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Description: PARP14 inhibitor; cell-permeable
Chemical Name: 3-(N-(2-(4-(2-(4-((3-Carbamoylphenyl)amino)-4-oxobutanamido)ethyl)-1H-1,2,3-triazol-1-yl)ethyl)sulfamoyl)benzoic acid
Purity: ≥98% (HPLC)
Biological Activity
PARP14 inhibitor (IC50 = 490 nM). Exhibits ~ 24- and 18-fold selectivity for PARP14 over PARP1 and TNKS1, respectively. Binds both the nicotinamide and adenine sites on PARP14. Inhibits PARP14 and induces apoptosis in HepG2 and RPMI-8226 in cancer cells in vitro.
Technical Data
| M. Wt | 557.58 |
| Formula | C24H27N7O7S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 2084811-68-5 |
| PubChem ID | 122707115 |
| InChI Key | MUOMSHSMJCWQFH-UHFFFAOYSA-N |
| Smiles | NC(C1=CC=CC(NC(CCC(NCCC2=CN(N=N2)CCNS(=O)(C3=CC(C(O)=O)=CC=C3)=O)=O)=O)=C1)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 27.88 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 557.58. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 3.59 mL | 17.93 mL | 35.87 mL |
| 2.5 mM | 0.72 mL | 3.59 mL | 7.17 mL |
| 5 mM | 0.36 mL | 1.79 mL | 3.59 mL |
| 25 mM | 0.07 mL | 0.36 mL | 0.72 mL |
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References
References are publications that support the biological activity of the product.
Peng et al (2017) Small molecule microarray based discovery of PARP14 inhibitors. Angew.Chem.Int.Ed.Engl. 56 248 PMID: 27918638
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Keywords: H10, H10 supplier, PARP14, inhibitors, inhibits, apoptosis, Poly(ADP-ribose), Polymerase, 6228, Tocris Bioscience
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In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.