KI-DX-014
Based on 1 Customer Validation
KI-DX-014 is a DDX21 inhibitor with high RNA-binding inhibitory activity (IC50 of 3.31 μM). KI-DX-014 targets DDX21’s intrinsically disordered C-terminal domain, inhibits DDX21-structured RNA interaction, modulates DDX21’s RNA-dependent ATPase activity, and disrupts DDX21 biomolecular condensate formation. KI-DX-014 attenuates in vitro P-TEFb release from the 7SK snRNP complex, suppresses P-TEFb-dependent RNA polymerase II CTD phosphorylation, and induces developmental defects in zebrafish embryos. KI-DX-014 acts as a chemical probe for dissecting DDX21 functions in normal physiology and disease states. KI-DX-014 can be used for cancers and neurodegenerative disorders research.
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- Pureté: 99.87%
- CAS No.: 1309288-83-2
- Formule: C17H22N4O3
- Masse moléculaire:330.38
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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
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Activité biologique
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RNA Polymerase |
KI-DX-014 (30 min preincubation with DDX21-FL at RT, 1 h incubation with RNA at RT) inhibits the interaction of full-length DDX21 with 7SK-SL4 RNA and 7SK-SL1 RNA with IC50 values of 3.31 μM and 3.79 μM[1].
KI-DX-014 inhibits the interaction of DDX21-HC+CTD with 7SK-SL4 RNA with an IC50 of 10.28 μM[1].
KI-DX-014 inhibits the interaction of DDX21-CTD with 7SK-SL4 RNA with an IC50 of 13.64 μM[1].
KI-DX-014 (10-100 μM; 1 h) attenuates the 7SK-SL4-stimulated ATPase activity of full-length DDX21 in a dose-dependent manner at concentrations of 10, 50, and 100 μM[1].
Ki-DX-014 (10-100 μM; 1 h) attenuates the U15-stimulated ATPase activity of full-length DDX21 in a dose-dependent manner at concentrations of 10, 50, and 100 μM[1].
KI-DX-014 (10-100 μM; 30 cycles (1 min on, 3 min off) at 4 °C) dose-dependently inhibits DDX21-mediated release of P-TEFb from the 7SK snRNP complex at concentrations of 10, 50, and 100 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Danio rerio embryos (wild-type, 1-2 cell stage)[1]
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Dosage:2.5 μM; 5 μM; 10 μM
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Administration:microinjection; single dose at 1-cell stage
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Result:Induced dose-dependent larval malformations, including curved body phenotypes and facial development defects.
Slightly reduced survival rate of treated embryos compared to vehicle controls at 24 hours postfertilization.
Detected dose-dependent reduction in phosphorylation of RNA polymerase II CTD serine 2 and serine 5 via Western blot.
Chemical Information
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CAS No. 1309288-83-2
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Appearance Oil
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Masse moléculaire 330.38
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Formule C17H22N4O3
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Color Colorless to light yellow
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SMILES
COC1=CC=C(C=C1)N2N=CC(CN3CCC(C(O)=O)(C3)N)=C2C
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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
DMSO : 100 mg/mL (302.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 100 mg/mL (302.68 mM; Need ultrasonic)
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (7.57 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 (7.57 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.
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Pureté et documentation
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Fiche technique (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)
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- 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 / H2O | 1 mM | 3.0268 mL | 15.1341 mL | 30.2682 mL | 75.6704 mL |
| 5 mM | 0.6054 mL | 3.0268 mL | 6.0536 mL | 15.1341 mL | |
| 10 mM | 0.3027 mL | 1.5134 mL | 3.0268 mL | 7.5670 mL | |
| 15 mM | 0.2018 mL | 1.0089 mL | 2.0179 mL | 5.0447 mL | |
| 20 mM | 0.1513 mL | 0.7567 mL | 1.5134 mL | 3.7835 mL | |
| 25 mM | 0.1211 mL | 0.6054 mL | 1.2107 mL | 3.0268 mL | |
| 30 mM | 0.1009 mL | 0.5045 mL | 1.0089 mL | 2.5223 mL | |
| 40 mM | 0.0757 mL | 0.3784 mL | 0.7567 mL | 1.8918 mL | |
| 50 mM | 0.0605 mL | 0.3027 mL | 0.6054 mL | 1.5134 mL | |
| 60 mM | 0.0504 mL | 0.2522 mL | 0.5045 mL | 1.2612 mL | |
| 80 mM | 0.0378 mL | 0.1892 mL | 0.3784 mL | 0.9459 mL | |
| 100 mM | 0.0303 mL | 0.1513 mL | 0.3027 mL | 0.7567 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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