| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Other Sizes |
Purity: ≥98%
| Targets |
PARP14 ( Kd = 2.1 μM )
GeA-69 targets macrodomain 2 (MD2) of poly(ADP-ribose) polymerase 14 (PARP14). PARP14 is an enzyme involved in ADP-ribosylation, a post-translational modification that regulates various cellular processes including DNA repair, transcription, and inflammation. By allosterically inhibiting PARP14 MD2, GeA-69 interferes with the enzyme's enzymatic activity and disrupts its cellular functions. The compound's selectivity for PARP14 over other PARP family members makes it a valuable tool for studying PARP14 biology. |
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| ln Vitro |
GeA-69 (compound 1) at 50 μM and 250 μM, with pre-damage for 1 hour or 0.5, 1, 2.5 min, engages PARP14 MD2 in intact cells and stops it from localizing to DNA damage sites in U-2 OS cells[2].
In HeLa, U-2 OS, and HEK293 cells, GeA-69 (25 nM-250 μM; 72 h) demonstrates moderate cytotoxicity and high cell permeability, with 2% passing paracellularly and 98% transcellularly across the membrane[2].
GeA-69 binds to PARP14 MD2 with a Kd of 860 nM (ITC) and inhibits with an IC50 of 720 nM. The compound inhibits PARP14 MD2 relocalization to sites of DNA damage in U2OS cells when used at a concentration of 50 μM. Its allosteric mechanism of action has been characterized in biochemical and cellular assays. The compound's cell permeability supports its use in cellular studies. |
| ln Vivo |
GeA-69 has been studied for its effects on PARP14 function in vivo. By inhibiting PARP14, the compound interferes with its cellular functions, which may have implications for cancer and inflammatory diseases. The compound's ability to inhibit PARP14 MD2 relocalization to DNA damage sites has been demonstrated in cellular models. Specific in vivo efficacy data is limited in the available literature.
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| Enzyme Assay |
In vitro binding assays for GeA-69 involve measuring its binding affinity to PARP14 macrodomain 2 using isothermal titration calorimetry (ITC) or surface plasmon resonance. The Kd value of 860 nM is determined from these binding studies. Inhibition of PARP14 enzymatic activity is measured using biochemical assays with appropriate substrates. Selectivity against other PARP family members and related enzymes is assessed using broad screening panels. These cell-free assays provide quantitative data on the compound's potency and selectivity.
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| Cell Assay |
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. In vitro cell-based assays for GeA-69 involve treating U2OS cells with the compound to assess its effects on PARP14 MD2 relocalization to DNA damage sites. Cells are treated with GeA-69 at 50 μM and then exposed to DNA-damaging agents. PARP14 localization is visualized by immunofluorescence microscopy. The compound's effects on PARP14-dependent cellular processes such as DNA repair, transcription, and inflammation are assessed using appropriate functional assays. Cell viability and cytotoxicity are evaluated using standard assays. |
| Animal Protocol |
In vivo animal experiments for GeA-69 have not been extensively reported. As a PARP14 inhibitor, the compound has potential applications in cancer and inflammatory disease models. Studies in tumor-bearing mice or models of inflammation would be needed to assess in vivo efficacy. The compound's cell permeability and selectivity support its potential for in vivo applications. Specific dosing regimens and detailed efficacy data are not available in the current literature.
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| ADME/Pharmacokinetics |
GeA-69 is a cell-permeable, selective allosteric inhibitor of PARP14 macrodomain 2. The compound has a Kd of 860 nM (ITC) and an IC50 of 720 nM. It is typically dissolved in DMSO for in vitro studies. Its cell permeability supports its use in cellular studies. Specific pharmacokinetic data such as absorption, distribution, metabolism, and elimination are not extensively reported. The compound is typically stored under recommended conditions for research compounds.
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| Toxicity/Toxicokinetics |
Specific toxicity data for GeA-69 is not extensively reported. As a PARP14 inhibitor, its safety profile is related to its effects on ADP-ribosylation and PARP14-dependent cellular functions. The compound is generally well-tolerated in cellular studies at concentrations used for target inhibition. Comprehensive toxicological studies would be required for therapeutic development. Standard safety precautions should be taken when handling the compound in research settings.
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| References |
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| Additional Infomation |
GeA-69 is a cell-permeable, selective allosteric inhibitor targeting PARP14 macrodomain 2 with a Kd of 860 nM and an IC50 of 720 nM. It inhibits PARP14 MD2 relocalization to DNA damage sites. The compound has potential applications in cancer and inflammatory disease research. GeA-69 is a valuable tool compound for studying PARP14 biology and ADP-ribosylation.
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| Molecular Formula |
C20H16N2O
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|---|---|
| Molecular Weight |
300.353844642639
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| Exact Mass |
300.13
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| Elemental Analysis |
C, 79.98; H, 5.37; N, 9.33; O, 5.33
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| CAS # |
2143475-98-1
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| Related CAS # |
2143475-98-1
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| PubChem CID |
135397654
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| Appearance |
White to off-white solid powder
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| LogP |
4.2
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
23
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| Complexity |
437
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(=O)NC1=CC=CC=C1C2=CC=CC3=C2NC4=CC=CC=C34
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| InChi Key |
LDPDVNYCIOHPGF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H16N2O/c1-13(23)21-18-11-4-2-7-14(18)16-9-6-10-17-15-8-3-5-12-19(15)22-20(16)17/h2-12,22H,1H3,(H,21,23)
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| Chemical Name |
N-[2-(9H-carbazol-1-yl)phenyl]acetamide
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| Synonyms |
GeA69; GeA-69; GeA 69
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~60 mg/mL (~199.8 mM)
Ethanol: ~10 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.93 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.93 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.3329 mL | 1.6647 mL | 3.3294 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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