289479-94-3
基本信息
化合物 T19583
2-Propynamide, N-[3-[[9-ethyl-2-[(trans-4-hydroxycyclohexyl)amino]-9H-purin-6-yl]amino]phenyl]-3-(4-methylphenyl)-
物理化學(xué)性質(zhì)
報價日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
2024/11/08 | HY-100826 | 289479-94-3 TN1 | 289479-94-3 | 5mg | 2900元 |
2024/11/08 | HY-100826 | 289479-94-3 TN1 | 289479-94-3 | 10mM * 1mLin DMSO | 3250元 |
2024/11/08 | HY-100826 | 289479-94-3 TN1 | 289479-94-3 | 10mg | 4200元 |
常見問題列表
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.