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QNZ

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Chemical Structure| 545380-34-5 同义名 : EVP4593;CAY10470
CAS号 : 545380-34-5
货号 : A230954
分子式 : C22H20N4O
纯度 : 99%+
分子量 : 356.42
MDL号 : MFCD06411436
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(98.2 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：
生物活性
靶点

  • TNF-α

    TNF-α, IC50:7 nM

  • NF-κB

    NF-κB, IC50:11 nM
描述 Nuclear factor-κB (NF-κB) is a protein complexes which is a pivotal transcription factor. It involves in regulating the immune system by enhancing the transcription of proinflammatory cytokines in the generation of acute inflammatory responses[1]. QNZ is a potent and selective NF-κB inhibitor with IC50 value of 11 nM[2].
SK-HEP-1 cells were treated with 0.4 µM QNZ and the cell viability measured by MTT assay was significantly inhibited in a time dependent manner. The NF-κB p65 (Ser536), anti-apoptotic proteins (XIAP, MCL-1 and c-FLIP) level examined by western blotting assay also inhibited after 48 hours of treatment[3].
BALB/c mice with infection in the right hind paw were i.p. injected with 0.001 g/kg of QNZ and 0.1 g/kg glucantime for five consecutive days. The combined treatment could decrease the lesion sizes of the infected paws significantly compared with the control group and increase IL-1β production in the supernatant from the excised infected paws measured by ELISA[4].
作用机制 QNZ inhibited the activation of NF-κB through inhibiting the phosphorylation of the its subunit IκBα and block the nuclear translocation of NF-κB[5][6].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
GABA MS-like neurons 100 nM Function assay rescues abnormal SOC-mediated calcium entry 27080129
GABA MS-like neurons 1000 nM Function assay normalizes the number of lysosomes/autophagosomes 27080129
GABA MS-like neurons 100 nM Function assay rescues aging neurons from cell death 27080129
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.81mL

0.56mL

0.28mL

14.03mL

2.81mL

1.40mL

28.06mL

5.61mL

2.81mL
参考文献

[1]Tobe M, Isobe Y, et al. Discovery of quinazolines as a novel structural class of potent inhibitors of NF-kappa B activation. Bioorg Med Chem. 2003;11(3):383-91.

[2]Tobe M, Isobe Y, et al. A novel structural class of potent inhibitors of NF-kappa B activation: structure-activity relationships and biological effects of 6-aminoquinazoline derivatives. Bioorg Med Chem. 2003;11(18):3869-78.

[3]Tsai JJ, Pan PJ, et al. Regorafenib induces extrinsic and intrinsic apoptosis through inhibition of ERK/NF-κB activation in hepatocellular carcinoma cells. Oncol Rep. 2017;37(2):1036-1044.

[4]Macedo SR, de Figueiredo Nicolete LD, et al. The pentavalent antimonial therapy against experimental Leishmania amazonensis infection is more effective under the inhibition of the NF-κB pathway. Int Immunopharmacol. 2015;28(1):554-9.

[5]Zhu X, Huang L, et al. NF-κB pathway link with ER stress-induced autophagy and apoptosis in cervical tumor cells. Cell Death Discov. 2017.

[6]Gupta SC, Sundaram C, et al. Inhibiting NF-κB activation by small molecules as a therapeutic strategy. Biochim Biophys Acta. 2010;1799(10-12):775-87.