Tenovin-6|1011557-82-6|-陌孚医药/Medlife

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Tenovin-6

目录号: PL04447 纯度: ≥98%

CAS No. :1011557-82-6

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中文名称	Tenovin-6
中文别名	Tenovin-6 抑制剂;TENOVIN-6, SIRT 抑制剂和 P53 激活剂
英文名称	Tenovin-6
英文别名	Tenovin-6;Tenovin 6;4-TERT-BUTYL-N-(4-(5-(DIMETHYLAMINO)PENTANAMIDO)PHENYLCARBAMOTHIOYL)BENZAMIDE HYDROCHLORIDE;N-[[[4-[[5-(Dimethylamino)-1-oxopentyl]amino]phenyl]amino]thioxomethyl]-4-(1,1-dimethylethyl)benzamide;4-(tert-Butyl)-N-((4-(4-(dimethylamino)butanamido)phenyl)carbAmothioyl)benzamide;Benzamide, N-[[[4-[[5-(dimethylamino)-1-oxopentyl]amino]phenyl]amino]thioxomethyl]-4-(1,1-dimethylethyl)-;N-[[[4-[[5-(Dimethylamino)-1-oxopentyl]amino]phenyl]amino]thioxomethyl]-4-(1,1-dimethylethyl)benzamide Tenovin-6
Cas No.	1011557-82-6
分子式	C₂₅H₃₄N₄O₂S
分子量	454.63
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	Tenovin-6 是 Tenovin-1 (HY-13423) 的类似物，是一种 p53 转录活性的激活剂。Tenovin-6 Hydrochloride 抑制纯化人 SIRT1、SIRT2 和 SIRT3 蛋白脱乙酰酶活性，IC₅₀ 分别为 21 μM、10 μM 和 67 μM。Tenovin-6 也能抑制二氢乳清酸脱氢酶 (DHODH)。
生物活性	Tenovin-6, an analog of Tenovin-1 (HY-13423), is an activator of p53 transcriptional activity. Tenovin-6 inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 with IC 50 s of 21 μM, 10 μM, and 67 μM, respectively. Tenovin-6 also inhibits dihydroorotate dehydrogenase (DHODH).
性状	Solid
IC50 & Target[1][2]	SIRT2 10 μM (IC50) SIRT1 21 μM (IC50
体外研究(In Vitro)	Tenovin-6 inhibits the growth of S. cerevisiae cultures with an IC50 of 30 μM and is more toxic to yeast than the less water-soluble tenovin-1. Tenovin-6 rapidly increases the levels of endogenous K382-Ac p53 in MCF-7 cells. Tenovin-6 (0 to 15?μM) dose dependently increases the level of LC3-II in diverse cell types, and the increase is ATG5/7 dependent. Tenovin-6 treatment also increases the number and intensity of autophagic vesicles with or without the presence of Torin 1, and prevents Torin 1-induced SQSTM1/p62 degradation. Tenovin-6 affects the acidification of autolysosomes and impairs the hydrolytic activity of lysosomes but does not affect the fusion between autophagosomes and lysosomes. That tenovin-6 inhibits autophagy does not correlate with p53 activation and SIRT1/2 inhibition by knockdown or knockout cannot mimic the effect of tenovin-6 on LC3B accu
体内研究(In Vivo)	Tenovin-6 (50 mg/kg, i.p.) inhibits the growth of tumor in mice. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Lain S, et al. Discovery, in vivo activity, and mechanism of action of a small-molecule p53 activator. Cancer Cell. 2008 May;13(5):454-63. [2]. Ladds MJGW, et al. Exploitation of DHODH and p53 activation as therapeutic targets - a case study in polypharmacology [published online ahead of print, 2020 Sep 8]. J Biol Chem. 2020;jbc.RA119.012056.

溶解度数据	In Vitro: DMSO : ≥ 31 mg/mL (68.19 mM)配制储备液

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