Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis. Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription. IWP-4 is an inhibitor of Wnt production that impairs Wnt pathway activity in vitro with an IC50 value of 25 nM. IWP-4 inactivates Porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins, which is essential for their signaling ability and secretion. At 5 μM, IWP-4 has been shown to block Wnt-dependent phosphorylation of the low-density lipoprotein receptor-related protein 6 receptor and the scaffold protein Dishevelled, preventing the accumulation of β-catenin. This compound has been used to induce cardiomyocyte differentiation from human pluripotent stem cells.
IWP 4制备储备液:
浓度溶解体积质量
1mg
5mg
10mg
1mM
2.1032mL
10.5159mL
21.0318mL
5mM
0.4206mL
2.1032mL
4.2064mL
10mM
0.2103mL
1.0516mL
2.1032mL
50mM
0.0421mL
0.2103mL
0.4206mL
IWP 4临床数据( 数据源于:http:// clinicaltrials.gov)
Conversion of different model animals based on BSA(Value based on data from FDA Draft Guidelines)
Animal A (mg/kg)=Animal B(mg/kg)multiplied by AnimalBm系数/AnimalAm系数 For example, to modify the dose of resveratrol uesd for a mouse(22.4mg/kg) to a dose based on the BSA for a rat, multiply 22.4mg/kg by the Km factor for a mouse and zhen divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2mg/kg