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GPI-16552 | PARG inhibitor

CAS:
443794-40-9
Catalog Number:
10-1502
Activity:
PARG inhibitor
Chemical Name:
N-bis-(3-Phenyl-propyl)-9-oxo-fluorene-2,7-diamide
Molecular Weight:
502.62
Molecular Formula:
C33H30N2O3
Solubility:
Soluble in DMSO (up to 25 mg/ml) or in DMF (up to 25 mg/ml).
Physical Properties:
Pale yellow solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
RT
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.
Shipping Code:
RT

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

References/Citations:

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

GPI-16552 | PARG inhibitor is also available in the Cellular Metabolism Library.
CAS:
443794-40-9
Catalog Number:
10-1502
Activity:
PARG inhibitor
Chemical Name:
N-bis-(3-Phenyl-propyl)-9-oxo-fluorene-2,7-diamide
Molecular Weight:
502.62
Molecular Formula:
C33H30N2O3
Solubility:
Soluble in DMSO (up to 25 mg/ml) or in DMF (up to 25 mg/ml).
Physical Properties:
Pale yellow solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
RT
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.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

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