Pyridone 6
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.
Pyridone 6(吡啶酮6)是一种可逆的和选择性的 ATP竞争性Janus活化激酶(JAK)抑制剂,IC50值为1-15 nM[1]。
JAK是一种酪氨酸激酶家族,是JAK-STAT信号传导途径的组成部分。细胞因子(如白介素和干扰素)或生长因子(如GH和EGF)与相关受体的结合导致受体的二聚化。二聚化可触发JAK的活化(自磷酸化),其与受体相结合。活化JAK引起的受体磷酸化可吸引STAT与受体相结合,并被JAK所激活。最后,激活的STAT进入细胞核,调节基因转录。JAK和STAT的持续激活可促进异常的细胞增殖。对JAK的抑制被认为是治疗恶性肿瘤的一种有效疗法。
Pyridone 6是一种有效的JAK抑制剂,抑制JAK1、JAK2、JAK3和TYK2的活性,IC50值分别为15 nM、1 nM、5 nM和1 nM。Pyridone 6也是一种选择性的JAK抑制剂,对其它激酶的IC50值超过130 nM[1,2,3]。
在B9细胞中,pyridone 6在250 nM浓度时显著减少IL-6诱导的STAT3的磷酸化,在1 μM时几乎完全抑制STAT3的磷酸化。此外,pyridone 6抑制细胞增殖,IC50值为250 nM。在U266细胞中,pyridone 6引起细胞生长的适度减少和G1期停滞,这与U266细胞的生长部分依赖于IL-6信号是一致的[1]。
Pyridone 6具有低的水溶性,因此,pyridone 6和乙醇酸的聚乳酸制剂通常被用于动物模型中。在特应性皮炎小鼠模型中,pyridone 6通过修饰Th细胞的分化和抑制肥大细胞的功能,从而具有治疗活性[2]。
参考文献:
1. Pedranzini L, Dechow T, Berishaj M, et al. Pyridone 6, a pan-Janus–activated kinase inhibitor, induces growth inhibition of multiple myeloma cells. Cancer research, 2006, 66(19): 9714-9721.
2. Nakagawa R, Yoshida H, Asakawa M, et al. Pyridone 6, a pan-JAK inhibitor, ameliorates allergic skin inflammation of NC/Nga mice via suppression of Th2 and enhancement of Th17. The Journal of Immunology, 2011, 187(9): 4611-4620.
3. Kwak H B, Kim H S, Lee M S, et al. Pyridone 6, A Pan-Janus-Activated Kinase Inhibitor, Suppresses Osteoclast Formation and Bone Resorption through Down-Regulation of Receptor Activator of Nuclear Factor-. KAPPA. B (NF-. KAPPA. B) Ligand (RANKL)-Induced c-Fos and Nuclear Factor of Activated T Cells (NFAT) c1 Expression. Biological and Pharmaceutical Bulletin, 2009, 32(1): 45-50.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 309.34 |
Cas No. | 457081-03-7 |
Formula | C18H16FN3O |
Synonyms | CMP 6; JAK Inhibitor |
Solubility | insoluble in H2O; ≥15.45 mg/mL in DMSO; ≥5.92 mg/mL in EtOH with gentle warming and ultrasonic |
Chemical Name | 2-(tert-butyl)-9-fluoro-1H-benzo[h]imidazo[4,5-f]isoquinolin-7(6H)-one |
SDF | Download SDF |
Canonical SMILES | CC(C)(C)C(N1)=NC2=C1C3=C(C4=C2C=CNC4=O)C=C(F)C=C3 |
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。 |
质量控制和MSDS
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