HTH-01-015

製品コードS7318 バッチS731802

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₆H₂₈N₈O
	分子量	468.55	CAS No.	1613724-42-7
Solubility (25°C)*	体外	DMSO	93 mg/mL warmed with 50ºC water bath (198.48 mM)
		Ethanol	47 mg/mL (100.3 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.

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生物活性

製品説明	HTH-01-015 is a potent and selective NUAK1 inhibitor with IC50 of 100 nM, >100-fold selectivity over NUAK2.
in vitro	In HEK-293 cells express NUAK1 as well as NUAK2, HTH-01-015 suppresses NUAK1-mediated MYPT1 phosphorylation. HTH-01-015 suppresses cell migration In NUAK1+/+ MEFs, and inhibit U2OS cell invasion. Moreover, HTH-01-015 inhibits cell proliferation in both cell lines. ^[1] HTH-01-015 inhibitors markedly restricted cells from entering into mitosis in U2OS cells. ^[2]

プロトコル(参考用のみ)

キナーゼアッセイ	Kinase activity assays
キナーゼアッセイ	In vitro activities of purified GST–NUAK1 and GST–NUAK1[A195T] are measured using Cerenkov counting of incorporation of radioactive 32P from [γ-³²P]ATP into Sakamototide substrate peptide. Reactions are carried out in a 50 μL reaction volume for 30 min at 30°C and reactions are terminated by spotting 40 μL of the reaction mix on to P81 paper and immediately immersing in 50 mM orthophosphoric acid. Samples are washed three times in 50 mM orthophosphoric acid followed by a single acetone rinse and air drying. The kinase-mediated incorporation of [γ-³²P]ATP into Sakamototide is quantified by Cerenkov counting. One unit of activity is defined as that which catalyses the incorporation of 1 nmol of [³²P]phosphate into the substrate over 1 h.
細胞アッセイ	細胞株	U2OS cells and MEFs
	濃度	10 μM
	反応時間	5 days
	実験の流れ	Cell proliferation assays are carried out colorimetrically in 96-well plates using the CellTiter 96® AQueous Non-Radioactive Cell Proliferation Assay kit following the manufacturer's protocol. Initially, 2000 cells per well are seeded for U2OS cells and 3000 cells per well are seeded for MEFs. The proliferation assays are carried out over 5 days in the presence or absence of 10 μM HTH-01-015.

参考

カスタマーフィードバック

: Data from [Data independently produced by , , Brain Behav Immun, 2017, doi: 10.1016/j.bbi.2017.11.003]

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：

Localized Inhibition of Protein Phosphatase 1 by NUAK1 Promotes Spliceosome Activity and Reveals a MYC-Sensitive Feedback Control of Transcription. [ Mol Cell, 2020, 77(6):1322-1339]	PubMed: 32006464
Development of MAP4 Kinase Inhibitors as Motor Neuron-Protecting Agents. [ Cell Chem Biol, 2019, 10.1016/j.chembiol.2019.10.005]	PubMed: 31676236
Functional genomics identifies specific vulnerabilities in PTEN-deficient breast cancer [ Breast Cancer Res, 2018, 20(1):22]	PubMed: 29566768

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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