UBCS039

• 常用名: UBCS039
• 英文名: UBCS039
• CAS号: 358721-70-7
• 分子量: 247.29
• 密度: N/A
• 沸点: N/A
• 分子式: C₁₆H₁₃N₃
• 熔点: N/A
• 闪点: N/A

UBCS039用途

UBCS039 是首个合成的,SIRT6 的特异性抑制剂,可在人癌细胞中诱导自噬,其EC50 值为38 μM.

UBCS039名称

• 中文名: UBCS039
• 英文名: UBCS039

UBCS039生物活性

• 描述: UBCS039 是首个合成的,SIRT6 的特异性抑制剂,可在人癌细胞中诱导自噬,其EC50 值为38 μM.
• 相关类别:
  信号通路 >> 表观遗传学 >> 抗衰老酶
  研究领域 >> 癌症
  信号通路 >> 细胞周期/DNA损伤 >> 抗衰老酶
• 靶点实验:

  SIRT6:38 μM (EC50)

• 体外研究: UBCS039(75μM,48或72小时)诱导人癌细胞中SIRT6靶向组蛋白H3位点的脱乙酰化[2]。 UBCS039导致人癌细胞中的自噬体积累[2]。 UBCS039通过AMP激活的蛋白激酶(AMPK)信号通路激活诱导自噬[2]。蛋白质印迹分析[2]细胞系：人H1299细胞。浓度：75μM。孵化时间：48小时和72小时。结果：诱导人H1299细胞中SIRT6靶向组蛋白H3位点的脱乙酰化。蛋白质印迹分析[2]细胞系：人H1299细胞。浓度：75μM。孵化时间：48小时和72小时。结果：诱导人H1299细胞中SIRT6靶向组蛋白H3位点的脱乙酰化。细胞增殖测定[2]细胞系：人H1299细胞。浓度：100μM。孵化时间：48小时和72小时。结果：与对照或DMSO处理的细胞相比,在H1299和HeLa细胞系中从生长的第3天(处理后48小时)开始,以剂量依赖性方式引起细胞增殖的强烈降低。
• 参考文献:

  [1]. Led to a strong decrease of cell proliferation in a dose-dependent manner when compared with control or DMSO-treated cells, starting from day 3 of growth (48 h after treatment) in both H1299 and HeLa cell lines.

  [2]. Sara Iachettini, et al. Pharmacological activation of SIRT6 triggers lethal autophagy in human cancer cells. Cell Death and Disease (2018) 9:996.

UBCS039物理化学性质

• 分子式: C₁₆H₁₃N₃
• 分子量: 247.29
• InChIKey: BSOBGTYXYGHUTD-UHFFFAOYSA-N
• SMILES: c1cncc(C2Nc3ccccc3-n3cccc32)c1
• 储存条件: 2-8℃

UBCS039靶点实验

查看更多实验

实验名称：Discovery of Small Molecules to Inhibit Human Cytomegalovirus Nuclear Egress 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School 靶标：HCMV UL50 External Id：HMS1262

实验名称：Activation of SIRT6 (unknown origin) deacetylase activity assessed as maximal activat... 来源：ChEMBL 靶标：NAD-dependent protein deacylase sirtuin-6 External Id：CHEMBL5227972

实验名称：Activation of recombinant SIRT6 (unknown origin) deacetylase activity using fluorogen... 来源：ChEMBL 靶标：NAD-dependent protein deacylase sirtuin-6 External Id：CHEMBL5355677

实验名称：Cytotoxicity against human A549-ACE2 cells assessed as inhibition of cell growth meas... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5355707

实验名称：A screen for compounds that inhibit the activity of LtaS in Staphylococcus aureus 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School External Id：HMS979

实验名称：Antiviral activity against SARS-CoV-2 infected in human A549-ACE2 cells assessed as v... 来源：ChEMBL 靶标：Severe acute respiratory syndrome coronavirus 2 External Id：CHEMBL5355706

实验名称：Activation of SIRT6 (unknown origin) deacetylase activity assessed as fold increase i... 来源：ChEMBL 靶标：NAD-dependent protein deacylase sirtuin-6 External Id：CHEMBL5355674

实验名称：A screen for compounds that inhibit viral RNA polymerase binding and polymerization a... 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School 靶标：Chain A, Poliovirus Polymerase With Gtp External Id：HMS750

实验名称：Antiinflammatory activity against LPS-induced mouse BV-2 cells assessed as reduction ... 来源：ChEMBL 靶标：BV-2 External Id：CHEMBL5355697

实验名称：Antiinflammatory activity against LPS-induced mouse BV-2 cells assessed as reduction ... 来源：ChEMBL 靶标：BV-2 External Id：CHEMBL5355695

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