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PARP1-IN-5 dihydrochloride {[allProObj[0].p_purity_real_show]}

货号:A1554512

PARP1-IN-5 dihydrochloride是一种具有低毒性和口服活性的 PARP-1 抑制剂,IC50 为 14.7 nM,适用于癌症治疗研究,尤其在 DNA 修复抑制和抗肿瘤药物开发中具有潜力。

PARP1-IN-5 dihydrochloride 化学结构 CAS号:2823308-89-8
PARP1-IN-5 dihydrochloride 化学结构
CAS号:2823308-89-8
PARP1-IN-5 dihydrochloride 3D分子结构
CAS号:2823308-89-8
PARP1-IN-5 dihydrochloride 化学结构 CAS号:2823308-89-8
PARP1-IN-5 dihydrochloride 3D分子结构 CAS号:2823308-89-8
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PARP1-IN-5 dihydrochloride 纯度/质量文件 产品仅供科研

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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。

PARP1-IN-5 dihydrochloride 生物活性

描述 PARP1-IN-5 dihydrochloride is a low-toxicity, orally active, potent, and selective inhibitor of PARP-1, with an IC50 of 14.7 nM. It is applicable for cancer research[1].
体内研究

PARP1-IN-5 dihydrochloride (1000 mg/kg; pO.) demonstrates no significant difference in body weight and blood parameters[1].

PARP1-IN-5 dihydrochloride (25 and 50 mg/kg; pO.; 12 days) significantly enhances carboplatin's inhibitory effect on A549 cells at 50 mg/kg[1].

PARP1-IN-5 dihydrochloride (50 mg/kg; pO.) positively correlates with PARP-1 expression[1].

PARP1-IN-5 dihydrochloride upregulates γ-H2AX expression and downregulates PAR expression[1].

体外研究

PARP1-IN-5 dihydrochloride (0.1~10 μM; A549 cells) dose-dependently enhances the cytotoxicity of CBP on A549 cells. In SK-OV-3 cells, it reduces the expressions of MCM2-7 within the same concentration range. PARP1-IN-5 dihydrochloride (0.1~320 μM; A549 cells) exhibits minimal cytotoxicity in A549 cells. Additionally, it significantly decreases the PAR level in SK-OV-3 cells[1].

PARP1-IN-5 dihydrochloride exerts its antitumor effects by targeting PARP-1. Additionally, it can upregulate the expression of γ-H2AX[1].

PARP1-IN-5 dihydrochloride 参考文献

[1]Long H, et al. Discovery of Novel Apigenin-Piperazine Hybrids as Potent and Selective Poly (ADP-Ribose) Polymerase-1 (PARP-1) Inhibitors for the Treatment of Cancer. J Med Chem. 2021;64(16):12089-12108.

PARP1-IN-5 dihydrochloride 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.86mL

0.37mL

0.19mL

9.30mL

1.86mL

0.93mL

18.61mL

3.72mL

1.86mL

PARP1-IN-5 dihydrochloride 技术信息

CAS号2823308-89-8
分子式C25H26Cl2N2O5S
分子量 537.455
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,2-8°C

溶解度

DMSO: 120 mg/mL(223.27 mM),配合低频超声助溶,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

H2O: 1 mg/mL(1.86 mM),配合低频超声,并水浴加热至45℃助溶

动物实验配方
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