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GPI-16552 | PARG inhibitor

GPI-16552 (443794-40-9) is a novel potent inhibitor of poly(ADP-ribose) glycohydrolase (PARG), IC50=1.7 μM1. Pre or post ischemia treatment (40 mg/kg) with GPI-16552 reduces brain infarct volumes in a rat model of cerebral ischemia2. 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 cells5.

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 reprofusion; 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-roibose) glycohydrolase inhibitor as chemosensitiser of malignant melanoma for temozolomide; Eur. J. Cancer, 41 2948

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GPI-16552 | 443794-40-9 | Structure | Supplier

Catalog#  10-1502

$60.00
Quantity
Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
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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 as supplied. Solutions in DMSO or DMF may be stored at -20° for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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