Nexturastat A

製品コードS7473 バッチS747301

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	C₁₉H₂₃ N₃ O₃
	分子量	341.4	CAS No.	1403783-31-2
Solubility (25°C)*	体外	DMSO	68 mg/mL (199.17 mM)
		Ethanol	2 mg/mL (5.85 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	Nexturastat A is a potent and selective HDAC6 inhibitor with IC50 of 5 nM, >190-fold selectivity over other HDACs.
in vitro	In B16 murine melanoma cells, Nexturastat A leads to a dose-dependent increase of acetyl α-tubulin levels without a concomitant elevation of histone H3 acetylation. Moreover, Nexturastat A potently inhibits the growth of B16 melanoma cells with GI50 of 14.3 μM. ^[1]
特徴	Urea-based HDAC6-selective inhibitor.

プロトコル(参考用のみ)

キナーゼアッセイ	HDAC inhibition assays
キナーゼアッセイ	HDAC inhibition assays are performed by Reaction Biology Corp. using isolated human, recombinant full2length HDAC1 and -6 from a baculovirus expression system in Sf9 cells. An acetylated fluorogenic peptide,RHKKAc, derived from residues 379-382 of p53 is used as substrate. The reaction buffer is made up of 50 mM Tris-HCl pH 8.0, 127 mM NaCl, 2.7 mM KCl, 1 mM MgCl₂, 1 mg/mL BSA, and a final concentration of 1% DMSO. Compounds are delivered in DMSO and delivered to enzyme mixture with preincubation of 5-10 min followed by substrate addition and incubation for 2 h at 30°C. Trichostatin A and developer are added to quench the reaction and generate fluorescence, respectively. Dose-response curves are generated starting at 30 μM compound with three-fold serial dilutions to generate a 10-dose plot. IC50 values are then generated from the resulting plots, and the values expressed are the average of duplicate trials ± standard deviation.
細胞アッセイ	細胞株	B16 murine melanoma cells
	濃度	~100 μM
	反応時間	48 hours
	実験の流れ	B16 murine melanoma cells are plated at 5000/well in 96 well flat bottom plates. The following day, media is changed to that containing various concentrations of HDACi or matched DMSO vehicle concentrations diluted in complete medium done in triplicate. Cells are incubated for 48 hours at 37°C and 5% CO2. Density of viable, metabolically active cells is quantified using a standard MTS assay as per manufacturer’s instructions. Briefly, 20μL of reagent are added per well and incubated at 37°C for 3 hours. Absorbances at 490nM are measured spectrophotometrically with background subtraction at 690 nM. All values are then normalized and expressed as a percentage of medium control (100%).

参考

[1] Bergman JA, et al. J Med Chem. 2012, 55(22), 9891-9899.

カスタマーフィードバック

: , , Oncotarget, 2016, 7(23):34384-94

: Data from [Data independently produced by , , Oncotarget, 2016, 7(39):63829-63838]

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：

HDAC Inhibition Induces CD26 Expression on Multiple Myeloma Cells via the c-Myc/Sp1-mediated Promoter Activation [ Cancer Res Commun, 2024, 4(2):349-364]	PubMed: 38284882
Selectivity of Hydroxamate- and Difluoromethyloxadiazole-Based Inhibitors of Histone Deacetylase 6 In Vitro and in Cells [ Int J Mol Sci, 2023, 24(5)4720]	PubMed: 36902164
Decreased expression of airway epithelial Axl is associated with eosinophilic inflammation in severe asthma [ Cancer Res Treat, 2022, 54(2):458-468]	PubMed: 34517693
Histone Deacetylase as a Valuable Predictive Biomarker and Therapeutic Target in Immunotherapy for Non-Small Cell Lung Cancer [ Cancer Res Treat, 2022, 54(2):458-468]	PubMed: 34517693
miR-4286 functions in osteogenesis and angiogenesis via targeting histone deacetylase 3 and alleviates alcohol-induced bone loss in mice [ Cell Prolif, 2021, 54(6):e13054]	PubMed: 33973278
MAPK Pathway Suppression Unmasks Latent DNA Repair Defects and Confers a Chemical Synthetic Vulnerability in BRAF-, NRAS-, and NF1-Mutant Melanomas. [ Cancer Discov, 2019, 9(4):526-545]	PubMed: 30709805
Class I-Histone Deacetylase (HDAC) Inhibition is Superior to pan-HDAC Inhibition in Modulating Cisplatin Potency in High Grade Serous Ovarian Cancer Cell Lines. [ Int J Mol Sci, 2019, 20(12)]	PubMed: 31234549
Continuous Activity Assay for HDAC11 Enabling Reevaluation of HDAC Inhibitors [ ACS Omega, 2019, 4(22):19895-19904]	PubMed: 31788622
The selective HDAC6 inhibitor Nexturastat A induces apoptosis, overcomes drug resistance and inhibits tumor growth in multiple myeloma. [ Biosci Rep, 2019, 39(3)]	PubMed: 30782785
mTOR and HDAC Inhibitors Converge on the TXNIP/Thioredoxin Pathway to Cause Catastrophic Oxidative Stress and Regression of RAS-Driven Tumors [ Cancer Discov, 2017, 7(12):1450-1463]	PubMed: 28963352

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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