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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder | ||||||||
化学式 | C16H14N4O |
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分子量 | 278.31 | CAS No. | 1628208-23-0 | ||||||||
Solubility (25°C)* | 体外 | Ethanol | 5 mg/mL (17.96 mM) | ||||||||
DMSO | Insoluble | ||||||||||
Water | Insoluble | ||||||||||
体内 (毎回新しく調製した物を用意してください) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | CPI-455 is a specific KDM5 inhibitor with an IC50 of 10 nM for full-length KDM5A in enzymatic assays. CPI-455 shows over 200-fold selectivity for KDM5 relative to KDM2, 3, 4, 6, and 7 enzymes. |
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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] |
in vivo | Dual blockade of B7-H4 and KDM5B (CPI-455, 50/70 mg/kg, ip, daily) in mice elicits protective immunity. Treatment with CPI-455 to selectively targets H3K4-specific JmjC demethylases. CPI-455 increases CXCL11, CXCL9, and CXCL10 following infection, with maximum levels observed 48 hours after infection. |
細胞アッセイ | 細胞株 | Melanoma (M14) cell lines, breast cancer (SKBR3) cell lines, NSCLC (PC9) cell lines |
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濃度 | 6.25-25 μM | |
反応時間 | 4 days, 5 days | |
実験の流れ | Cells are plated in 6-well plates and treated with various concentrations of CPI-455 for up to 4 d. Cells are collected at various time points, and global levels of H3K4me3 and total H3 are determined using MSD ELISA. |
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動物実験 | 動物モデル | Six-week-old male C57BL/6 mice (One- to 2-mm fragments of P. gingivalis –positive PDXs are implanted subcutaneously into the flank region of humanized mice.) |
投薬量 | 50 mg/kg, 70 mg/kg | |
投与方法 | i.p. |
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Priming therapy by targeting enhancer-initiated pathways in patient-derived pancreatic cancer cells [ EBioMedicine, 2023, 92:104602] | PubMed: 37148583 |
Epigenetically suppressed tumor cell intrinsic STING promotes tumor immune escape [ Biomed Pharmacother, 2023, 157:114033] | PubMed: 36436495 |
Epigenetic alterations of CXCL5 in Cr(VI)-induced carcinogenesis [ Sci Total Environ, 2022, 838(Pt 1):155713] | PubMed: 35660107 |
pncCCND1_B Engages an Inhibitory Protein Network to Downregulate CCND1 Expression upon DNA Damage [ Cancers (Basel), 2022, 14(6)1537] | PubMed: 35326688 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。