. 2015 Feb 13;58(4):1717–1735. doi: 10.1021/jm501436m

Table 2. Assessment of Compounds 9 and 33 in Cell-Based Assays in Which WNT Signaling Is Activated at Distinct Levels by Inducible Expression of cDNAs Encoding Activating Components of the Canonical WNT Pathway^a.

		IC₅₀ (μM)
WNT pathway activation level	reporter	9	33
Dvl-ER (7dF3 primary assay)	TCF-luc	1.76	0.037
Tet-O-ΔN-LRP6	TCF-luc	0.91	0.020
Tet-O-Dvl2	TCF-luc	1.20	0.020
Tet-O-Axin-GID	TCF-luc	1.50	0.024
Tet-O-ΔN-β-catenin	TCF-luc	2.73	0.070
Tet-O-VP16-TCF4	TCF-luc	7.61	0.23

Activating components of the canonical WNT pathway: ΔN-LRP6 (a constitutively activating component of the WNT receptor), Dvl-2 (a Disheveled homologue and activator of WNT signaling), Axin-GID (Axin-GSK3β Interaction Domain, a dominant negative form of Axin that binds to and inhibits GSK-3β), ΔN-β-catenin (a stabilized form of β-catenin resistant to degradation), or VP16-TCF (a TCF transcription factor that is constitutively active in the absence of β-catenin). See the Supplementary Information for assay protocols.

Table 2. Assessment of Compounds 9 and 33 in Cell-Based Assays in Which WNT Signaling Is Activated at Distinct Levels by Inducible Expression of cDNAs Encoding Activating Components of the Canonical WNT Pathwaya.

Table 2. Assessment of Compounds 9 and 33 in Cell-Based Assays in Which WNT Signaling Is Activated at Distinct Levels by Inducible Expression of cDNAs Encoding Activating Components of the Canonical WNT Pathway^a.