AO-365/43472821
Based on 1 Customer Validation
AO-365/43472821 is a selective, brain-penetrant Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) inhibitor (IC50 = 0.29 μM) and shows a significant inhibitory effect on (CDC-like kinase 1) CLK1 (IC50 = 0.08 μM). AO-365/43472821 could protect the human neuroblastoma cell line SH-SY5Y from Okadaic acid (HY-N6785) (OA)-induced injury. AO-365/43472821 decreased tau (pSer396)/tau and Aβ1-42 protein expression. AO-365/43472821 can be used for the study of Alzheimer's disease.
For research use only. We do not sell to patients.
- Purity: 99.94%
- CAS No.: 1081122-55-5
- Formula: C19H16N4O5S
- Molecular Weight:412.42
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Biological Activity
|
CLK1 0.08 μM (IC50) |
DYRK1A 0.29 μM (IC50) |
AO-365/43472821 (Compound Y16-5) (1 μM, 48 h) significantly protects SH-SY5Y cells from OA-induced damage and improves cell survival[1].
AO-365/43472821 (1-10 μM) significantly reduces the tau (pSer 396)/tau level in SH-SY5Y cells in a concentration-dependent manner, and also reduces the expression of Aβ1-42 protein[1].
AO-365/43472821 (48 h) shows a CC50 greater than 100 μM in both SH-SY5Y and HL-7702 cells, indicating no cytotoxicity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SH-SY5Y cells with OA (100 nM) for 24 h
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Concentration:1 μM
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Incubation Time:48 h, incubate for 24 hours, then add OA and incubate for another 24 hours
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Result:Protected SH-SY5Y cells from the OA-induced injury in a statistically significant way.
Chemical Information
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CAS No. 1081122-55-5
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Appearance Solid
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Molecular Weight 412.42
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Formula C19H16N4O5S
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Color White to light brown
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SMILES
COC1=CC=CC=C1OCC2=NN3C(COC4=CC5=C(OCO5)C=C4)=NN=C3S2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 25 mg/mL (60.62 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.06 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4247 mL | 12.1236 mL | 24.2471 mL | 60.6178 mL |
| 5 mM | 0.4849 mL | 2.4247 mL | 4.8494 mL | 12.1236 mL | |
| 10 mM | 0.2425 mL | 1.2124 mL | 2.4247 mL | 6.0618 mL | |
| 15 mM | 0.1616 mL | 0.8082 mL | 1.6165 mL | 4.0412 mL | |
| 20 mM | 0.1212 mL | 0.6062 mL | 1.2124 mL | 3.0309 mL | |
| 25 mM | 0.0970 mL | 0.4849 mL | 0.9699 mL | 2.4247 mL | |
| 30 mM | 0.0808 mL | 0.4041 mL | 0.8082 mL | 2.0206 mL | |
| 40 mM | 0.0606 mL | 0.3031 mL | 0.6062 mL | 1.5154 mL | |
| 50 mM | 0.0485 mL | 0.2425 mL | 0.4849 mL | 1.2124 mL | |
| 60 mM | 0.0404 mL | 0.2021 mL | 0.4041 mL | 1.0103 mL |