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FM-381
产品别名
FM-381
2-Cyano-3-(5-(1-cyclohexyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-2-yl)furan-2-yl)-N,N-dimethylacrylamide
(E)-2-Cyano-3-(5-(1-cyclohexyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-2-yl)furan-2-yl)-N,N-dimethylacrylamide
结构式
基本信息
| Empirical Formula【经验(实验)分子式】 | C24H24N6O2 |
| Molecular weight | 428.49 |
| NACRES | NA.77 |
| Biochem/physiol Actions【生化/生理作用】 | FM-381 is a highly potent and JAK3-selective janus kinase (JAK) inhibitor (IC50 = 127 pM/JAK3, 52 nM/JAK1, 346 nM/JAK2, 459 nM/TYK2 by radiometric assay; [ATP] = 10 μM) that targets JAK3 gatekeeper (GK) Cys909 for a reversible covalent interaction, exhibiting much reduced or little potency against a panel of 409 other kinases. FM-381 is >3-fold more potent than the JAK1/3 inhibitor Tofacitinib (IC50 = 292 pM/JAK3, 496 pM/JAK1, 2.2 nM/JAK2, 8.9 nM/TYK2 by radiometric assay; [ATP] = 10 μM) in blocking JAK1/JAK3-mediated STAT5 phosphorylation in human CD4+ T-cells upon IL-2 stimulation (ECmax ∼100 nM with FM-381), while being ineffective (up to 1 μM) against JAK3-independent STAT1/3 phosphorylation following IL-6 or TNFα stimulation. For characterization details of FM-381, please visit the FM-381 probe summary on the Structural Genomics Consortium (SGC) website. FM-479 is the negative control for the active probe, FM-381. FM-479 is available from Sigma. To learn more about and purchase FM-479, click here. To learn about other SGC chemical probes, visit sigma.com/sgc |
| Features and Benefits【特点和优势】 | FM-381 is a chemical probe available through a partnership with the Structural Genomics Consortium (SGC). To learn more and view other SGC chemical probes, visit sigma.com/SGC. |
产品性质
| Assay【测定】 | ≥98% (HPLC) |
| form【形式】 | powder |
| color【颜色】 | white to beige |
| solubility【溶解性】 | DMSO: 2 mg/mL, clear (warmed) |
| storage temp.【储存温度】 | 2-8℃ |
| SMILES string | CN(C(/C(C#N)=C/C(O1)=CC=C1C2=NC3=CN=C(NC=C4)C4=C3N2C5CCCCC5)=O)C |
安全信息
| Storage Class Code【储存分类代码】 | 13 - Non Combustible Solids |
| WGK | WGK 3 |
