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CAS No. : 1011557-82-6
MCE 国际站:Tenovin-6
产品活性: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)。
研究领域:Apoptosis | Metabolic Enzyme/Protease | Cell Cycle/DNA Damage | Epigenetics | Autophagy
作用靶点:MDM-2/p53 | Dihydroorotate Dehydrogenase | Sirtuin | Autophagy
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 accumulation.
Tenovin-6 (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 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 induces apoptosis through the extrinsic cell-death pathway.
Tenovin-6 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.
In Vivo: Tenovin-6 (50 mg/kg, i.p.) inhibits the growth of tumor in mice.
相关产品:Bioactive Compound Library Plus | Apoptosis Compound Library | Cell Cycle/DNA Damage Compound Library | Epigenetics Compound Library | Metabolism/Protease Compound Library | Histone Modification Research Compound Library | Anti-Cancer Compound Library | Autophagy Compound Library | Anti-Aging Compound Library | Antioxidant Compound Library | Reprogramming Compound Library | Oxygen Sensing Compound Library | Ferroptosis Compound Library | Pyroptosis Compound Library | Glutamine Metabolism Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | Anti-Cancer Metabolism Compound Library | Mitochondria-Targeted Compound Library | Transcription Factor-Targeted Library | Anti-Colorectal Cancer Compound Library | Farudodstat | E1231 | Cambinol | DHODH-IN-21 | p53 (17-26) | p53 and MDM2 proteins-interaction-inhibitor (racemic) | PROTAC Sirt2 Degrader-1 | Navtemadlin | Antitumor agent-60 | Roslin 2 bromide | Resveratrol | Amifostine trihydrate | SRT 1720 Hydrochloride | MX69 | ADH-6 TFA | RG7112 | SCH529074 | CBL0137 hydrochloride | MA242 | SIRT-IN-3 | MD-224 | DHODH-IN-23 | MB710 | NSC59984 | MDM2/4-p53-IN-1 | Oxychlororaphine | Pifithrin-β hydrobromide | p53-MDM2-IN-1 | SRT 2104 | PK11000
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