性能参数
产品名称
JAK-IN-1
规格
250mg 500mg
货号
GOY-Y3513
含量
>98.00%
CAS
1334673-53-8
别名
N/A
化学名
分子式
C20H24N6O2
分子量
分子量 380.44
溶解度
Soluble in DMSO
储存条件
Store at -20°C
General tips
用途
仅供科研
价格
电询
详细内容
JAK-IN-1 is a JAK1/2/3 inhibitor with IC50s of 0.26, 0.8 and 3.2 nM, respectively. JAK-IN-1 shows improved selectivity for JAK3 over JAK1.
JAK-IN-1 inhibits the proliferation of human CD4 and CD8 T cells in a dose-dependent manner upon stimulation by anti-CD3/anti-CD28 antibody-coated beads partially mimicking the activation signals brought to a Tcell by an antigen-presenting cell. JAK-IN-1 is active in both mechanistic and functional cell-based assays using T-cells, one of the major cell types in which JAK3 is potentially relevant[1].
JAK-IN-1 is JAK3 selective in vivo, as judged by higher potency inhibiting JAK1/JAK3- vs JAK2- or JAK1/JAK2/TYK2-driven signaling in whole blood assays. JAK-IN-1 potently inhibits IL-2 stimulated plasma concentrations of JAK-IN-1 for each dose. JAK-IN-1 prevents IL-2-driven STAT5 phosphorylation in a dose- and concentration-dependent manner, with approximately 50% inhibition observed at the 10 mg/kg dose (plasma concentration ~480 nM)[1].
[1]. Soth M, et al. 3-Amido pyrrolopyrazine JAK kinase inhibitors: development of a JAK3 vs JAK1 selective inhibitor and evaluation in cellular and in vivo models. J Med Chem. 2013 Jan 10;56(1):345-56.
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传真号码:021-39596320 021-39921927
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产品均为实验试剂,仅供科研实验使用,非药品、非食品、不可用于动物及人体!