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。
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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。 |
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]. |
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 |
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 |