| Name | GeA-69 |
| Description | GeA-69 (GeA69) is a selective and allosteric PARP14 macrodomain 2 (MD2) inhibitor (Kd: 0.86 μM in ITC assays). |
| Kinase Assay | Binding experiments were carried out on a VP-ITC microcalorimeter. All experiments were performed in 50 mM HEPES (pH 7.4), 300 mM NaCl, 5 % glycerol, 0.5 mM TCEP at 12 °C, a reference power of 12 μCal/sec and a stirring speed of 307 rpm. The titrations were conducted using an initial injection of 2 μL followed by 28 identical injections of 10 μL with duration of 4 sec (per injection) and a spacing of 240 sec between injections. Competition experiments were performed on an iTC200 instrument at 20 °C, a reference power of 12 μCal/sec and a stirring speed of 1000 rpm. Following an initial injection of 0.2 μL, 20 identical injections of 2 μL were run with a duration of 4 sec (per injection) and a spacing of 150 sec between injections. Data analysis was carried out using Origin software with the MicroCal plugin. Thermodynamic parameters were calculated using ΔG = ΔH ? TΔS = ?RTlnKB, where ΔG, ΔH, and ΔS are the changes in free energy, enthalpy, and entropy of binding, respectively. In all cases, a single binding site model was employed. |
| In vitro | The macrodomain recruitment was significantly decreased in cells pre-treated with 50 μM GeA-69 and completely prevented in cells exposed to 250 μM GeA-69. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 120 mg/mL (399.53 mM)
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| Keywords | PARP | HeLa | U-2 OS | GeA69 | cytotoxicity | DNA damage repair mechanism | intact cell | GeA-69 | Inhibitor | cell permeable | GeA 69 | inhibit | poly ADP ribose polymerase | HEK293 |
| Inhibitors Related | 4'-Methoxychalcone | Niraparib tosylate monohyrate | VPC-70063 | 3-Aminobenzamide | XAV-939 | Niraparib | 3-Methoxybenzamide | NU1025 | Olaparib | Benzamide | Picolinamide | OUL35 |
| Related Compound Libraries | DNA Damage & Repair Compound Library | Bioactive Compound Library | Anti-Breast Cancer Compound Library | Anti-Ovarian Cancer Compound Library | Inhibitor Library | NO PAINS Compound Library | Anti-Cardiovascular Disease Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library |
United States
