Tenovin-6 Hydrochloride 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 Hydrochloride 也能抑制二氢乳清酸脱氢酶(DHODH)。
| 生物活性 | Tenovin-6 Hydrochloride, an analog of Tenovin-1 (HY-13423), is an activator ofp53transcriptional activity. Tenovin-6 Hydrochloride inhibits the protein deacetylase activities of purified humanSIRT1,SIRT2, andSIRT3with IC50s of 21 μM, 10 μM, and 67 μM, respectively. Tenovin-6 Hydrochloride also inhibitsdihydroorotate dehydrogenase(DHODH)[1][2]. |
| IC50& Target[1] | SIRT2 10 μM (IC50) | SIRT1 21 μM (IC50) | SIRT3 67 μM (IC50) | HDAC8 | MDM-2/p53 |
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体外研究
(In Vitro) | Tenovin-6 Hydrochloride 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 Hydrochloride rapidly increases the levels of endogenous K382-Ac p53 in MCF-7 cells[1].
Tenovin-6 Hydrochloride (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 Hydrochloride 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 Hydrochloride 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 Hydrochloride inhibits autophagy does not correlate with p53 activation and SIRT1/2 inhibition by knockdown or knockout cannot mimic the effect of Tenovin-6 Hydrochloride on LC3B accumulation[3].
Tenovin-6 Hydrochloride (0, 1, 2.5, 5 or 10 μM) potently inhibits cell proliferation in a dose- and time-dependent manner in all OCI-Ly1, DHL-10, U2932, RIVA, HBL1 and OCI-Ly10 cell lines. Tenovin-6 Hydrochloride consistently increases LC3B-II level in DLBCL cell lines by inhibiting the classical autophagy pathway, without activating p53, and the increase is independent of SIRT1/2/3 and p53. Tenovin-6 Hydrochloride induces apoptosis through the extrinsic cell-death pathway[4.
Tenovin-6 Hydrochloride suppresses the growth of UM cells with IC50 of 12.8 μM, 11.0 μM, 14.58 μM and 9.62 μM for 92.1, Mel 270, Omm 1 and Omm 2.3 cells, respectively[5].
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体内研究
(In Vivo) | Tenovin-6 Hydrochloride (50 mg/kg, i.p.) inhibits the growth of tumor in mice[1].
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : ≥ 49 mg/mL(99.78 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 2.0363 mL | 10.1814 mL | 20.3629 mL | | 5 mM | 0.4073 mL | 2.0363 mL | 4.0726 mL | | 10 mM | 0.2036 mL | 1.0181 mL | 2.0363 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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