1048371-03-4|UPF-1069|CsnPharm

CAS No.: 1048371-03-4

UPF 1069 Catalog No. CSN17138

Synonyms: GKT237841

UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM, which is ~27-fold selective against PARP1.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

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].
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.5805 mL
- 17.9025 mL
- 35.8051 mL
- 5 mM
- 0.7161 mL
- 3.5805 mL
- 7.1610 mL
- 10 mM
- 0.3581 mL
- 1.7903 mL
- 3.5805 mL

技术信息

CAS号

1048371-03-4

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H13NO3

运输

蓝冰

分子量

279.29

别名

GKT237841

溶解度

DMSO	55.0 mg/mL (196.9 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

2% DMSO+30% PEG 300+5% Tween 80+water

5 mg/mL

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