| Identification | Back Directory | [Name]
GPI-16552
(GPI16552) | [CAS]
443794-40-9 | [Synonyms]
GPI 16552
GPI-16552
(GPI16552)
9H-Fluorene-2,7-dicarboxamide, 9-oxo-N2,N7-bis(3-phenylpropyl)- | [Molecular Formula]
C33H30N2O3 | [MOL File]
443794-40-9.mol | [Molecular Weight]
502.6 |
| Chemical Properties | Back Directory | [Boiling point ]
763.2±60.0 °C(Predicted) | [density ]
1.217±0.06 g/cm3(Predicted) | [storage temp. ]
RT | [solubility ]
Soluble in DMSO (up to 25 mg/ml) or in DMF (up to 25 mg/ml). | [form ]
solid | [pka]
11.45±0.20(Predicted) | [color ]
Pale yellow | [Stability:]
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or DMF may be stored at -20° for up to 3 months. |
| Hazard Information | Back Directory | [Description]
GPI-16552 (443794-40-9) is a novel potent inhibitor of poly(ADP-ribose) glycohydrolase (PARG), IC50=1.7 μM.1 Pre or post ischemia treatment (40 mg/kg) with GPI-16552 reduces brain infarct volumes in a rat model of cerebral ischemia.2?It modulates the inflammatory response to ischemia/reperfusion in a rat splanchnic artery occlusion model3?and reduces the degree of spinal cord inflammation and tissue injury after experimental spinal cord trauma4. GPI-16552 synergizes with temozolomide in decreasing melanoma cell invasion and metastatic spreading in mice injected with B16 melanoma cells.5 | [Uses]
GPI 16552 is a a novel PARG inhibitor that ameliorates ischemic brain damage in rat. | [References]
1) Zhang?et al. (2002),?PARP and PARG as novel therapeutic targets; Drugs Future,?27?371
2) Lu?et al. (2003),?Post-treatment with a novel PARG inhibitor reduces infarct in cerebral ischemia in the rat; Brain Res.,978?99
3) Cuzzocrea?et al. (2005),?PARG activity mediates intestinal injury induced by splanchnic artery occlusion and reperfusion; FASEB J.,?19?558
4) Cuzzocrea?et al. (2006),?Poly(ADP-ribose) glycohydrolase activity mediates post-traumatic inflammatory reaction after experimental spinal cord trauma; J. Pharmacol. Exp. Ther.,?319?127
5) Tentori?et al. (2005),?Poly(ADP-ribose) glycohydrolase inhibitor as chemosensitiser of malignant melanoma for temozolomide; Eur. J. Cancer,?41?2948 |
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