1. Cell Cycle/DNA Damage
  2. DNA/RNA Synthesis
  3. CRT0044876

CRT0044876 is a potent and selective apurinic/apyrimidinic endonuclease 1 (APE1) inhibitor (IC50=~3 μM). CRT0044876 inhibits the AP endonuclease, 3′-phosphodiesterase and 3′-phosphatase activities of APE1, and is a specific inhibitor of the exonuclease III family of enzymes to which APE1 belongs. CRT0044876 potentiates the cytotoxicity of several DNA base-targeting compounds.

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CRT0044876 Chemical Structure

CRT0044876 Chemical Structure

CAS No. : 6960-45-8

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

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Description

CRT0044876 is a potent and selective apurinic/apyrimidinic endonuclease 1 (APE1) inhibitor (IC50=~3 μM). CRT0044876 inhibits the AP endonuclease, 3′-phosphodiesterase and 3′-phosphatase activities of APE1, and is a specific inhibitor of the exonuclease III family of enzymes to which APE1 belongs. CRT0044876 potentiates the cytotoxicity of several DNA base-targeting compounds[1].

In Vitro

A key step in BER is the processing of an apurinic/apyrimidinic (AP) site intermediate by an AP endonuclease. CRT0044876 has an IC50 for inhibition of APE1 of ∼3 μM and not only inhibits AP site cleavage catalyzed by purified APE1, but also cleavage directed by APE1 in a HeLa whole cell extract. CRT0044876 inhibits the 3′-phosphoglycolate diesterase activity of APE1 with an IC50 of ∼5 μM[1].
CRT0044876 inhibits both the exonuclease and AP endonuclease activities of exonuclease III, but shows no inhibitory activity towards endonuclease IV. CRT0044876 has minimal effects on BamHI restriction endonuclease or topoisomerase I even at CRT0044876 concentrations of 100 μM[1].
At non-toxic concentrations, CRT0044876 potentiates the cytotoxicity of several DNA damaging agents, which generate damage that is repaired in the BER pathway, including some currently-used anticancer drugs. The combination of MMS and CRT0044876 leads to a synergistic increase in the level of AP sites. Consistent with CRT0044876 being a specific BER inhibitor, a strong potentiation of hmdUrd cytotoxicity is seen in CRT0044876-treated cells (HT1080 cells)[1].

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

Molecular Weight

206.15

Formula

C9H6N2O4

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C(N1)=CC2=C1C([N+]([O-])=O)=CC=C2)O

Shipping

Room temperature in continental US; may vary elsewhere.

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

DMSO : 50 mg/mL (242.54 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.8508 mL 24.2542 mL 48.5084 mL
5 mM 0.9702 mL 4.8508 mL 9.7017 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

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This equation is commonly abbreviated as: C1V1 = C2V2

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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 (12.13 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.
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
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.8508 mL 24.2542 mL 48.5084 mL 121.2709 mL
5 mM 0.9702 mL 4.8508 mL 9.7017 mL 24.2542 mL
10 mM 0.4851 mL 2.4254 mL 4.8508 mL 12.1271 mL
15 mM 0.3234 mL 1.6169 mL 3.2339 mL 8.0847 mL
20 mM 0.2425 mL 1.2127 mL 2.4254 mL 6.0635 mL
25 mM 0.1940 mL 0.9702 mL 1.9403 mL 4.8508 mL
30 mM 0.1617 mL 0.8085 mL 1.6169 mL 4.0424 mL
40 mM 0.1213 mL 0.6064 mL 1.2127 mL 3.0318 mL
50 mM 0.0970 mL 0.4851 mL 0.9702 mL 2.4254 mL
60 mM 0.0808 mL 0.4042 mL 0.8085 mL 2.0212 mL
80 mM 0.0606 mL 0.3032 mL 0.6064 mL 1.5159 mL
100 mM 0.0485 mL 0.2425 mL 0.4851 mL 1.2127 mL
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CRT0044876 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.

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CRT0044876
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HY-W014622
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