GLPG0634 analogue
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
GLPG0634是一种强效的和选择性的JAK1抑制剂,作用于JAK1\ JAK2\JAK3和TYK2的IC50值分别为10 nM\28 nM\810 nM和116 nM[1].
Janus激酶1(JAK1)是JAK家族的成员之一,并且是一种非受体酪氨酸激酶.JAKs在免疫系统中起重要作用.JAK1是治疗免疫炎性疾病的潜在靶点[1].
GLPG0634是一种强效的和选择性的JAK1抑制剂.GLPG0634抑制JAK1\ JAK2\JAK3和TYK2,IC50值分别为10 nM\28 nM\810 nM和116 nM.在CD4 + T细胞中,GLPG0634显著减少IL-6诱导的STAT1磷酸化,IC50值为629 nM,这表明对JAK 1的抑制.在CD33 + T细胞中,GLPG0634降低GM-CSF诱导的STAT5磷酸化,IC50值为17.5 μM,这表明对JAK2的抑制.GLPG0634抑制分别由IL-4和IL-12介导的Th1和Th2细胞的分化.此外,GLPG0634抑制由TGF-β\IL-23\IL-6和IL-1β诱导的Th17分化[1].
在大鼠中,GLPG0634显著降低由IFN-α-JAK1/TYK2信号调控的Mx2的mRNA水平.在胶原诱导的关节炎(CIA)大鼠模型中,GLPG0634显著减少炎性细胞浸润并降低IL-6\IP-10\XCL1和MCP-1的水平[1].
参考文献：
[1]. Van Rompaey L, Galien R, van der Aar EM, et al. Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases. J Immunol, 2013, 191(7): 3568-3577.
| Physical Appearance | A solid |
| Storage | Desiccate at -20°C |
| M.Wt | 410.43 |
| Cas No. | 1206101-20-3 |
| Formula | C23H18N6O2 |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥31.67 mg/mL in DMSO with gentle warming |
| Chemical Name | (E)-N-(5-(4-((6-cyanopyridin-3-yl)methoxy)phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2(3H)-ylidene)cyclopropanecarboxamide |
| SDF | Download SDF |
| Canonical SMILES | N#CC1=NC=C(COC2=CC=C(C3=CC=CC4=N/C(NN34)=N\C(C5CC5)=O)C=C2)C=C1 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 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。 |
| Description | GLPG0634是一种选择性JAK1抑制剂,作用于JAK1\JAK2\JAK3和TYK2的IC50分别为10 nM\28 nM\810 nM和116 nM. | |||||
| 靶点 | JAK1 | JAK2 | TYK2 | JAK3 | ||
| IC50 | 10 nM | 28 nM | 116 nM | 810 nM | ||
质量控制和MSDS
- 批次:
化学结构
