产品说明书
NCGC00244536
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同义名 : | - |
| CAS号 : | 2003260-55-5 | |
| 货号 : | A860757 | |
| 分子式 : | C25H22N2O2 | |
| 纯度 : | 95% | |
| 分子量 : | 382.454 | |
| MDL号 : | MFCD31382180 | |
| 存储条件： |
粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 35 mg/mL(91.51 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 |
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| 动物实验配方： |
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| 描述 | Histone methylation is a key epigenetic marker involved in tumorigenesis. The overexpression of histone lysine demethylase KDM4 has been observed in multiple human cancer. NCGC00244536 is a novel, potent KDM4 inhibitor with an IC50 value of 10 nM. It showed a high selective inhibitory effect on the fast-growing AR-negative PC3 cells with an IC50 value of 40 nM. It potently inhibited AR-positive LNCaP and VCaP cell lines with IC50 values less than 1 μM. It also impeded the growth of breast cancer cell lines MDA-MB2 and MCF-7 with IC50 values in the micromolar range. Treatment of LNCaP and PC3 cells with 1 μM NCGC00244536 decreased the number of S phase cells. In SCID mice, daily treatment with 20 mg/kg NCGC00244536 significantly inhibited the tumor growth as compared to the vehicle-treated group without causing any major toxicity. Tumors harvested from NCGC00244536-treated mice showed a significant amount of cell necrosis, apoptosis, and fibrosis[1]. | ||
| 作用机制 | NCGC00244536 is a potent KDM4 inhibitor. It specifically binds to the domain of KDM4s, significantly suppressing the binding of KDM4B to the promoter or enhancer regions of target genes. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.61mL 0.52mL 0.26mL |
13.07mL 2.61mL 1.31mL |
26.15mL 5.23mL 2.61mL |
| 参考文献 |
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