Table 1. Selected Small Molecule Tools Targeting Wnt Pathway Components.
compound identifier | molecular target | effect on canonical Wnt signaling | structural information in public domain | furthest progress to date | refs |
---|---|---|---|---|---|
ICG-001, 5 | CBP | inhibit | no | preclinical | (45) |
IWP-2, 9 | Porcupine | inhibit | no | preclinical | (51) |
endo-IWR-1, 11 | TNKS1/2 | inhibit | yes | preclinical | (51) |
XAV939, 12 | TNKS1/2 | inhibit | yes | preclinical | (57,59) |
G007-LK | TNKS1/2 | inhibit | yes | preclinical | (60,63) |
NVP-TNKS656 | TNKS1/2 | inhibit | no | preclinical | (61) |
MSC2504877 | TNKS1/2 | inhibit | no | preclinical | (62) |
BML-268, 13 | DVL3 | inhibit | yes | early discovery | (65) |
NPL-4011, 14 | DVL3 | inhibit | yes | early discovery | (66) |
NSC654259, 15 | FZD8 | inhibit | yes | early discovery | (67) |
carbamazepine, 16 | FZD8 | inhibit | yes | preclinicala | (68) |
SRI37892, 17 | FZD7 | inhibit | yes | early discovery | (70) |
gallocyanine, 21 | LRP6 | enhance | yes | early discovery | (77) |
WAY-362692, 22 | sFRP-1 | enhance | no | preclinical | (82−84) |
WAY-262611, 23 | DKK1 | enhance | no | preclinical | (85) |
LP-922056, 26 | Notum | enhance | yes | preclinical | (95) |
ABC99, 27 | Notum | enhance | no | preclinical | (118) |
ARUK3001185, 28 | Notum | enhance | no | preclinical | (126) |
Carbamazepine is an approved anticonvulsant drug used clinically in the treatment of epilepsy and neuropathic pain.