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S84784

TN1

源叶(MedMol) 98%
  • 英文名:
  • TN1
  • 别名:
  • CAS号:
  • 289479-94-3
  • 分子式:
  • C29H31N7O2
  • 分子量:
  • 509.6021
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源叶(MedMol) S84784-1mg 98% ¥1100.00元 预计交期:2-3天 - - - EA 加入购物车
源叶(MedMol) S84784-5mg 98% ¥3500.00元 预计交期:2-3天 - - - EA 加入购物车
源叶(MedMol) S84784-10mg 98% ¥5000.00元 预计交期:2-3天 - - - EA 加入购物车
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  • 提示:详情请下载说明书。
  • 产品描述: TN1 is a potent fetal hemoglobin (HbF) inducer.
  • 靶点: fetal hemoglobin (HbF)
  • 体外研究:
    A high-throughput screen of a large chemical library identifies a 2,6-diamino-substituted purine, TN1, which induces fetal hemoglobin (HbF) more potently than hydroxyurea in KU812 and K562 leukemia cell lines.TN1 increases HbF protein in both leukemic KU812 and K562 cells in a dose-dependent manner. At 100 nM concentration, Western blot analysis indicated that TN1 increased γ-globin expression (2.9- and 3.7-fold increase in KU812 cell and K562 cell, respectively) to higher levels than 50-100 μM HU (1.8- and 1.9-fold increase in KU812 cell and K562 cell, respectively), the first drug approved for the treatment of SCD. The EC50 value for TN1-mediated HbF induction is approximately three orders of magnitude lower than that of HU (HU: EC50=50-100 μM; TN1: EC50=100 nM). In addition, TN1 is more potent than a number of previously reported small-molecule HbF inducers including sodium butyrate and other histone deacetylase (HDAC) inhibitors. At the concentrations tested, TN1, as well as hemin and HU, increase γ-globin mRNA transcription (greater than fourfold), indicating that TN1 increases γ-globin levels at both the transcriptional and protein level. The time course of TN1-induced γ-globin mRNA and protein synthesis is measured and both increase after approximately 24 h of treatment. TN1 also induces β-globin mRNA in addition to γ-globin mRNA, similar to hydroxyurea
  • 参考文献:
    1. Nam TG, et al. Identification and characterization of small-molecule inducers of fetal hemoglobin. ChemMedChem. 2011 May 2;6(5):777-80.
  • 溶解性: Soluble  in  DMSO
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 1.962 ml 9.812 ml 19.623 ml
    5 mM 0.392 ml 1.962 ml 3.925 ml
    10 mM 0.196 ml 0.981 ml 1.962 ml
    50 mM 0.039 ml 0.196 ml 0.392 ml
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