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FM-381,≥98% (HPLC)

别名:FM381;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

Empirical Formula (Hill Notation): C24H24N6O2 分子量: 428.49 NACRES: NA.77
制造商品牌: 西格玛 Sigma-Aldrich
货号(SKU): SML1979
增值税发票 √ 免费送货 √ 订货电话:010-68689484
€361.16

说明

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
 
FM-381 是一种高效的 JAK3 选择性 janus 激酶 (JAK) 抑制剂(IC50 = 127 pM/JAK3、52 nM/JAK1、346 nM/JAK2、459 nM/TYK2,通过放射测定;[ATP] = 10 μM) 靶向 JAK3 看门人 (GK) Cys909 进行可逆共价相互作用,对一组 409 种其他激酶表现出大大降低或很小的效力。 FM-381 的效力比 JAK1/3 抑制剂 Tofacitinib 强 3 倍以上(IC50 = 292 pM/JAK3、496 pM/JAK1、2.2 nM/JAK2、8.9 nM/TYK2,通过放射测定;[ATP] = 10 μM) 在 IL-2 刺激后阻断人 CD4+ T 细胞中 JAK1/JAK3 介导的 STAT5 磷酸化(ECmax ∼100 nM 与 FM-381),同时对 IL 后 JAK3 非依赖性 STAT1/3 磷酸化无效(高达 1 μM) -6 或 TNFα 刺激。
 

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.
 

属性

测定

≥98% (HPLC)

形式

powder

颜色

white to beige

溶解性

DMSO: 2 mg/mL, clear (warmed)

储存温度

2-8°C

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

RIDADR

NONH for all modes of transport

WGK Germany

WGK 3

商品规格
属性名称属性值
储存温度 Storage temp.2-8°C冷藏
全球实时库存 Availability √美国St. Louis ≥ 33 | 欧洲Eur. ≥ 27 | 東京Tokyo ≥ 9 | 香港与北京 ≥ 16