TN1
目录号 : GC34024
TN1是一种有效的胎儿型血红蛋白(HbF)诱导剂。
Cas No.:289479-94-3
Sample solution is provided at 25 µL, 10mM.
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TN1 is a potent fetal hemoglobin (HbF) inducer.
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].
[1]. Nam TG, et al. Identification and characterization of small-molecule inducers of fetal hemoglobin. ChemMedChem. 2011 May 2;6(5):777-80.
Cell experiment: | 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]. |
References: [1]. Nam TG, et al. Identification and characterization of small-molecule inducers of fetal hemoglobin. ChemMedChem. 2011 May 2;6(5):777-80. | |
| Cas No. | 289479-94-3 | SDF | |
| Canonical SMILES | O=C(NC1=CC=CC(NC2=C3N=CN(CC)C3=NC(N[C@H]4CC[C@H](O)CC4)=N2)=C1)C#CC5=CC=C(C)C=C5 | ||
| 分子式 | C29H31N7O2 | 分子量 | 509.6 |
| 溶解度 | DMSO : 100 mg/mL (196.23 mM);Water : < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet