TN1 - 10mM in DMSO , CAS No.289479-94-3

CAS: 289479-94-3 Cat. No.: T656904 Formula: C₂₉H₃₁N₇O₂ Peso molecolare: 509.60 PubChem CID: 69828124

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Panoramica

TN1 is a potent fetal hemoglobin ( HbF ) inducer.

In Vitro

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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IC50& Target:fetal hemoglobin (HbF)

Specifications

Specifiche e purezza

10mM in DMSO

Meccanismi biochimici e fisiologici

TN1 is a potent fetal hemoglobin ( HbF ) inducer.

Condizioni di conservazione di stoccaggio

Store at -80°C

Spedito in

Dry ice packs + Cold packs

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Nomi e identificatori

• Isomeri SMILES: CCN1C=NC2=C(N=C(N=C21)NC3CCC(CC3)O)NC4=CC(=CC=C4)NC(=O)C#CC5=CC=C(C=C5)C
• PubChem CID: 69828124
• Peso molecolare: 509.60