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CPI-455 是一种特异性的泛KDM5抑制剂,对 KDM5A 的IC50为 10 nM。它介导 KDM5 抑制,提高 H3K4me3 的整体水平,有抗肿瘤作用。
CPI-455 是一种特异性的泛KDM5抑制剂,对 KDM5A 的IC50为 10 nM。它介导 KDM5 抑制,提高 H3K4me3 的整体水平,有抗肿瘤作用。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 297 | 现货 | |
2 mg | ¥ 439 | 现货 | |
5 mg | ¥ 693 | 现货 | |
10 mg | ¥ 1,130 | 现货 | |
25 mg | ¥ 2,180 | 现货 | |
50 mg | ¥ 3,320 | 现货 | |
100 mg | ¥ 4,730 | 现货 | |
500 mg | ¥ 9,790 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 683 | 现货 |
产品描述 | CPI-455 is a specific KDM5 inhibitor. |
靶点活性 | KDM5A:10 nM (IC50) |
体外活性 | CPI-455在多种接受标准化疗或靶向治疗的癌症细胞模型中通过抑制KDM5,提高全局H3K4三甲基化水平(H3K4me3),并减少DTPs数量。CPI-455对KDM5蛋白具有高度亲和力。在24小时内,CPI-455和CPI-766能剂量依赖性地提升H3K4me3水平,但不影响H3K4me2。对于3个腺癌乳腺癌细胞系MCF-7、T-47和EFM-19,CPI-455的IC50值分别为35.4、26.19和16.13 μM。 |
细胞实验 | All cell lines were treated with DMSO, CPI-4203 or CPI-455 for 5 d with two changes of medium and drug. Thereafter, the cells (PC9, Colo205, Hs888, M14, SKBR3 and EVSA-T) were plated at 2×105 cells in six-well plates in triplicate and treated for an additional 9-15 d, depending on the cell line model. The Incucyte HD imaging system was used to monitor numbers of drug-tolerant cells after cells were stained with Nuclear-ID Red stain. (Only for Reference) |
别名 | CPI-455 HCl |
分子量 | 278.31 |
分子式 | C16H14N4O |
CAS No. | 1628208-23-0 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
溶解度信息 | H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 5.63 mg/mL (20.21 mM) | |||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||
DMSO
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