产品名称
Wnt拮抗剂I,IWR-1-endo, Wnt Antagonist I, IWR-1-endo, is a cell-permeable inhibitor of TNKS1/PARP5a (IC50 = 131 nM) & TNKS2/PARP5b (IC50 = 56 nM). Suppress Wnt-stimulated transcription activity (IC50 = 180 nM).
Quality Segment
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
off-white
solubility
DMSO: 10 mg/mL
shipped in
ambient
storage temp.
2-8°C
General description
一种细胞渗透性对亚氨基苯甲酰氨基喹啉,内非对映异构体,在体外自动PARsylation分析(IC50分别为131和56 nM)中显示抑制TNKS1/PARP5a和TNKS2/PARP5b的活性,并在基于L-Wnt-STF的报告分析(IC50=180 nM)中有效抑制Wnt刺激的转录活性,而对PARP1或PARP2几乎没有活性(IC50 >18.75 µM)。 尽管IWR-1-endo和XAV939都是可逆的Wnt途径抑制剂,并且在体外和体内表现出相似的药理作用,但IWR-1-endo通过与Axin的相互作用发挥其作用,而XAV939直接与TNK结合。
Packaging
用惰性气体包装
Preparation Note
复溶后,等分并冷冻保存(-20°C)。贮备溶液在-20°C下可稳定保存至多3个月。
Other Notes
Chen, B., et al. 2009.Nature Chem. Biol.5, 100.
Huang, S.M., et al. 2009.Nature461, 614.
Huang, S.M., et al. 2009.Nature461, 614.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
毒性:标准处理(A)
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable