STAT5 Inhibitor
(Synonyms: Signal Transducers and Activators of Transcription 5) 目录号 : GC13647
Prevents activation of STAT5 via its SH2 domain
Cas No.:285986-31-4
Sample solution is provided at 25 µL, 10mM.
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STAT5 Inhibitor is a cell-permeable inhibitor of STAT5 with IC50 value of 47 μM against STAT5β SH2 domain EPO peptide binding activity [1].
Signal Transducers and Activators of Transcriptions (STATs) are a family of transcription factors that are primarily activated by membrane receptor-associated Janus kinases (JAK) in response to a large number of extracellular signaling molecules including interferons, cytokines, and growth factors, and mediate many aspects of cellular immunity, proliferation, apoptosis and differentiation [2][3]. STAT5 consists of two isoforms STAT5α and STAT5β and is overactive in several kinds of cancers [1].
STAT5 Inhibitor is a cell-permeable STAT5 inhibitor. STAT5 Inhibitor inhibited STAT5β SH2 domain EPO peptide binding activity with IC50 value of 47 μM and exhibited less potency inhibiting the SH2 domain of STAT1, STAT3, and LCK by 36%, 26% and 7% at 500 μM, respectively [1]. In lysates from K562 cells, STAT5 Inhibitor reduced the concentration of STAT5/STAT5/DNA complex in a dose-dependent way [1].
References:
[1]. Müller J, Sperl B, Reindl W, et al. Discovery of chromone-based inhibitors of the transcription factor STAT5. Chembiochem. 2008 Mar 25;9(5):723-7.
[2]. Leonard WJ, O'Shea JJ. Jaks and STATs: biological implications. Annu Rev Immunol. 1998;16:293-322.
[3]. Schindler C, Darnell JE Jr. Transcriptional responses to polypeptide ligands: the JAK-STAT pathway. Annu Rev Biochem. 1995;64:621-51.
| Cas No. | 285986-31-4 | SDF | |
| 别名 | Signal Transducers and Activators of Transcription 5 | ||
| 化学名 | 2-[(4-oxo-4H-1-benzopyran-3-yl)methylene]hydrazide 3-pyridinecarboxylic acid | ||
| Canonical SMILES | O=C(N/N=C/C1=COC(C=CC=C2)=C2C1=O)C3=CC=CN=C3 | ||
| 分子式 | C16H11N3O3 | 分子量 | 293.3 |
| 溶解度 | ≤5mg/ml in DMSO;2mg/ml in dimethyl formamide | 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 | 3.4095 mL | 17.0474 mL | 34.0948 mL |
| 5 mM | 0.6819 mL | 3.4095 mL | 6.819 mL |
| 10 mM | 0.3409 mL | 1.7047 mL | 3.4095 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
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet