WntHedgehogNotchPathway抑制剂整理版.doc

Wnt inhibitors ICG-001 M.Wt: 548.63 Formula: C33H32N4O4 Solubility: DMSO ≥110mg/mL Water 1mg/mL Ethanol ≥45mg/mL Purity: 99% Storage: at -20℃ 2 years CAS No.: 780757-88-2 Biological Activity ICG-001 is a selective Wnt/β-catenin signalling inhibitor with an IC50 of 3μM. After selectively binding of ICG-001 to the NH2 terminus of cyclic AMP response element binding protein (CREB), ICG-001 prevented beta-catenin/TCF signaling. ICG-001 elevated the activities of caspase in colon carcinoma cell lines, but not normal cells via down regulation of survivin. It is exhibited that ICG-001 rescues defects in neuronal differentiation and reverse pulmonary fibrosis. ICG-001 also suppressed the interaction between CREB and γ-catenin. [1]ICG-001 selectively induces apoptosis in transformed cells but not in normal colon cells. And ICG-001 reduces in vitro growth of colon carcinoma cells. ICG-001 efficaciously treated the colon cancer in the Min mouse and nude mouse xenograft models. XAV 939 M.Wt: 312.31 Formula: C14H11F3N2OS Solubility: DMSO ≥3mg/mL Water 1mg/mL Ethanol ≥5mg/mL Purity: 99% Storage: at -20℃ 2 years CAS No.: 284028-89-3 Biological Activity XAV 939 is a small molecule and selective Wnt pathway transcription factor β-catenin-mediated transcription inhibitor and axin stabilizing agent with IC50 of 11 and 4nM for the inhibition of TNKS1 and TNKS2, respectively. It stimulates beta-catenin degradation by stabilizing axin, the concentration-limiting component of the destruction complex and stabilizes axin by inhibiting the poly-ADP-ribosylating enzymes tankyrase 1 and tankyrase 2. Both tankyrase isoforms interact with a highly conserved domain of axin and stimulate its degradation through the ubiquitin-proteasome pathway. Deregulated Wnt/b-catenin pathway activity has been implicated in many cancers. Hedgehog inhibitors Cyclopamine M.Wt: 411.62 Formula: C27H41NO2 Solubility: DMSO ≥6mg/mL Water 1mg/mL Ethanol ≥39mg/mL Purity: 99% Storage: at