2. Membrane Transporter/Ion Channel Cell Cycle/DNA Damage
  3. ATP Synthase DNA/RNA Synthesis
  4. KI-DX-014

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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KI-DX-014

KI-DX-014 Chemical Structure

CAS No. : 1309288-83-2

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Oil + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

KI-DX-014 Related Antibodies

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Description

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[1].

IC50 & Target

RNA Polymerase

 

In Vitro

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.

KI-DX-014 Related Antibodies
In Vivo

KI-DX-014 (2.5-10 μM; microinjection; single dose at 1-cell stage) induces dose-dependent developmental defects and reduces RNA polymerase II CTD serine 2 and serine 5 phosphorylation in Danio rerio embryos by inhibiting DDX21-dependent P-TEFb release[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Danio rerio embryos (wild-type, 1-2 cell stage)[1]
Dosage: 2.5 μM; 5 μM; 10 μM
Administration: microinjection; single dose at 1-cell stage
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.
Molecular Weight

330.38

Formula

C17H22N4O3
CAS No.
Appearance

Oil

Color

Colorless to light yellow

SMILES

COC1=CC=C(C=C1)N2N=CC(CN3CCC(C(O)=O)(C3)N)=C2C
Shipping

Room temperature in continental US; may vary elsewhere.
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
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0268 mL 15.1341 mL 30.2682 mL
5 mM 0.6054 mL 3.0268 mL 6.0536 mL
View the 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.

* 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Volume
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
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 / 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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KI-DX-014 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

KI-DX-0141309288-83-2ATP SynthaseDNA/RNA Synthesisintrinsically disordered C-terminal domainzebrafish embryosDDX21P-TEFbbiomolecular condensatestructured RNARNA-dependent ATPase activityRNA polymerase II CTD phosphorylation7SK snRNP complexbreast cancerInhibitorinhibitorinhibit

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