Chemren Bio-Engineering Co., Ltd.

Chemical Information

Biological Activity of UPF 1069

UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM; ~27-fold selective against PARP1.
IC50 Value:  0.3 μM
Target: PARP2
in 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