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UPF 1069 98%

货号：A906956 同义名： GKT237841 Ambeed 开学季，买赠积分，赢豪礼

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

UPF 1069 化学结构 CAS号：1048371-03-4
UPF 1069 化学结构
CAS号：1048371-03-4
UPF 1069 3D分子结构
CAS号：1048371-03-4
UPF 1069 化学结构 CAS号：1048371-03-4
UPF 1069 3D分子结构 CAS号：1048371-03-4
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UPF 1069 纯度/质量文件 产品仅供科研

货号：A906956 标准纯度： 98%
批次查询： 批次纯度:

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产品名称 PARP ↓ PARP1 ↓ PARP2 ↓ PARP3 ↓ 其他靶点 纯度
PJ34 HCl ++

PARP, EC50: 20 nM

 		99%+
Rucaparib phosphate ++++

PARP, Ki: 1.4 nM

 		99%+
3-Aminobenzamide ++

PARP, IC50: <50 nM

 		98%
AZD-2461 ✔ 99%+
BGP-15 ✔ 99%+
NU1025 +

PARP, IC50: 400 nM

 		97%
Benzamide +

PARP, IC50: 3.3 μM

 		98%
Picolinamide +

PARP, IC50: 95 μM

 		98%
AG14361 +++

PARP1, Ki: <5 nM

 		98+%
Iniparib ✔ 98%
Talazoparib ++++

PARP1, IC50: 0.57 nM

 		99%+
NMS-P118 ++

PARP1, Kd: 0.009 μM

 		98+%
UPF 1069 +

PARP1, IC50: 8.0 μM

 		++

PARP2, IC50: 0.3 μM

 		98%
A-966492 ++++

PARP1, EC50: 1 nM

PARP1, Ki: 1 nM

 		+++

PARP2, Ki: 1.5 nM

 		99%+
Veliparib ++

PARP1, Ki: 5.2 nM

 		+++

PARP2, Ki: 2.9 nM

 		98%
Niraparib tosylate +++

PARP1, IC50: 3.8 nM

 		+++

PARP2, IC50: 2.1 nM

 		99%+
Stenoparib ++++

PARP1, IC50: 1 nM

 		++++

PARP2, IC50: 1.2 nM

 		98%
Olaparib +++

PARP1, IC50: 5 nM

 		++++

PARP2, IC50: 1 nM

 		98%
Niraparib +++

PARP1, IC50: 3.8 nM

 		+++

PARP2, IC50: 2.1 nM

 		98%
ME0328 +

PARP1, IC50: 6.3 μM

 		+

PARP3, IC50: 0.89 μM

 		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

UPF 1069 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].

UPF 1069 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

UPF 1069 实验方案

计算器
存储液制备 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

UPF 1069 技术信息

CAS号1048371-03-4
分子式C17H13NO3
分子量 279.29
别名 GKT237841
运输蓝冰
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

Tags: UPF 1069 | 1048371-03-4 | UPF1069 | UPF-1069 | PARP Inhibitor | Cell Cycle/DNA Damage | Epigenetics | PARP | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | UPF 1069 纯度/质量文件 | UPF 1069 亚型比较 | UPF 1069 生物活性 | UPF 1069 参考文献 | UPF 1069 实验方案 | UPF 1069 技术信息

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