| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| ln Vitro |
Aquinoxaline effectively inhibits the deubiquitinase (DUB) activity of recombinant full-length GST-CYLD with an IC50 value of 30 μM. Its mechanism of action is through targeting the catalytic domain of the enzyme rather than disrupting substrate binding [1]. Aquinoxaline inhibits the DUB activity of the USP catalytic domain of truncated CYLD with an IC50 value of approximately 65.4 μM, confirming that it targets the catalytic region of CYLD [1]. Aquinoxaline (25-100 μM) can inhibit the DUB activity of CYLD-WT and CYLD-Y940F, but its inhibitory effect on CYLD-Y940A is weakened, indicating that Tyr940 of CYLD is crucial for optimal interaction with aquinoxaline [1]. Aquinoxaline (20) is a selective inhibitor of USP family deubiquitinases and has no inhibitory activity against DUBs of the OTU, UCH, JAMM, or MJD/Josephin family [1]. Aquinoxaline (20-40 μM; 2 h) increases non-degradable M1-linked and K63-linked polyubiquitin chains in HeLa cells [1]. Aquinoxaline (20-40 μM; 12 h) enhances LUBAC and TNFα-mediated NF-κB activation in HEK293T cells [1]. Aquinoxaline (20-30 μM; 2 h) enhances phosphorylation of key NF-κB signaling pathway components in TNFα-stimulated HeLa and HEK293T cells and delays IκBα degradation [1].
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: HeLa Cells Tested Concentrations: 20, 40 μM Incubation Duration: 2 hours Experimental Results: Total polyubiquitin chains increased, especially M1-linked and K63-linked polyubiquitin chains. K48-linked polyubiquitin chains were unaffected. RIP1 and NEMO polyubiquitination increased, especially M1-linked polyubiquitin chains were restored in CYLD overexpression cells. |
| References |
| Molecular Formula |
C20H27N3O4S
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|---|---|
| Molecular Weight |
405.51
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| Appearance |
White to off-white solid
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| SMILES |
O=C1N(CC(C)C)C=C(NC(NC(CCSC)C(OC)=O)=O)C2=C1C=CC=C2
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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 (~246.60 mM; with sonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3 mg/mL (7.40 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 canAdd 100 μL of DMSO stock solution (30.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of physiological saline: Dissolve 0.9 g of sodium chloride in double-distilled water and dilute to 100 mL to obtain clear physiological saline. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 3 mg/mL (7.40 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 canAdd 100 μL of DMSO stock solution (30.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD saline (4°C, store for one week): Dissolve 2 g of SBE-β-CD powder in 10 mL of saline until completely dissolved and clear. 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: ≥ 3 mg/mL (7.40 mM)(saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4660 mL | 12.3302 mL | 24.6603 mL | |
| 5 mM | 0.4932 mL | 2.4660 mL | 4.9321 mL | |
| 10 mM | 0.2466 mL | 1.2330 mL | 2.4660 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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