and ubiquitinated NALP7 (STAMBP-Ub-NALP7). By inhibiting STAMBP, the compound reduces the protein level of NALP7, an inflammasome substrate, and suppresses the release of the pro-inflammatory cytokine IL-1β after TLR stimulation.
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| ln Vitro |
STAMBP-IN-1 (0.1-10 μM; 6 h) shows the most capacity to reduce endogenous NALP7 abundance in THP-1 cells and to specifically reduce NALP7 abundance, but not NALP6[1]. The cleavage of K63-linked di-Ub (200 nM) to mono-Ub by pure recombinant STAMBP (25 nM) is inhibited by STAMBP-IN-1 (0.01 -100 μM; 37 °C; 2 h) in a concentration-dependent manner[1]. In vitro, STAMBP-IN-1 (0.01-0.10 μM; 37 ℃; 60 min) inhibits the concentration-dependent deubiquitination of Ub-NALP7 mediated by STAMBP[1]. STAMBP-IN-1 has an IC50 of 106 μg/mL and is toxic to THP-1 cells[1].
In vitro, STAMBP-IN-1 inhibits the deubiquitinase activity of STAMBP. It decreases the protein level of NALP7 and suppresses IL-1β release after Toll-like receptor (TLR) stimulation. These effects have been demonstrated in cell-based assays, confirming its mechanism of action as a STAMBP inhibitor. |
| ln Vivo |
In vivo data for STAMBP-IN-1 are limited. As a STAMBP inhibitor, it is expected to have potential for treating inflammatory diseases. However, specific in vivo studies have not been detailed in the available literature. Further research is needed to evaluate its efficacy and safety in animal models.
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| Enzyme Assay |
The in vitro assay for STAMBP-IN-1 typically involves measuring its ability to inhibit STAMBP deubiquitinase activity. This can be done using a biochemical assay with recombinant STAMBP and a ubiquitinated substrate. The compound's ability to interrupt the STAMBP-Ub-NALP7 interaction is assessed using co-immunoprecipitation or proximity ligation assays.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: THP-1 cells Tested Concentrations: 0.01, 0.1, 1, 10, and 100 μM Incubation Duration: 6 hrs (hours) Experimental Results: Inhibited the activity of STAMBP to cleave recombinant di-Ub in a concentrationdependent manner with an IC50 of 0.33 mM (0.09-1.21 mM). Cellular assays for STAMBP-IN-1 are performed using cells that express STAMBP and NALP7. Cells are treated with the compound, and the protein level of NALP7 is measured by Western blotting. IL-1β release is measured by ELISA after TLR stimulation. These assays confirm its activity. |
| Animal Protocol |
In vivo animal protocols for STAMBP-IN-1 are not available in the literature. As a STAMBP inhibitor, it would typically be evaluated in mouse models of inflammation or cancer. However, such studies have not been reported. The compound is currently used primarily for in vitro research.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of STAMBP-IN-1 have not been characterized. It is a small molecule with a molecular weight of 504.60. The compound is typically dissolved in DMSO for in vitro studies. Further studies are needed to determine its ADME profile.
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| Toxicity/Toxicokinetics |
Toxicity data for STAMBP-IN-1 are limited. As a STAMBP inhibitor, it may have effects on immune function. The compound is intended for research use only and is not approved for human therapeutic use. Comprehensive toxicological studies are needed.
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| References | |
| Additional Infomation |
STAMBP-IN-1 is a small-molecule inhibitor of STAMBP deubiquitinase. It interrupts the STAMBP-Ub-NALP7 interaction and suppresses IL-1β release. The compound is used as a research tool for studying inflammasome biology and is not currently in clinical trials.
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| Molecular Formula |
C27H32N4O4S
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|---|---|
| Molecular Weight |
508.6324
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| Exact Mass |
504.183
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| CAS # |
896683-78-6
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| PubChem CID |
3293286
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| Appearance |
White to light yellow solid powder
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| LogP |
3.5
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
36
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| Complexity |
784
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C([H])([H])C(N([H])C([H])([H])[C@@]1([H])C([H])([H])C([H])([H])C([H])([H])O1)=O)C1=NC2C([H])=C([H])C(=C([H])C=2C(N1C([H])([H])C([H])([H])C1C([H])=C([H])C([H])=C([H])C=1[H])=O)N1C([H])([H])C([H])([H])OC([H])([H])C1([H])[H]
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| InChi Key |
HBAWGWWMULJGHR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H28N4O4S/c32-25(28-18-22-7-4-14-35-22)19-36-27-29-24-9-8-21(30-12-15-34-16-13-30)17-23(24)26(33)31(27)11-10-20-5-2-1-3-6-20/h1-9,14,17H,10-13,15-16,18-19H2,(H,28,32)
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| Chemical Name |
N-(furan-2-ylmethyl)-2-[6-morpholin-4-yl-4-oxo-3-(2-phenylethyl)quinazolin-2-yl]sulfanylacetamide
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : 3.29 mg/mL (6.52 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 | 1.9661 mL | 9.8303 mL | 19.6607 mL | |
| 5 mM | 0.3932 mL | 1.9661 mL | 3.9321 mL | |
| 10 mM | 0.1966 mL | 0.9830 mL | 1.9661 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.
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