GNF-6231 0636457-O-C3-COOH 4-dioxopentan-3-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-4-[[(2S)-3-(1H-indol-3-yl)-2-(phenylmethoxycarbonylamino)propanoyl]amino]-5-oxopentanoate

4-dioxopentan-3-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-4-[[(2S)-3-(1H-indol-3-yl)-2-(phenylmethoxycarbonylamino)propanoyl]amino]-5-oxopentanoate

O=S(=O)(C1C=CC(=CC=1)C1C=C2N=CC=CC2=CC=1)N1CCC2(CN(C3CC3)C(=O)CO2)CC1

CAS Number: 252025-52-8

at hydroxylation sites in the oxygen-dependent degradation domain (ODDD)

Smiles: CC1=NN(C2=CC(NCCCOCCOCCOCCOCCOCCCNCC3C=CC(=CC=3)/C(/C=C/C3=[N+](CCCCS([O-])(=O)=O)C4=CC=CC=C4C3(C)C)=C\C=C3\N(CCCCS(O)(=O)=O)C4=CC=CC=C4C\3(C)C)=C(C=C2)C(N)=O)C2CC(C)(C)CC(=O)C1=2

GNF-6231 0636457-O-C3-COOH 4-dioxopentan-3-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-4-[[(2S)-3-(1H-indol-3-yl)-2-(phenylmethoxycarbonylamino)propanoyl]amino]-5-oxopentanoateGNF 6231 is a potent, selective, and orally bioavailable Porcupine inhibitor that blocks Wnt signaling. 1) GNF 6231 shows IC50s of greater than 10 M on all CYP isoforms tested2) GNF 6231 have favorable potency and a PK profile across preclinical species upon oral administration. 3) The reference for orally in MMTV Wnt1 tumor bearing mice is dosed at 3 mg kg. 4) GNF 6231 showed very robust dose related antitumor efficacy. Product information CAS