HLM006474

製品コードS8963 バッチS896301

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
* <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 HLM006474 results in down regulation of total E2F4 protein as well as known E2F targets. The effects of HLM006474 treatment on different cell lines varies, but includes a reduction in cell proliferation and an increase in apoptosis.^[1] HLM006474 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 HLM006474 leads to significant downregulation of E2F4 protein.^[1] Short exposure of Chx10Cre;Rb^f/f;p107^−/− embryos to HLM006474 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 HLM006474 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

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：

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

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。

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