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TN1 

Cat. No.: HY-100826 Purity: 95.14%
Handling Instructions

TN1 is a potent fetal hemoglobin (HbF) inducer.

For research use only. We do not sell to patients.

TN1 Chemical Structure

TN1 Chemical Structure

CAS No. : 289479-94-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 471 In-stock
Estimated Time of Arrival: December 31
1 mg USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

TN1 is a potent fetal hemoglobin (HbF) inducer.

IC50 & Target

fetal hemoglobin (HbF)[1]

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 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].

Molecular Weight

509.60

Formula

C₂₉H₃₁N₇O₂

CAS No.

289479-94-3

SMILES

O=C(NC1=CC=CC(NC2=C3N=CN(CC)C3=NC(N[[email protected]]4CC[[email protected]](O)CC4)=N2)=C1)C#CC5=CC=C(C)C=C5

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (196.23 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9623 mL 9.8116 mL 19.6232 mL
5 mM 0.3925 mL 1.9623 mL 3.9246 mL
10 mM 0.1962 mL 0.9812 mL 1.9623 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.91 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.91 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

Representative images of PBMC culture in the presence of test compounds. PBMC are cultured in methylcellulose medium containing 0.9% methylcellulose, 30% fetal bovine serum (FBS), 2 mM glutamine, 1% deionized bovine serum albumin (BSA), 100 μM 2-mercaptoethanol, 10 ng recombinant human (rh) IL-3, and 3 U/mL rh erythropoietin (EPO) for 16 days in the presence of TN1 (30 nM) or HU (50 μM). HU treatment leads to smaller colonies and inhibition of maturation towards the erythrocyte lineage; b) Western blot of HbF with BFU-E colonies treated with DMSO, TN1 (30 nM), and HU (50 μM) after incubation for 18 days. β-actin is used as an internal control[1].

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

References
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TN1
Cat. No.:
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