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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 | ¥ 282 | In stock | |
| 2 mg | ¥ 417 | In stock | |
| 5 mg | ¥ 658 | In stock | |
| 10 mg | ¥ 1,070 | In stock | |
| 25 mg | ¥ 2,070 | In stock | |
| 50 mg | ¥ 2,980 | In stock | |
| 100 mg | ¥ 4,490 | In stock | |
| 200 mg | ¥ 6,290 | In stock | |
| 1 mL x 10 mM (in DMSO) | ¥ 649 | In stock |
CPI-455 相关产品
| 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) |
| 分子量 | 278.31 |
| 分子式 | C16H14N4O |
| CAS No. | 1628208-23-0 |
| Smiles | CC(C)c1c([nH]c2c(cnn2c1=O)C#N)-c1ccccc1 |
| 密度 | 1.28 g/cm3 (Predicted) |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| 溶解度信息 | H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 5.63 mg/mL (20.23 mM), Sonication is recommended. | |||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (3.59 mM), Sonication is recommended. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 | |||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||
DMSO
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