CPI-455 是一种特异性的泛KDM5抑制剂，对 KDM5A 的IC50为 10 nM，CPI-455 介导 KDM5 抑制，提高 H3K4me3 的整体水平，并减少多肿瘤细胞系模型中耐药的持久癌细胞的数量。
| 生物活性 | CPI-455 is a specific, pan-KDM5inhibitor with anIC50of 10 nM for KDM5A. CPI-455 mediatesKDM5inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persistercancercells in multiplecancercell line models treated with standard chemotherapy or targeted agents[1]. |
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体外研究
(In Vitro) | CPI-455 mediates KDM5 inhibition, elevates global levels of H3K4 trimethylation (H3K4me3) and decreases the number of DTPs in multiple cancer cell line models treated with standard chemotherapy or targeted agents[1].
CPI-455, with high measured affinity for the target KDM5 proteins. Within 24 hours, increases in H3K4me3, are observed after exposure to either of the two active compounds, CPI-455 and CPI-766, in a dosedependent manner. IC50calculation for KDM5 Inhibitor CPI0455 in 3 luminal breast cancer cell lines MCF-7, T-47 and EFM-19 are 35.4, 26.19 and 16.13 μM, respectively[2].
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体内研究
(In Vivo) | Dual blockade of B7-H4 and KDM5B (CPI-455, 50/70 mg/kg, ip, daily) in mice elicits protective immunity[2].
| Animal Model: | Six-week-old male C57BL/6 mice (One- to 2-mm fragments ofP. gingivalis–positive PDXs were implanted subcutaneously into the flank region of humanized mice.) | | Dosage: | 50 mg/kg or 70 mg/kg (combined with anti–B7-H4). | | Administration: | IP, daily, 14-28 days. | | Result: | Histopathology analysis revealed no inflammation in either group at 2 weeks in response to the primary infection. However, at 8 weeks after inoculation, mice receiving monotherapy exhibited mild inflammation, whereas the combined treatment presented with heavy to severe inflammation, which persisted at 12 and 16 weeks after challenge.
Treatment with CPI-455 to selectively target H3K4-specific JmjC demethylases increased CXCL11, CXCL9, and CXCL10 following infection, with maximum levels observed 48 hours after infection.
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : ≥ 34 mg/mL(122.17 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 3.5931 mL | 17.9656 mL | 35.9312 mL | | 5 mM | 0.7186 mL | 3.5931 mL | 7.1862 mL | | 10 mM | 0.3593 mL | 1.7966 mL | 3.5931 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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