Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GeA-69 (GeA69) is a selective and allosteric PARP14 macrodomain 2 (MD2) inhibitor (Kd: 0.86 μM in ITC assays).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
5 mg | In stock | $ 59.00 | |
10 mg | In stock | $ 97.00 | |
25 mg | In stock | $ 197.00 | |
50 mg | In stock | $ 347.00 | |
100 mg | In stock | $ 479.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 75.00 |
Description | GeA-69 (GeA69) is a selective and allosteric PARP14 macrodomain 2 (MD2) inhibitor (Kd: 0.86 μM in ITC assays). |
Targets&IC50 | PARP14:0.86 μM (Kd, in ITC assays) |
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. |
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. |
Molecular Weight | 300.35 |
Formula | C20H16N2O |
CAS No. | 2143475-98-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 120 mg/mL (399.53 mM)
You can also refer to dose conversion for different animals. More
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GeA-69 2143475-98-1 Chromatin/Epigenetic DNA Damage/DNA Repair PARP HeLa U-2 OS GeA69 cytotoxicity DNA damage repair mechanism intact cell Inhibitor cell permeable GeA 69 inhibit poly ADP ribose polymerase HEK293 inhibitor