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| 5mg |
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| Targets |
Biotinylated isoxazole targets RNA-binding proteins (RBPs) that constitute RNA granules, including stress granules and P-bodies. It precipitates hundreds of RNA-binding proteins with significant overlap to the constituents of RNA granules. Additionally, it has been reported to bind to ribosomal protein S6 kinase (RSK). The compound's mechanism involves the reversible aggregation of RNA granule-like structures, allowing the identification and study of proteins involved in RNA metabolism and cellular stress responses.
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| ln Vitro |
Biotinylated isoxazole demonstrates potent activity in precipitating RNA-binding proteins from cell and tissue lysates. In one study, approximately 580 proteins were precipitated by biotin-isoxazole, showing significant overlap with RNA granule components. The compound effectively induces the formation of aggregates associated with RNA granules in a reversible manner. It has been shown to inhibit protein synthesis in mammalian cells by targeting the RSK/4E-BP1 signaling axis. The compound's activity is concentration-dependent and is widely utilized as a tool for studying RNA-binding protein networks and granule dynamics.
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| ln Vivo |
In vivo activity data for biotinylated isoxazole is limited, as the compound is primarily utilized as a research tool for in vitro biochemical studies. However, it has been employed in tissue lysate-based assays to study RNA granule composition and dynamics. The compound's ability to reversibly aggregate and disaggregate RNA granule-like structures suggests potential for studying stress granule formation and clearance in cellular models. Further in vivo studies would be required to evaluate its pharmacokinetic properties and therapeutic potential.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for biotinylated isoxazole typically involve incubation of cell or tissue lysates with the biotinylated compound, followed by streptavidin pull-down to precipitate RNA-binding proteins. The precipitated proteins are then identified by mass spectrometry or Western blotting. The compound reversibly aggregates and disaggregates structures similar to RNA granules, allowing for the study of protein-RNA interactions. This assay format enables the identification of RNA granule components and the study of their dynamics under various cellular conditions.
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| Cell Assay |
In vitro cellular assays for biotinylated isoxazole involve treating cultured mammalian cells with the compound, followed by cell lysis and streptavidin pull-down to precipitate biotinylated protein complexes. The precipitated proteins are analyzed by mass spectrometry or immunoblotting to identify RNA-binding proteins. Additionally, the compound's effects on protein synthesis can be assessed by measuring phosphorylation of RSK and 4E-BP1 in treated cells. These assays are widely used to study RNA granule dynamics and RNA-protein interaction networks.
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| Animal Protocol |
In vivo animal experiments for biotinylated isoxazole are not extensively documented, as the compound is primarily employed as an in vitro research tool. If used in animal models, typical protocols would involve administration of the compound via intraperitoneal or intravenous injection, followed by tissue collection and analysis of RNA granule composition using streptavidin pull-down and mass spectrometry. The compound's reversible aggregation properties could be exploited to study stress granule dynamics in vivo.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for biotinylated isoxazole are not well characterized in the literature. As a biotinylated small molecule, its absorption, distribution, metabolism, and excretion properties would be influenced by the biotin moiety, which may facilitate binding to streptavidin and affect tissue distribution. The compound is typically used in in vitro settings, and its pharmacokinetic profile in vivo has not been systematically studied. Further investigations are needed to determine its systemic exposure, half-life, and bioavailability.
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| Toxicity/Toxicokinetics |
Toxicological data for biotinylated isoxazole are not well documented. As a research tool primarily used in in vitro biochemical assays, its safety profile in vivo has not been extensively characterized. The compound contains a biotin moiety, which is generally considered safe, but the isoxazole scaffold may contribute to cytotoxicity at higher concentrations. Standard laboratory safety precautions should be followed when handling this compound, including the use of personal protective equipment and proper waste disposal.
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| References |
[1]. Kato M, et, al. Cell-free formation of RNA granules: low complexity sequence domains form dynamic fibers within hydrogels. Cell. 2012 May 11;149(4):753-67.
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| Additional Infomation |
Biotinylated isoxazole (CAS#: 1377605-22-5) is a chemical probe used for studying RNA-binding proteins and RNA granules. Its molecular formula is C24H32N4O5S2. The compound precipitates hundreds of RNA-binding proteins with significant overlap to the constituents of RNA granules. It is not an approved therapeutic drug but rather a research tool for biochemical and cell biology applications. The compound is available from various chemical suppliers for research use only and is not intended for human therapeutic use.
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| Molecular Formula |
C24H32N4O5S2
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|---|---|
| Molecular Weight |
520.66468334198
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| Exact Mass |
520.181
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| CAS # |
1377605-22-5
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| PubChem CID |
97301453
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| Appearance |
White to off-white solid powder
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| Density |
1.251±0.06 g/cm3(Predicted)
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| Boiling Point |
800.4±65.0 °C(Predicted)
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| LogP |
3.2
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
15
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| Heavy Atom Count |
35
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| Complexity |
730
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| Defined Atom Stereocenter Count |
3
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| SMILES |
C1[C@H]2[C@@H]([C@@H](S1)CCCCC(=O)OCCCCCCNC(=O)C3=NOC(=C3)C4=CC=CS4)NC(=O)N2
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| InChi Key |
KZZXSHXZDYGEDW-XJABCFGWSA-N
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| InChi Code |
InChI=1S/C24H32N4O5S2/c29-21(10-4-3-8-20-22-17(15-35-20)26-24(31)27-22)32-12-6-2-1-5-11-25-23(30)16-14-18(33-28-16)19-9-7-13-34-19/h7,9,13-14,17,20,22H,1-6,8,10-12,15H2,(H,25,30)(H2,26,27,31)/t17-,20-,22-/m0/s1
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| Chemical Name |
6-[(5-thiophen-2-yl-1,2-oxazole-3-carbonyl)amino]hexyl 5-[(3aS,4S,6aR)-2-oxo-1,3,3a,4,6,6a-hexahydrothieno[3,4-d]imidazol-4-yl]pentanoate
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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 : 41.67 mg/mL (80.03 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 | 1.9206 mL | 9.6032 mL | 19.2064 mL | |
| 5 mM | 0.3841 mL | 1.9206 mL | 3.8413 mL | |
| 10 mM | 0.1921 mL | 0.9603 mL | 1.9206 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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