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. Author manuscript; available in PMC: 2022 Jul 1.
Published in final edited form as: Med Res Rev. 2021 Jan 21;41(4):2109–2129. doi: 10.1002/med.21787

Table 1.

Small-molecule inhibitors that were reported to directly bind with β-catenin.

graphic file with name nihms-1664379-t0001.jpg
Compound M.W. Discovery method Direct binding KD, μM Binding sites TOP-Flash, IC50, μM In vivo efficacy
PNU-74654 320 virtual screening NMR, ITC 0.450 K435, R469 N.D. N.D.
UU-T01 230 hot spot-based design ITC, mutagenesis 0.531 K435, K469 K508 N.D. N.D.
UU-T02 665 peptidomimetic design ITC, mutagenesis 0.418 K435, R469 R474, K508 R515 SW480: 232 N.D.
MSAB 305 luciferase-reporter screening SPR, NMR N.D. residues 301–670 HCT116: 0.58 20 mg/kg p.o., q.2d.
HI-B1 255 rational design based on a hit protein pull-down N.D. K312 DLD1: 13 CACO2: 13 50mg/kg i.p., q.d.
carnosic acid 332 screening by in vitro ELISA NMR 5–20 ARD N-terminus SW480: ~25 diet containing 0.1% or 1% carnosate
PNPB-22 646 hot spot-based design ITC, mutagenesis 0.330 L156, L159, V167, A171, M174, L178 SW480: 13 N.D.

N.D.: not determined. ARD: Armadillo repeat domain.