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JAK3-IN-6 是 JAK3 的一个有效的、选择性的、不可逆的抑制剂,其 IC50 值为 0.15 nM。
生物活性 JAK3-IN-6 is a potent, selective irreversible Janus Associated Kinase 3 (JAK3) inhibitor, with an IC50 of 0.15 nM.
IC50 & Target JAK3
0.15 nM (IC50)
体外研究
(In Vitro)JAK3-IN-6 (compound 2), a potent inhibitor of JAK3 (0.15 nM) is 4300-fold selective for JAK3 over JAK1 in enzyme assays, 67-fold (IL-2 vs. IL-6) or 140-fold (IL-2 vs. EPO or GMCSF) selective in cellular reporter assays and >35-fold selective in human PBMC assays (IL-7 vs. IL-6 or GMCSF). Irreversible JAK3-IN-6 with a JAK1 selective inhibitor 3 (JAK1: 0.96 nM, JAK2: 14 nM, JAK3: >1500 nM, TYK2: 10 nM) are cross titrated to determine if there is an additive or synergistic effect of co-inhibiting JAK1 and JAK3 enzymes on IL-7 signaling in CD3+, CD4+ PBMCs. As shown, the predicted levels of pSTAT5 inhibition based on addition of JAK1 and JAK3 inhibition are very close to the measured effects of cross titrating each compound, demonstrating that there is an additive effect but no synergistic effect of inhibiting JAK1 and JAK3 on blocking STAT5 phosphorylation. Furthermore inhibition of either JAK1 or JAK3 alone is sufficient to fully inhibit pSTAT5[2].
分子量
350.37
Formula
C19H18N4O3
CAS 号
1443235-95-7
性状
固体
颜色
White to light yellow
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year 关键词:- JAK3-IN-6
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产品组分
内容
型号
规格 储存温度
JAK3-IN-6 T3043-01 1mg -20°C JAK3-IN-6 T3043-02 5mg -20°C JAK3-IN-6 T3043-03 10mg -20°C JAK3-IN-6 T3043-04 25mg -20°C JAK3-IN-6 T3043-05 50mg -20°C JAK3-IN-6 T3043-06 100mg -20°C 操作手册
1 1 常温
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注意事项
保存建议 厂家推荐蓝冰运输。当您收到产品后,按照说明书建议保存于-20°C。 -
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