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UPF 1069

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Chemical Structure| 1048371-03-4 同义名 : GKT237841
CAS号 : 1048371-03-4
货号 : A906956
分子式 : C17H13NO3
纯度 : 98%
分子量 : 279.29
MDL号 : MFCD14051631
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(375.95 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

2% DMSO+30% PEG 300+5% Tween 80+water 5 mg/mL

生物活性
靶点

  • PARP1

    PARP1, IC50:8.0 μM

  • PARP2

    PARP2, IC50:0.3 μM
描述 Poly(ADP-ribose) polymerases (PARPs) are a relatively large family of enzymes that catalyse the transfer of ADP-ribose units from NAD+ to acceptor proteins. They are involved in key cellular functions including DNA repair, telomere integrity, gene expression, cell division, cell survival and cell death. UPF 1069 is a specific PARP2 inhibitor with IC50 of 0.3 M, which is about 27 times more selective than PARP1. 10 µM UPF-1069 was able to reduce PARP activity by 80% in PARP-1-deficient fibroblasts, but only slightly inhibited the enzymic activity in wild-type fibroblasts. The effect of UPF-1069 on organotypic hippocampal slices exposed to 20 min OGD (oxygen-glucose deprivation) was tested at concentrations (0.1–1 µM) selectively acting on PARP-2. It significantly enhanced CA1 hippocampal damage. UPF-1069 displayed a significant neuroprotective activity both at a concentration (1 µM) selectively acting on PARP-2 and at a concentration (10 µM) that inhibits both PARP-1 and PARP-2 activities[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.58mL

0.72mL

0.36mL

17.90mL

3.58mL

1.79mL

35.81mL

7.16mL

3.58mL
参考文献

[1]Moroni F, Formentini L, et al. 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.

[2]Moroni F, Formentini L, Gerace E, et al. Selective PARP-2 inhibitors increase apoptosis in hippocampal slices but protect cortical cells in models of post-ischaemic brain damage. Br J Pharmacol. 2009;157(5):854-862