289479-94-3
中文名称 | 289479-94-3 |
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中文同义词 | 化合物 T19583;化合物TN1 |
英文名称 | TN1 |
英文同义词 | TN1;2-Propynamide, N-[3-[[9-ethyl-2-[(trans-4-hydroxycyclohexyl)amino]-9H-purin-6-yl]amino]phenyl]-3-(4-methylphenyl)-;TN1,TN-1 |
CAS号 | 289479-94-3 |
分子式 | C29H31N7O2 |
分子量 | 509.6 |
EINECS号 | |
相关类别 | |
Mol文件 | 289479-94-3.mol |
结构式 |
289479-94-3 性质
密度 | 1.31±0.1 g/cm3(Predicted) |
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储存条件 | Store at -20°C |
溶解度 | DMSO:100 mg/mL (196.23 mM);水:< 0.1 mg/mL(不溶) |
形态 | 固体 |
酸度系数(pKa) | 10.49±0.70(Predicted) |
颜色 | 白色至米白色 |
fetal hemoglobin (HbF)
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.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-100826 | 289479-94-3 TN1 | 289479-94-3 | 5mg | 2900元 |
2024/08/19 | HY-100826 | 289479-94-3 TN1 | 289479-94-3 | 10mM * 1mLin DMSO | 3250元 |