GPI-16552 (GPI16552) Chemical Properties

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).

pka

11.45±0.20(Predicted)

form 

solid

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.

GPI-16552 (GPI16552) Usage And Synthesis

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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