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289479-94-3

中文名稱 289479-94-3
英文名稱 TN1
CAS 289479-94-3
分子式 C29H31N7O2
分子量 509.6
MOL 文件 289479-94-3.mol
更新日期 2024/12/03 15:40:34
289479-94-3 結(jié)構(gòu)式 289479-94-3 結(jié)構(gòu)式

基本信息

中文別名
化合物TN1
化合物 T19583
英文別名
TN1
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)

密度1.31±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度DMSO : 100 mg/mL (196.23 mM);Water : < 0.1 mg/mL (insoluble)
酸度系數(shù)(pKa)10.49±0.70(Predicted)
形態(tài)Solid
顏色White to off-white
289479-94-3價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08HY-100826289479-94-3
TN1
289479-94-35mg2900元
2024/11/08HY-100826289479-94-3
TN1
289479-94-310mM * 1mLin DMSO3250元
2024/11/08HY-100826289479-94-3
TN1
289479-94-310mg4200元

常見問題列表

生物活性
TN1 是一種有效的胎兒型血紅蛋白 (HbF) 誘導(dǎo)劑。
靶點

fetal hemoglobin (HbF)

體外研究

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.

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