HLM006474

製品コードS8963 バッチS896301

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₂₅H₂₅N₃O₂

分子量

399.48

CAS No.

353519-63-8

Solubility (25°C)*

体外

DMSO

10 mg/mL (25.03 mM)

Water

˂1 mg/mL

Ethanol

˂1 mg/mL

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%DMSO 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 (1.25mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clarified DMSO 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 adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil 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。	2.500mg/ml (6.26mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. 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	HLM006474 is a small molecule pan-E2F inhibitor that inhibits DNA binding to E2F4 with IC50 of 29.8 µM in A375 cells. HLM006474 induces a reduction in cell proliferation and an increase in apoptosis. The CDK/Rb/E2F pathway is commonly disrupted in lung cancer, and HLM006474 is shown to have efficacy in lung cancer.
in vitro	Treatment of multiple cell lines with HLM006474 results in the loss of intracellular E2F4 DNA-binding activity within hours. Overnight exposure to this compound results in down regulation of total E2F4 protein as well as known E2F targets. The effects of this chemical treatment on different cell lines varies, but includes a reduction in cell proliferation and an increase in apoptosis.^[1] This compound reduces the viability of both SCLC and NSCLC lines with a biological IC50 that varies between 15 and 75 mM, but with no significant difference between the groups.^[2]
in vivo	HLM006474 inhibits E2F4 DNA-binding and activity in vivo. In vivo this compound leads to significant downregulation of E2F4 protein.^[1] Short exposure of Chx10Cre;Rb^f/f;p107^−/− embryos to this chemical has a dramatic effect on tumorigenesis. Thus, modest and temporary pharmaceutical E2f inhibition blocks retinoblastoma initiation.^[3]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	3T3 MEFS, A375, MDA-MB-231, MCF7, T47D, HFFs, MDA-MB-468, SK-BR3, 8226-s, 8226-dox40, 8226-MR20
	濃度	0-100 μM
	反応時間	0-24 h
	実験の流れ	Human A375 melanocytes are treated for 9-hrs with the indicated concentration of HLM006474. A375 cells are treated with 40 μM this compound and EMSA and Western analyses performs at the indicated time intervals.
動物実験	動物モデル	Chx10Cre mice, Rb^f/f mice, p107^−/− mice
	投薬量	100 mg/kg
	投与方法	IP

参考

https://pubmed.ncbi.nlm.nih.gov/18676853/
https://pubmed.ncbi.nlm.nih.gov/24831239/
https://pubmed.ncbi.nlm.nih.gov/22286767/

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：

Tribbles pseudokinase 3 drives cancer stemness in oral squamous cell carcinoma cells by supporting the expression levels of SOX2 and EGFR [ Int J Mol Med, 2025, 55(3)44]	PubMed: 39791220
METTL8 links mt-tRNA m3C modification to the HIF1α/RTK/Akt axis to sustain GBM stemness and tumorigenicity [ Cell Death Dis, 2024, 15(5):338]	PubMed: 38744809
E2F and STAT3 provide transcriptional synergy for histone variant H2AZ activation to sustain glioblastoma chromatin accessibility and tumorigenicity [ Cell Death Differ, 2022, 10.1038/s41418-021-00926-5]	PubMed: 35058574

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。