UPF 1069

"目录号: HY-14478

Cell Cycle/DNA DamageEpigenetics-

UPF 1069是PARP2选择性抑制剂，IC50为0.3 μM，比对PARP1的抑制性高27倍。

PARP

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生物活性

Description

UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM; ~27-fold selective against PARP1.IC50 Value:  0.3 μMTarget: PARP2in vitro: In organotypic hippocampal slices, PARP-2 inhibition with UPF-1069 (0.01-1 micromolxL(-1)) caused a concentration-dependent exacerbation (up to 155%) of OGD-induced CA1 pyramidal cell death. Higher concentrations, acting on both PARP-1 and PARP-2, had no effect on OGD injury [1].in vivo: In organotypic hippocampal slices, PARP-2 inhibition with UPF-1069 (0.01-1 mM) causes a concentration-dependent exacerbation (up to 155%) of oxygen-glucose deprivation (OGD)-induced CA1 pyramidal cell death. Higher concentrations, acting on both PARP-1 and PARP-2, have no effect on OGD injury. In mouse mixed cortical cells exposed to OGD, UPF-1069 (1-10 mM) significantly reduces post-ischaemic damage.Clinical trial: N/A

References

[1].Moroni F, Formentini L, Gerace E, Selective PARP-2 inhibitors increase apoptosis in hippocampal slices but protect cortical cells in models of post-ischaemic brain damage. Br J Pharmacol. 2009 Jul;157(5):854-62.