1. Cell Cycle/DNA Damage
  2. DNA/RNA Synthesis
  3. PolQi2

PolQi2 is a PolΘ inhibitor that targets and inhibits alt-EJ (alternative end-joining) repair by inhibiting the helicase domain at the N-terminus of PolΘ. PolQi2 enhances the precision and integration efficiency of gene editing at different loci and in various cell lines. Furthermore, the combined use of PolQi2 with DNA-PK inhibitors reduces the off-target effects of Cas9. PolQi2 can be used in gene editing research.

For research use only. We do not sell to patients.

CAS No. : 2565638-16-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

    PolQi2 purchased from MedChemExpress. Usage Cited in: Nat Biotechnol. 2024 Nov 27.  [Abstract]

    Quantification by long-read sequencing of the fraction of total reads with a length greater than a defined size and the quantified frequency of deletions larger than 1 kb in edited RPE-1 p53−/− cells was performed. Editing with combined AZD7648 and PolQi2 (3 µM; 3 d) reduced AZD7648-induced kilobase-scale deletions.

    PolQi2 purchased from MedChemExpress. Usage Cited in: Nat Biotechnol. 2024 Nov 27.  [Abstract]

    Editing with combined AZD7648 and PolQi2 (3 μM; 3 d) maintained elevated HDR levels. Frequencies of HDR and indels detected by short-read sequencing in RPE-1 p53−/− and RPE-1 p53+/+ cells edited at HBB, CCR5, and GAPDH were recorded.

    PolQi2 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 May 13:2025.05.10.653283.  [Abstract]

    Quantification of Ec78 retron precise editing was performed in comparison with no reverse transcriptase control (No RT), in the absence (Ec78) or the presence (Ec78 + inhib) of inhibitors, AZD7648 and PolQi2 (3 μM; 48 h), and the same experiments were conducted with the Mestre-1531 retron (RT 1531) using the same inhibitors.

    PolQi2 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Nov 29.

    PolQi2, a potent Polθ inhibitor, suppresses the MMEJ repair pathway and enhances HDR efficiency during CRISPR/Cas9-mediated gene editing. Splenic T cells from transgenic Cas9 mice were activated with Dynabeads and transduced with the specified MOI of AAV after 48 hours in 1 μM AZD7468 and 3 μM PolQi2. Percentage of cells expressing GFP above baseline level was determined by flow cytometry 5 days after transduction.

    PolQi2 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Nov 29.

    Knock-in efficiency was assessed by flow cytometry as the percentage of GFP+ cells among CD3- cells. Treatment with AZD7648 and PolQi2 (3 μM) resulted in the highest editing efficiency, achieving a knock-in rate of up to 80% under AAV transduction conditions.

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    PolQi2 is a PolΘ inhibitor that targets and inhibits alt-EJ (alternative end-joining) repair by inhibiting the helicase domain at the N-terminus of PolΘ. PolQi2 enhances the precision and integration efficiency of gene editing at different loci and in various cell lines. Furthermore, the combined use of PolQi2 with DNA-PK inhibitors reduces the off-target effects of Cas9. PolQi2 can be used in gene editing research[1][2].

    IC50 & Target

    Helicase

     

    In Vitro

    PolQi2 (3 μM, 14 days), in combination with DNA-PK inhibitors (1 μM, 14 days), efficiently and stably achieves targeted gene insertion in HeLa and Jurkat cells, without adversely affecting cell proliferation [1].

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

    Molecular Weight

    453.90

    Formula

    C21H16ClN5O3S

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1=CC=NC=C1C2=C(OC)C=CC=C2)NC3=NN=C(S3)OCC4=NC=C(C=C4)Cl

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 70 mg/mL (154.22 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2031 mL 11.0156 mL 22.0313 mL
    5 mM 0.4406 mL 2.2031 mL 4.4063 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

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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 (5.51 mM); Clear solution; Need ultrasonic

      This protocol yields a clear solution of 2.5 mg/mL.

      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% Corn Oil

      Solubility: 2.5 mg/mL (5.51 mM); Clear solution; Need ultrasonic

      This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    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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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    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).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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

    Purity: 98.91%

    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. 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 2.2031 mL 11.0156 mL 22.0313 mL 55.0782 mL
    5 mM 0.4406 mL 2.2031 mL 4.4063 mL 11.0156 mL
    10 mM 0.2203 mL 1.1016 mL 2.2031 mL 5.5078 mL
    15 mM 0.1469 mL 0.7344 mL 1.4688 mL 3.6719 mL
    20 mM 0.1102 mL 0.5508 mL 1.1016 mL 2.7539 mL
    25 mM 0.0881 mL 0.4406 mL 0.8813 mL 2.2031 mL
    30 mM 0.0734 mL 0.3672 mL 0.7344 mL 1.8359 mL
    40 mM 0.0551 mL 0.2754 mL 0.5508 mL 1.3770 mL
    50 mM 0.0441 mL 0.2203 mL 0.4406 mL 1.1016 mL
    60 mM 0.0367 mL 0.1836 mL 0.3672 mL 0.9180 mL
    80 mM 0.0275 mL 0.1377 mL 0.2754 mL 0.6885 mL
    100 mM 0.0220 mL 0.1102 mL 0.2203 mL 0.5508 mL
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    • 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.

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    Cat. No.:
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