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GeA-69

Catalog No. T5399   CAS 2143475-98-1

GeA-69 (GeA69) is a selective and allosteric PARP14 macrodomain 2 (MD2) inhibitor (Kd: 0.86 μM in ITC assays).

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GeA-69 Chemical Structure
GeA-69, CAS 2143475-98-1
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
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Purity: 99.75%
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Biological Description
Chemical Properties
Storage & Solubility Information
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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 120 mg/mL (399.53 mM)

TargetMolReferences and Literature

1. Schuller M, et al. Discovery of a Selective Allosteric Inhibitor Targeting Macrodomain 2 of Polyadenosine-Diphosphate-Ribose Polymerase 14. ACS Chem Biol. 2017 Nov 17;12(11):2866-2874.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library DNA Damage & Repair Compound Library Anti-Aging Compound Library Bioactive Compounds Library Max Anti-Cancer Compound Library NO PAINS Compound Library Anti-Ovarian Cancer Compound Library Anti-Cardiovascular Disease Compound Library Bioactive Compound Library Anti-Pancreatic Cancer Compound Library

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Keywords

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

 

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