TN1 是一种有效的胎儿型血红蛋白 (HbF) 诱导剂。

TN1 is a potent inducer of fetal hemoglobin (HbF).

TN1 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[1].

289479-94-3

C29H31N7O2

509.6

TN1

DMSO:90.0 mg/mL (176.6 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years