IWP-2 inhibits the WNT pathway (IC₅₀ = 27 nM) at the level of the pathway activator Porcupine. Porcupine is a membrane-bound acyltransferase that palmitoylates WNT proteins, which leads to WNT secretion and signaling capability.

IWP-2 is an inhibitor of Wnt processing and secretion with an IC 50 of 27 nM. IWP-2 targets the membrane-bound O-acyltransferase porcupine (Porcn) and thus preventing a crucial Wnt ligand palmitoylation. IWP-2 is also an ATP-competitive CK1δ inhibitor with an IC 50 of 40 nM for the gatekeeper mutant M82F CK1δ.

IWP-2是一种Wnt信号和分泌抑制剂，无细胞试验中IC50为27 nM，选择性阻断Porcn介导的Wnt棕榈酰化，一般不影响Wnt/β-catenin，且对Wnt刺激的细胞反应没有影响。

IWP-2, an inhibitor of Wnt processing and secretion (IC50=27 nM) in a cell-free assay, selectively blocks Porcn-mediated Wnt palmitoylation.

2017年5月3日 · A549 BAR cells were plated at a density of 5,000 cells per well in the presence of 2 μM IWP-2 (Calbiochem) to suppress endogenous Wnt secretion, and treatment was started after 48 h in fresh ...

IWP-2 (IWP2)是Wnt分泌和加工的抑制剂，IC 50 值为27 nM，作用于Porcn使其失活，选择性地抑制Porcn介导的Wnt棕榈酰化。IWP-2抑制R1胚胎干细胞的自我更新，并促进hPSC分化为心肌细胞，被广泛用于再生医学和肿瘤研究。

IWP-2 is a Wnt pathway inhibitor by inactivating the Porcupine O-acyltransferase which palmitoylates Wnt proteins. It is reported to inhibit embryonic stem cell self-renewal and promote cardiomyocyte differentiation from human stem cells.

IWP-2 is an inhibitor of Wnt production that impairs Wnt pathway activity in vitro with an IC 50 value of 27 nM. 1 IWP-2 inactivates Porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins, which is essential for their signaling ability and secretion. 1 At 5 μM, IWP-2 has been shown to block Wnt-dependent ...