MU1787
Based on 1 Customer Validation
MU1787 is a highly selective homeodomain-interacting protein kinase (HIPK) inhibitor with a furopyridine core, and shows improved selectivity against CLKs, with inactivity against DYRK1B, DYRK2, and MLK2/3 in in vitro cellular assays. MU1787 can be used for the research of malignancies.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 99.84%
- CAS No.: 2624098-97-9
- Formule: C19H18N4O
- Masse moléculaire:318.37
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
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HIPK1 285 nM (IC50) |
HIPK2 123 nM (IC50) |
HIPK3 283 nM (IC50) |
DYRK1A 213 nM (IC50) |
DYRK1B 956 nM (IC50) |
DYRK2 1309 nM (IC50) |
In Vitro
MU1787 potently inhibits purified human HIPK1 (IC50=187 nM), HIPK2 (IC50=29 nM), HIPK3 (IC50=159 nM), DYRK1A (IC50=213 nM), DYRK1B (IC50=956 nM), DYRK2 (IC50=1309 nM), CLK1 (IC50=8 nM), CLK2 (IC50=20 nM), and CLK4 (IC50=12 nM), but shows no significant inhibitory activity against CLK3[1].
MU1787 (10 μM) exhibits high selectivity for human HIPK1, HIPK2 and HIPK3 in a screening panel containing 373 purified kinases, only partially inhibits HIPK4 (51%), and shows extremely low off-target activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
Chemical Information
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CAS No. 2624098-97-9
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Appearance Solid
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Masse moléculaire 318.37
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Formule C19H18N4O
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Color White to off-white
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SMILES
CC(C)(C)C1=CC=C(C=C1)C2=COC(C=C3)=C2N=C3C4=CN=NN4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (314.10 mM; Need ultrasonic; 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)
In Vivo:
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 (7.85 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.85 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
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.
Pureté et documentation
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Fiche technique (276 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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Instruction de manipulation (2659 KB)
Références
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 | 3.1410 mL | 15.7050 mL | 31.4100 mL | 78.5250 mL |
| 5 mM | 0.6282 mL | 3.1410 mL | 6.2820 mL | 15.7050 mL | |
| 10 mM | 0.3141 mL | 1.5705 mL | 3.1410 mL | 7.8525 mL | |
| 15 mM | 0.2094 mL | 1.0470 mL | 2.0940 mL | 5.2350 mL | |
| 20 mM | 0.1570 mL | 0.7852 mL | 1.5705 mL | 3.9262 mL | |
| 25 mM | 0.1256 mL | 0.6282 mL | 1.2564 mL | 3.1410 mL | |
| 30 mM | 0.1047 mL | 0.5235 mL | 1.0470 mL | 2.6175 mL | |
| 40 mM | 0.0785 mL | 0.3926 mL | 0.7852 mL | 1.9631 mL | |
| 50 mM | 0.0628 mL | 0.3141 mL | 0.6282 mL | 1.5705 mL | |
| 60 mM | 0.0523 mL | 0.2617 mL | 0.5235 mL | 1.3087 mL | |
| 80 mM | 0.0393 mL | 0.1963 mL | 0.3926 mL | 0.9816 mL | |
| 100 mM | 0.0314 mL | 0.1570 mL | 0.3141 mL | 0.7852 mL |
MU1787 Related Classifications
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