289479-94-3
- CAS号:289479-94-3
- 英文名:TN1
- 中文名:289479-94-3
- CBNumber:CB93155072
- 分子式:C29H31N7O2
- 分子量:509.6
- MOL File:289479-94-3.mol
- 密度 :1.31±0.1 g/cm3(Predicted)
- 储存条件 :Store at -20°C
- 溶解度 :DMSO : 100 mg/mL (196.23 mM);Water : < 0.1 mg/mL (insoluble)
- 形态 :Solid
- 酸度系数(pKa) :10.49±0.70(Predicted)
- 颜色 :White to off-white
289479-94-3性质、用途与生产工艺
- 生物活性 TN1 是一种有效的胎儿型血红蛋白 (HbF) 诱导剂。
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靶点
fetal hemoglobin (HbF)
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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 EC 50 value for TN1-mediated HbF induction is approximately three orders of magnitude lower than that of HU (HU: EC 50 =50-100 μM; TN1: EC 50 =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.
- 更新日期:2024/11/08
- 产品编号:HY-100826
- 产品名称:289479-94-3 TN1
- CAS编号:289479-94-3
- 包装:5mg
- 价格:2900元
- 更新日期:2024/11/08
- 产品编号:HY-100826
- 产品名称:289479-94-3 TN1
- CAS编号:289479-94-3
- 包装:10mM * 1mLin DMSO
- 价格:3250元
- 公司名称:Musechem
- 联系电话:+1-800-259-7612
- 电子邮件:info@musechem.com
- 国家:美国
- 产品数:4660
- 优势度:60
- 公司名称:TargetMol Chemicals Inc.
- 联系电话:+1-781-999-5354 +1-00000000000
- 电子邮件:marketing@targetmol.com
- 国家:美国
- 产品数:32161
- 优势度:58
- 公司名称:MedChemExpress
- 联系电话:--
- 电子邮件:sales@medchemexpress.com
- 国家:美国
- 产品数:6398
- 优势度:58