PolQi1
Based on 1 Customer Validation
PolQi1 is a selective inhibitor targeting the Polθ domain of DNA polymerase. PolQi1 inhibits the Polθ-mediated microhomology end joining (TMEJ/alt-EJ) pathway, reducing insertion/deletion (Indels) and imprecise editing events during DNA repair. PolQi1 can enhance the efficiency and accuracy of homology-directed repair (HDR) or Prime editing, and reduce off-target effects; and in combination with DNA-PK inhibitor AZD-7648 (HY-111783), exert efficient genome editing capabilities with dual pathway regulation. PolQi1 can be mainly used in gene editing research (such as CRISPR-Cas9 or Prime editing system optimization) to improve the precision editing efficiency of difficult-to-edit cells (such as primary hepatocytes and mouse embryos).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.42%
- CAS. Nr.: 2607139-80-8
- Formel: C18H14ClF5N4O2
- Molecular Weight:448.77
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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DNA Polymerase |
PolQi1 (3 μM; 3 h) combines with AZD7648, can enhance homology-directed repair (HDR)-mediated gene knock-in efficiency and reduce insertions/deletions (InDels) in HEK293T and human induced pluripotent stem cells (hiPSCs)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293T and hiPSCs (SpCas9-inducible)
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Concentration:0.3, 3, 10 μM for HEK293T cells; 3 μM for hiPSCs
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Incubation Time:3 h; combined with AZD7648 (1 μM)
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Result:Increased HDR-mediated knock-in efficiency by 3.9-fold and reduced InDels by 17.4-fold compared to DMSO controls.
At 10 μM, without significant additional improvement.
Increased HDR efficiency by 6.6-fold and reduced InDels by 2.3-fold compared to DMSO controls.
Chemical Information
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CAS. Nr. 2607139-80-8
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Appearance Solid
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Molecular Weight 448.77
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Formel C18H14ClF5N4O2
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Color White to off-white
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SMILES
CN(C1=C(C(Cl)=C(C=C1)F)F)C([C@H]2N(C3=CC(C(F)(F)F)=CC(C)=N3)C(NC2)=O)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (222.83 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. 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (5.57 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.
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.
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.
Reinheit & Dokumentation
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Data Sheet (280 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)
Verweise
[1]. Wimberger S, et al. Simultaneous inhibition of DNA-PK and Polϴ improves integration efficiency and precision of genome editing. Nat Commun. 2023 Aug 14;14(1):4761. [Content Brief]
[3]. Mentani A, et al. Prime Editing: Mechanistic Insights and DNA Repair Modulation. Cells. 2025 Feb 13;14(4):277. [Content Brief]
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 | 2.2283 mL | 11.1416 mL | 22.2831 mL | 55.7078 mL |
| 5 mM | 0.4457 mL | 2.2283 mL | 4.4566 mL | 11.1416 mL | |
| 10 mM | 0.2228 mL | 1.1142 mL | 2.2283 mL | 5.5708 mL | |
| 15 mM | 0.1486 mL | 0.7428 mL | 1.4855 mL | 3.7139 mL | |
| 20 mM | 0.1114 mL | 0.5571 mL | 1.1142 mL | 2.7854 mL | |
| 25 mM | 0.0891 mL | 0.4457 mL | 0.8913 mL | 2.2283 mL | |
| 30 mM | 0.0743 mL | 0.3714 mL | 0.7428 mL | 1.8569 mL | |
| 40 mM | 0.0557 mL | 0.2785 mL | 0.5571 mL | 1.3927 mL | |
| 50 mM | 0.0446 mL | 0.2228 mL | 0.4457 mL | 1.1142 mL | |
| 60 mM | 0.0371 mL | 0.1857 mL | 0.3714 mL | 0.9285 mL | |
| 80 mM | 0.0279 mL | 0.1393 mL | 0.2785 mL | 0.6963 mL | |
| 100 mM | 0.0223 mL | 0.1114 mL | 0.2228 mL | 0.5571 mL |