| Catalog | Description | Size | Price (USD) | Qty |
|---|---|---|---|---|
| GBM-3779-5MG | UPF-1069 | 5mg | $116.00 | |
| GBM-3779-25MG | UPF-1069 | 25mg | $357.00 |
| Bioassays Specification | |
| Bio-Activity | PARP-2 inhibitor |
| Chemical Name | 5-(2-Oxo-3-phenylethoxy)-1(2H)-isoquinolinone |
| Function / Pharmacology | PARP inhibitor selective for PARP-2 (IC50=0.3 μM; ~ 27-fold selective against PARP-1).1,2 Increases apoptosis in hippocampal slices but protects cortical cells in models of post-ischemic brain damage.3 Blocks the interaction between PARP-2 and FOXA1, attenuating androgen receptor-mediated gene expression and inhibiting androgen receptor-positive prostate cancer growth.4 |
| CAS# | 1048371-03-4 |
| MW | 279.3 |
| Molecular Formula | C17H13NO3 |
| Solubility | Soluble in DMSO up to 40 mg/ml |
| Supplied | powder |
| Storage as supplied | -20°C |
| Ship temp | Ambient |
| References | 1) Pellicciari et al. (2008), On the way to selective PARP-2 inhibitors. Design, synthesis, and preliminary evaluation of a series of isoquinolinone derivatives; Chem. Med. Chem., 3 914 2) Thorsell et al. (2017), Structural Basis for Potency and Promiscuity in Poly(ADP-ribose) Polymerase (PARP) and Tankyrase Inhibitors; J. Med. Chem., 60 1262 3) Moroni et al. (2009), Selective PARP-2 inhibitors increase apoptosis in hippocampal slices but protect cortical cells in models of post-ischaemic brain damage; Br. J. Pharmacol., 157 854 4) Gui et al. (2019), Selective targeting of PARP-2 inhibits androgen receptor signaling and prostate cancer growth through disruption of FOXA1 function; Proc. Natl. Acad. Sci. USA, 116 14573 |
| Protein Specification | |
| Purity | >98% |
| Bioassays Specification | |
| Bio-Activity | PARP-2 inhibitor |
| Chemical Name | 5-(2-Oxo-3-phenylethoxy)-1(2H)-isoquinolinone |
| Function / Pharmacology | PARP inhibitor selective for PARP-2 (IC50=0.3 μM; ~ 27-fold selective against PARP-1).1,2 Increases apoptosis in hippocampal slices but protects cortical cells in models of post-ischemic brain damage.3 Blocks the interaction between PARP-2 and FOXA1, attenuating androgen receptor-mediated gene expression and inhibiting androgen receptor-positive prostate cancer growth.4 |
| CAS# | 1048371-03-4 |
| MW | 279.3 |
| Molecular Formula | C17H13NO3 |
| Solubility | Soluble in DMSO up to 40 mg/ml |
| Supplied | powder |
| Storage as supplied | -20°C |
| Ship temp | Ambient |
| References | 1) Pellicciari et al. (2008), On the way to selective PARP-2 inhibitors. Design, synthesis, and preliminary evaluation of a series of isoquinolinone derivatives; Chem. Med. Chem., 3 914 2) Thorsell et al. (2017), Structural Basis for Potency and Promiscuity in Poly(ADP-ribose) Polymerase (PARP) and Tankyrase Inhibitors; J. Med. Chem., 60 1262 3) Moroni et al. (2009), Selective PARP-2 inhibitors increase apoptosis in hippocampal slices but protect cortical cells in models of post-ischaemic brain damage; Br. J. Pharmacol., 157 854 4) Gui et al. (2019), Selective targeting of PARP-2 inhibits androgen receptor signaling and prostate cancer growth through disruption of FOXA1 function; Proc. Natl. Acad. Sci. USA, 116 14573 |
| Protein Specification | |
| Purity | >98% |
