KG-501

製品コードS8409 バッチS840901

化学情報

	Synonyms	2-naphthol-AS-E-phosphate	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₁₇H1₃ClNO₅P
	分子量	377.72	CAS No.	18228-17-6
Solubility (25°C)*	体外	DMSO	20 mg/mL (52.94 mM)
		Water	Insoluble
		Ethanol	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	KG-501は、cAMP応答配列結合タンパク質（CREB）阻害剤であり、CREB依存性転写（Ki = 10 μM）およびCREB:CBP相互作用（Ki = 50 μM）を阻害します。また、結合アッセイの線形範囲内のCREB濃度を使用し、約90 μMのKiでリン酸化（Ser-133）CREBのKIXへの結合を阻害します。
in vitro	KG-501 inhibits induction of cAMP-responsive genes, at least in part, by blocking the CREB:CBP interaction. The inhibition of the CREB pathway using this compound induces an inhibition of neurite outgrowth and synaptogenesis, as well as a decrease of MAP2+ neuronal cells.
in vivo	KG-501 inhibits CREB, CCL2 expression and ERK phosphorylation, also significantly lowers the cAMP level. CREB might contribute to the neuroprotection opposed neuroinflammation through cAMP/ERK adjustment pathway. This compound significantly promots the neurological outcomes of AOM-treated mice, reduces phosphorylation of ERK and the concentration of cAMP in cortex.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	HEK293T cells
	濃度	5, 10, 25 μM
	反応時間	20 min
	実験の流れ	EVX-1 luciferase reporter plasmid was transfected into HEK293T cells. At 24 h posttransfection, cells were pretreated with the indicated amount of KG-501 or DMSO vehicle for 20 min followed by coincubation with forskolin or DMSO. Cells were harvested at 4 h, and luciferase activity was measured.
動物実験	動物モデル	Murine azoxymethane (AOM) model of hepatic encephalopathy (Adult male C57BL/6 mice)
	投薬量	10, 20, or 50 μM
	投与方法	intracerebroventricular infusion

参考

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC539725/
https://pubmed.ncbi.nlm.nih.gov/25150140/
http://www.ijcep.com/files/ijcep0040171.pdf

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：

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Long non-coding RNA Lnc-408 promotes invasion and metastasis of breast cancer cell by regulating LIMK1 [ Oncogene, 2021, 10.1038/s41388-021-01845-y]	PubMed: 34079084
Recombinant Annexin A2 Administration Improves Neurological Outcomes After Traumatic Brain Injury in Mice [ Front Pharmacol, 2021, 12:708469]	PubMed: 34400908
Cathepsin D deficiency in mammary epithelium transiently stalls breast cancer by interference with mTORC1 signaling [ Nat Commun, 2020, 11(1):5133]	PubMed: 33046706
Cynandione A Alleviates Neuropathic Pain Through α7-nAChR-Dependent IL-10/β-Endorphin Signaling Complexes [ Front Pharmacol, 2020, 11:614450]	PubMed: 33584292

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。