compound 3i (666-15)

製品コードS8846 バッチS884601

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₃₃H₃₁Cl₂N₃O₅
	分子量	620.52	CAS No.	1433286-70-4
Solubility (25°C)*	体外	DMSO	100 mg/mL (161.15 mM)
		Ethanol	3 mg/mL (4.83 mM)
		Water	Insoluble
* <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	Compound 3i (666-15)は、CREBを介した遺伝子転写の強力かつ選択的な阻害剤（IC50 = 0.081 ± 0.04 μM）であり、正常細胞に害を与えることなく癌細胞の増殖を強力に阻害します。
in vitro	Compound 3i (666-15) could potently inhibit cancer cell growth. In MDA-MB-231 and MDA-MB-468 cells, the GI50 for this compound is 73 and 46 nM, respectively. In A549 and MCF-7 cells, it exhibits robust activity as well with GI50 of 0.47 and 0.31 μM. It inhibits CREB’s transcription activity in living cells independent of direct CREB or CBP binding interaction.
in vivo	In an in vivo MDA-MB-468 xenograft model, compound 3i (666-15) completely suppresses tumor growth without overt toxicity. Preliminary toxicity studies show that intraperitoneal (ip) injection of 10 mg/kg of it is well tolerated in mice.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	HEK 293T cells
	濃度	0.05, 0.1, 0.5 μM
	反応時間	--
	実験の流れ	After treatment of HEK 293T cells with different concentrations of compound 3i (666-15), forskolin was added, and the relative mRNA level of Nurr1/NR4A2 was determined by qRT-PCR analysis.
動物実験	動物モデル	6- to 8-week old BALB/c nude mouse inoculated subcutaneously at the right flank with MDA-MB-468 cells
	投薬量	10 mg/kg
	投与方法	IP

参考

https://pubmed.ncbi.nlm.nih.gov/26023867/

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：

Transcriptional Repression of CCL2 by KCa3.1 K+ Channel Activation and LRRC8A Anion Channel Inhibition in THP-1-Differentiated M2 Macrophages [ Int J Mol Sci, 2025, 26(15)7624]	PubMed: 40806751
Renalase activates mitochondrial leak metabolism in response to cellular stress and to repair damage after injury [ bioRxiv, 2025, 2025.08.19.671117]	PubMed: 40894758
Characterization of dipyridamole as a novel ferroptosis inhibitor and its therapeutic potential in acute respiratory distress syndrome management [ Theranostics, 2024, 14(18):6947-6968]	PubMed: 39629132
Enforced activation of the CREB/KDM2B axis prevents alcohol-induced embryonic developmental delay [ Cell Rep, 2024, 43(12):115075]	PubMed: 39661511
The PKA-CREB1 axis regulates coronavirus proliferation by viral helicase nsp13 association [ J Virol, 2024, 98(4):e0156523]	PubMed: 38445884
The delta subunit of the GABAA receptor is necessary for the GPT2-promoted breast cancer metastasis [ Theranostics, 2023, 13(4):1355-1369]	PubMed: 36923530
Inhibiting the glycerophosphodiesterase EDI3 in ER-HER2+ breast cancer cells resistant to HER2-targeted therapy reduces viability and tumour growth [ J Exp Clin Cancer Res, 2023, 42(1):25]	PubMed: 36670508
MLK4 promotes glucose metabolism in lung adenocarcinoma through CREB-mediated activation of phosphoenolpyruvate carboxykinase and is regulated by KLF5 [ Oncogenesis, 2023, 12(1):35]	PubMed: 37407566
Paradoxical Induction of ALOX15/15B by Cortisol in Human Amnion Fibroblasts: Implications for Inflammatory Responses of the Fetal Membranes at Parturition [ Int J Mol Sci, 2023, 24(13)10881]	PubMed: 37446059
LIM1 contributes to the malignant potential of endometrial cancer [ Front Oncol, 2023, 13:1082441]	PubMed: 36969081

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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