2. Cell Cycle/DNA Damage Epigenetics
  3. PARP
  4. GeA-69

GeA-69 is a selective, allosteric inhibitor of poly-adenosine-diphosphate-ribose polymerase 14 (PARP14) targeting macrodomain 2 (MD2), with a Kd value of 2.1 μM. GeA-69 involves in DNA damage repair mechanisms and prevents recruitment of PARP14 MD2 to sites of laser-induced DNA damage.

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

GeA-69 Chemical Structure

GeA-69 Chemical Structure

CAS No. : 2143475-98-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 66 In-stock
Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Solid
1 mg USD 30 In-stock
5 mg USD 60 In-stock
10 mg USD 100 In-stock
25 mg USD 190 In-stock
50 mg USD 340 In-stock
100 mg USD 460 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

GeA-69 Related Antibodies

Top Publications Citing Use of Products

View All PARP Isoform Specific Products:

View All Isoforms
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GeA-69 is a selective, allosteric inhibitor of poly-adenosine-diphosphate-ribose polymerase 14 (PARP14) targeting macrodomain 2 (MD2), with a Kd value of 2.1 μM. GeA-69 involves in DNA damage repair mechanisms and prevents recruitment of PARP14 MD2 to sites of laser-induced DNA damage[1][2].

IC50 & Target[1]

PARP14

2.1 μM (Kd)

In Vitro

GeA-69 (compound 1) (50 μM and 250 μM; pre-damage for 1 h or 0.5, 1, 2.5 min) engages PARP14 MD2 in intact cells and prevents its localisation to sites of DNA damage in U-2 OS cells[2].
GeA-69 (25 nM-250 μM; 72 h) exhibits moderate cytotoxicity among HeLa, U-2 OS and HEK293 cells and highly cell permeable with 2 % passing paracellular and 98 % transcellular over the membrane[2].

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

GeA-69 Related Antibodies

Cell Cytotoxicity Assay[2]

Cell Line: HeLa, U-2 OS and HEK293 cells
Concentration: 25 nM-250 μM
Incubation Time: 72 hours
Result: Resulted moderate cytotoxicity against normal cells with EC50_HeLa=58 µM, EC50_U-2 OS=52 µM, EC50_HEK293=54 µM.
Molecular Weight

300.35

Formula

C20H16N2O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(NC1=CC=CC=C1C2=CC=CC3=C2NC4=C3C=CC=C4)=O
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 : ≥ 125 mg/mL (416.18 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3294 mL 16.6472 mL 33.2945 mL
5 mM 0.6659 mL 3.3294 mL 6.6589 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 2.08 mg/mL (6.93 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (6.93 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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, 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 1 mM 3.3294 mL 16.6472 mL 33.2945 mL 83.2362 mL
5 mM 0.6659 mL 3.3294 mL 6.6589 mL 16.6472 mL
10 mM 0.3329 mL 1.6647 mL 3.3294 mL 8.3236 mL
15 mM 0.2220 mL 1.1098 mL 2.2196 mL 5.5491 mL
20 mM 0.1665 mL 0.8324 mL 1.6647 mL 4.1618 mL
25 mM 0.1332 mL 0.6659 mL 1.3318 mL 3.3294 mL
30 mM 0.1110 mL 0.5549 mL 1.1098 mL 2.7745 mL
40 mM 0.0832 mL 0.4162 mL 0.8324 mL 2.0809 mL
50 mM 0.0666 mL 0.3329 mL 0.6659 mL 1.6647 mL
60 mM 0.0555 mL 0.2775 mL 0.5549 mL 1.3873 mL
80 mM 0.0416 mL 0.2081 mL 0.4162 mL 1.0405 mL
100 mM 0.0333 mL 0.1665 mL 0.3329 mL 0.8324 mL
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GeA-69 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:

GeA-692143475-98-1GeA69GeA 69PARPpoly ADP ribose polymeraseDNA damage repair mechanismHeLaU-2 OSHEK293cytotoxicitycell permeableintact cellInhibitorinhibitorinhibit

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