UPF 1069

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 activities².

溶解方案(细胞实验)

DMSO 中的溶解度 : ≥ 100 mg/mL (358.05 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)|* "≥" means soluble, but saturation unknown.

溶解方案(动物实验)

"方案 一": "请依序添加每种溶剂：10% DMSO 40% PEG300 5% Tween-80 45% SalineSolubility: ≥ 2.5 mg/mL (8.95 mM); 澄清溶液 此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。"

"方案 二": "请依序添加每种溶剂：10% DMSO 90% Corn OilSolubility: ≥ 2.5 mg/mL (8.95 mM); 澄清溶液 此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。"