| CAS NO: | 285986-31-4 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 293.3 |
| Cas No. | 285986-31-4 |
| Formula | C16H11N3O3 |
| Synonyms | Signal Transducers and Activators of Transcription 5 |
| Solubility | ≥9.58 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
| Chemical Name | 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 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
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.
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