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JAK3-IN-6

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产品名称: JAK3-IN-6
产品型号: GOY-Y3509
产品展商: 谷研
产品文档: 无相关文档
发布时间:2023-05-08

简单介绍

JAK3-IN-6DMSO: 260 mg/mL (742.07 mM)


JAK3-IN-6  的详细介绍

性能参数

产品名称

JAK3-IN-6

规格

250mg 500mg

货号

GOY-Y3509

 含量

>98.00%

CAS

1443235-95-7

别名

N/A

 

 

化学名

N/A

分子式

C19H18N4O3

分子量

分子量 350.37

溶解度

DMSO: 260 mg/mL (742.07 mM)

储存条件

Store at -20°C

General tips

 

用途

仅供科研

价格

电询

详细内容

JAK3-IN-6 is a potent, selective irreversible Janus Associated Kinase 3 (JAK3) inhibitor, with an IC50 of 0.15 nM.

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].

 

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