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FM-381

CAS号

2226521-65-7

分子式

C24H24N6O2

主要靶点

JAK

仅限科研使用

Cat No : CM04894

Print datasheet

Synonyms

Inhibitor|JAK|JAK3|Janus kinase|inhibit|FM381|FM-381|FM 381

验证数据展示

  • CAS No.: 2226521-65-7

    FM-381
    CAS#: 2226521-65-7

产品信息

CAS号 2226521-65-7
分子式 C24H24N6O2
主要靶点 JAK
主要通路 表观遗传|蛋白酪氨酸激酶|干细胞|血管生成|JAK/STAT 信号通路
分子量 428.49
纯度 99.33%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 Inhibitor|JAK|JAK3|Janus kinase|inhibit|FM381|FM-381|FM 381

靶点活性

JAK3:127 pM

体外活性

FM-381是一种针对JAK3独特的Cys909位点在门卫(GK)位置+7的强效可逆共价抑制剂，显示出对JAK3的显著IC50值为0.127 nM，分别对JAK1、JAK2和TYK2具有400倍、2700倍及3600倍的选择性。在常被激活的BRDs（BRD4、BRPF、CECR、FALZ、TAF1、BRD9）选择性面板中，FM-381未显示活性。FM-381在剂量依赖性BRET测定中表现出100 nM的明显EC50，并在100 nM时阻断了IL2刺激下的（JAK3/JAK1依赖的）STAT5磷酸化，但在高达1 μM的剂量下不影响JAK3独立的IL6刺激下的（JAK1/2/TYK依赖的）STAT3信号在人类CD4+ T细胞中的传导[1]。

溶解度

H2O:Insoluble;DMSO:12.5 mg/mL (29.17 mM)

细胞实验

CD4+ T Cell cytokine stimulation assay is performed. T cells are purified from peripheral blood mononuclear cells from human donors. Equal numbers of cells are incubated for 1 hr with JAK inhibitors (FM381) (0, 10, 50, 100, 300 nM) or DMSO control and stimulated with cytokines for 30 min. The cells are lysed, and the proteins are separated via PAGE and transferred to a polyvinylidene fluoride membrane. The proteins of interest are blotted with specific antibodies and visualized with an infrared imaging system[1].

参考文献

1.Forster M, et al. Selective JAK3 Inhibitors with a Covalent Reversible Binding Mode Targeting a New Induced Fit Binding Pocket. Cell Chem Biol. 2016 Nov 17;23(11):1335-1340.

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