Chemical Structure : Dual JAK3-TEC kinase inhibitor ZZB
CAS No.:
2913218-49-0
Dual JAK3-TEC kinase inhibitor ZZB
货号: PC-23784Not For Human Use, Lab Use Only.
Dual JAK3-TEC kinase inhibitor ZZB is a potent, selective, covalent dual JAK3/TEC family kinases inhibitor with IC50 of 0.80 nM against JAK3 and 11.56 nM against TEC kinase interleukin-2-inducible T-cell kinase (ITK) respectively.
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纯度 & COA & 质检文件 纯度:
>98% (HPLC)
生物&药学活性
Dual JAK3-TEC kinase inhibitor ZZB is a potent, selective, covalent dual JAK3/TEC family kinases inhibitor with IC50 of 0.80 nM against JAK3 and 11.56 nM against TEC kinase interleukin-2-inducible T-cell kinase (ITK) respectively.
ZZB binds to the unique cysteine residue at position 909 (Cys909) in JAK3 and Cys442 in ITK. does not inhibit JAK1, JAK2 and TYK2.
ZZB selectively inhibits JAK3-dependent cytokine signaling, represses ITK-mediated CD4+ T cell activation (IC50=82.07 nM).
ZZB inhibited CD4+ T cell proliferation in a dose-dependent manner with an IC50 value of 50.52 nM.
ZZB inhibited cytotoxicity of CD8+ T cells.
ZZB (100 mg/kg) markedly improved skin condition and reduced immune cell infiltration, matching the efficacy of the positive drug dexamethasone, in mouse model of atopic dermatitis (AD).
物理化学性质&存储条件
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分子量
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293.33
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分子式
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C16H15N5O
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外观性状
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Solid
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CAS No.
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储存条件
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- 固体粉末
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-20°C 12 个月; 4°C 6 个月
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- 配置液
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-80°C 6 个月; -20°C 6 个月
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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1-(3-(1H-pyrrolo[2,3-b]pyridin-4-yl)-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)prop-2-en-1-one
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参考文献
1. Du Y, et al. Biochem Pharmacol. 2025 Jan 5:116740.
