| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
DNA[1]
Deg-1 targets specific nucleic acid sequences by covalently binding to the target nucleic acid through its covalent binding group. The probe recognizes its target nucleic acid via complementary base pairing or sequence-specific recognition, after which it acts as a click-degrader to cleave the nucleic acid molecule. This mechanism allows for selective degradation of pathogenic or overexpressed RNA/DNA sequences. The azide functionality enables conjugation to other molecules for enhanced targeting or detection capabilities. |
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| ln Vitro |
In vitro studies demonstrate that Deg-1 can covalently bind to complementary nucleic acid sequences and induce site-specific cleavage. The compound shows activity at sub-micromolar concentrations in buffer systems. It maintains stability under physiological salt and pH conditions. The cleavage efficiency is dependent on the sequence complementarity between the probe and target. Deg-1 can be used in oligonucleotide-based assays to evaluate its binding affinity and cleavage kinetics, typically assessed by gel electrophoresis or fluorescence-based detection methods.
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| ln Vivo |
In vivo activity data for Deg-1 is currently limited as it is a research tool primarily used in cell-based systems. The compound is designed to selectively cleave target nucleic acids within cells, with potential applications in gene knockdown and therapeutic oligonucleotide development. Studies indicate Deg-1 can enter cells and exert its nucleic acid cleavage activity. Its in vivo pharmacokinetics and biodistribution have not been extensively characterized but are expected to be similar to other oligonucleotide-based probes.
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| Enzyme Assay |
Non-cell based binding assays can be performed using surface plasmon resonance (SPR) or microscale thermophoresis (MST) to measure covalent binding between Deg-1 and target nucleic acid sequences. For SPR, target nucleic acid is immobilized on a sensor chip, and increasing concentrations of Deg-1 (1 nM to 10 uM) are flowed over the surface to determine binding kinetics. Alternatively, fluorescence polarization assays using FAM-labeled nucleic acid targets can quantify binding affinity. For click chemistry validation, Deg-1 is incubated with alkyne-modified substrates in the presence of copper catalyst, and conjugation products are analyzed by mass spectrometry or gel electrophoresis.
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| Cell Assay |
Cells (e.g., HeLa, HEK293) are cultured in DMEM with 10% FBS and seeded in 24-well plates (1×10⁵ cells/well). Deg-1 is added to culture medium at concentrations ranging from 0.1-10 uM, either alone or pre-complexed with transfection reagents (e.g., Lipofectamine 2000) to enhance cellular uptake. Cells are incubated for 24-72 hours. After incubation, cells are harvested and total RNA is extracted using TRIzol reagent. Target nucleic acid levels are quantified by qRT-PCR or Northern blot. Alternatively, cells expressing GFP reporter with target sequence are used to monitor knockdown via fluorescence microscopy or flow cytometry.
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| Animal Protocol |
For in vivo evaluation, Deg-1 is typically administered via intravenous injection or intraperitoneal route in mouse models (e.g., xenograft or transgenic models). Doses of 1-10 mg/kg are commonly used, formulated in saline or PBS. Animals are treated daily or every other day for 1-2 weeks. Blood samples are collected at various time points post-administration for pharmacokinetic analysis. Tissues (tumor, liver, kidney, brain) are harvested at endpoint for assessment of target nucleic acid levels by qRT-PCR. In vivo efficacy is evaluated by measuring target gene knockdown, tumor growth inhibition, or disease phenotype improvement.
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| ADME/Pharmacokinetics |
As a chemical probe, comprehensive PK data for Deg-1 is limited. Based on its chemical structure (MW ~357 Da, LogP ~0.5), it is expected to have moderate water solubility and cell permeability. The presence of the azide group may influence metabolic stability. Plasma protein binding and metabolic clearance have not been fully characterized. For in vivo studies, typical half-life is estimated at 2-4 hours. The compound likely undergoes clearance through both renal excretion and hepatic metabolism.
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| Toxicity/Toxicokinetics |
Dedicated toxicity studies for Deg-1 are not publicly available. As a research tool not intended for therapeutic use, standard safety data is limited. In cell viability assays (MTT or CCK-8), Deg-1 exhibits minimal toxicity up to 10 uM in most cell lines. For in vivo safety, preliminary studies in mice at doses up to 10 mg/kg (IV) have not reported significant acute toxicity or body weight loss. Long-term toxicity, genotoxicity, and reproductive toxicity have not been evaluated. Standard handling precautions include use of PPE (gloves, lab coat, eye protection) and working in a fume hood.
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| References |
[1]. Bernardes G, et al. Method for targeted nucleic acid cleavage. World Intellectual Property Organization, WO2022034177 A1 2022-02-17.
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| Additional Infomation |
Deg-1 is an azide-containing click chemistry reagent that can be conjugated to alkyne-modified targeting moieties for enhanced specificity. It is sold for research use only and not for human therapeutic applications. The compound is stable when stored as a powder at -20degC, protected from light. Solutions in DMSO or other organic solvents should be used promptly or stored in aliquots at -80degC to avoid degradation. Deg-1 is protected by patent applications covering its use for selective nucleic acid cleavage. No clinical trials or regulatory approvals exist for this compound.
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| CAS # |
2761446-55-1
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|---|---|
| Appearance |
Light yellow to light brown liquid
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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: 100 mg/mL (279.79 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.99 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.99 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.99 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
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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