| 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 | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (13.32 mM), Sonication is recommended.
DMSO : 120 mg/mL (399.53 mM), Sonication is recommended.
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| Keywords | U-2 OS | poly ADP ribose polymerase | PARP14 | PARP | intact cell | Inhibitor | inhibit | HeLa | HEK293 | GeA-69 | GeA69 | GeA 69 | DNA damage repair mechanism | cytotoxicity | cell permeable |
| Inhibitors Related | BGP-15 | Niraparib tosylate monohyrate | 7-Methylguanine | 3-Aminobenzamide | XAV-939 | Niraparib | AZ9482 | RMC-7977 | RBN-2397 | Olaparib | Benzamide | OUL35 |
| Related Compound Libraries | DNA Damage & Repair Compound Library | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library | Anti-Breast Cancer Compound Library | Anti-Ovarian Cancer Compound Library | Inhibitor Library | Anti-Prostate Cancer Compound Library | Anti-Cardiovascular Disease Compound Library | NO PAINS Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library |
United States
