S81050 |
Quisinostat (JNJ-26481585) |
源叶(MedMol) | 98% |
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- 产品描述: Quisinostat (JNJ-26481585) is a potent, second-generation and orally active pan-HDAC inhibitor (HDACi), with IC50 values ranging from 0.11 nM to 0.64 nM for HDAC1, HDAC2, HDAC4, HDAC10 and HDAC11. Quisinostat has a broad spectrum antitumoral activity. Quisinostat can induce autophagy in neuroblastoma cells
- 靶点: HDAC1:0.11 nM (IC50);HDAC2:0.33 nM (IC50);HDAC4:0.64 nM (IC50);HDAC10:0.46 nM (IC50);HDAC11:0.37 nM (IC50);HDAC3:4.86 nM (IC50);HDAC5:3.69 nM (IC50);HDAC8:4.26 nM (IC50);HDAC9:32.1 nM (IC50);HDAC6:76.8 nM (IC50);HDAC7:119 nM (IC50);Apoptosis; HDAC; Autophagy
- 体内研究:
Quisinostat (40 mg/kg; p.o.; once daily; for 3 days) acts as a potent HDAC1 inhibitor p21waf1,cip1 ZsGreen tumors in vivo. Quisinostat induces continuous H3 acetylation in tumor tissue in vivo. Quisinostat (10 mg/kg; once daily; i.p.; for 14 days) strongly inhibits the growth of large pre-established HCT116 colon xenografts
- 参考文献:
1. Arts J, et al. JNJ-26481585, a novel second-generation oral histone deacetylase inhibitor, shows broad-spectrum preclinical antitumoral activity. Clin Cancer Res. 2009 Nov 15;15(22):6841-51. 2. Vamsi Krishna Kommalapati, et al. Inhibition of JNJ-26481585-mediated autophagy induces apoptosis via ROS activation and mitochondrial membrane potential disruption in neuroblastoma cells. Mol Cell Biochem. 2020 May;468(1-2):21-34.
- 溶解性: Soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.535 ml 12.675 ml 25.35 ml 5 mM 0.507 ml 2.535 ml 5.07 ml 10 mM 0.254 ml 1.268 ml 2.535 ml 50 mM 0.051 ml 0.254 ml 0.507 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)