LF3 是一种典型 Wnt 信号传导的特异性抑制剂,通过破坏 β-CATenin 和 TCF4 之间的相互作用(IC50< 2 μM)
产品描述
LF3 is a specific inhibitor of canonical Wnt signaling by disrupting the interaction between β-catenin and TCF4 (IC50< 2 μM)
体外活性
LF3 inhibited Wnt/β-catenin signals in cells with exogenous reporters and in colon cancer cells with endogenously high Wnt activity. LF3 also suppressed features of cancer cells related to Wnt signaling, including high cell motility, cell-cycle progression, and the overexpression of Wnt target genes[1].
体内活性
LF3 reduced tumor growth and induced differentiation in a mouse xenograft model of colon cancer.LF3 is a specific inhibitor of canonical Wnt signaling with anticancer activity[1].
动物实验
Unsorted GFPlow and GFPhigh SW480 cells (1 × 10^4) were subcutaneously injected into the back skin of NOD/SCID mice. Tumor growth was monitored over a period of 45 days. For therapy, LF3 was administered i.v. at 50 mg/kg body weight for three rounds over 5 consecutive days, with 2-day breaks[1].
Cas No.
664969-54-4
分子式
C20H24N4O2S2
分子量
416.56
储存和溶解度
DMSO:32 mg/mL (76.82 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years