CPI-455

製品コードS6389 バッチS638902

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₁₆H₁₄N₄O

分子量

278.31

CAS No.

1628208-23-0

Solubility (25°C)*

体外

DMSO

56 mg/mL (201.21 mM)

Ethanol

5 mg/mL (17.96 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%absolute ethyl alcohol 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.500mg/ml (1.80mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clarified absolute ethyl alcohol stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to make it clear. Volume up to 1 mL. The mixed solution should be used immediately for optimal results.

* <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.

溶剤液（一定の濃度）を調合する

生物活性

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.
in vitro	This compound 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 this compound to selectively targets H3K4-specific JmjC demethylases. This compound increases CXCL11, CXCL9, and CXCL10 following infection, with maximum levels observed 48 hours after infection.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Melanoma (M14) cell lines, breast cancer (SKBR3) cell lines, NSCLC (PC9) cell lines
	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.
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.

参考

https://pubmed.ncbi.nlm.nih.gov/27214401/
https://www.science.org/doi/full/10.1126/scitranslmed.aag2112

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

HIF-independent oxygen sensing via KDM6A regulates ferroptosis [ Mol Cell, 2025, 85(15):2973-2987.e6]	PubMed: 40712585
Histone methyltransferases MLL2 and SETD1A/B play distinct roles in H3K4me3 deposition during the transition from totipotency to pluripotency [ EMBO J, 2024, 44(2):437-456.]	PubMed: 39639179
Patient derived tumoroids of high grade neuroendocrine neoplasms for more personalized therapies [ NPJ Precis Oncol, 2024, 8(1):59]	PubMed: 38429350
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。