ETC-159 | B3257

ETC-159 is a selective small molecule inhibitor of porcupine (PORCN), an enzyme required for palmitoylation and secretion of all Wnt ligands. It inhibits β-catenin reporter activity (IC50 = 2.9 nM) and reduces the interaction of Wnt with its carrier protein WLS via decreased Wnt palmitoylation in STF3A cells, an effect that is reversed by overexpression of recombinant PORCN. In preclinical studies, ETC-159 induces tumor regression in patient-derived xenograft models.

ETC-159 is a selective small molecule inhibitor of porcupine (PORCN), an enzyme required for palmitoylation and secretion of all Wnt ligands. It inhibits β-catenin reporter activity (IC50 = 2.9 nM) and reduces the interaction of Wnt with its carrier protein WLS via decreased Wnt palmitoylation in STF3A cells, an effect that is reversed by overexpression of recombinant PORCN. In preclinical studies, ETC-159 induces tumor regression in patient-derived xenograft models.

B3257 | ETC-159 DataSheet

Alternate Name/Synonyms: ETC-1922159 ETC159 1,2,3,6-tetrahydro-1,3-dimethyl-2,6-dioxo-N-(6-phenyl-3-pyridazinyl)-7H-purine-7-acetamide

Appearance: Crystalline solid

Formulation:

CAS Number: 1638250-96-0

Structure Available?: Yes

Peptide sequence: No

Salt Form: N/A

Molecular Formula: C₁₉H₁₇N₇O₃

Molecular Weight: 391.4

Cell-Permeable?: True

Purity: ≥95%

Solubilities:

Handling: Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.

Country of Origin: USA

Tag Line: A selective small molecule porcupine inhibitor

MDL Number:

PubChem CID: 86280523

SMILES: O=C1N(C)C(C(N(CC(NC2=NN=C(C3=CC=CC=C3)C=C2)=O)C=N4)=C4N1C)=O

InChi: InChI=1S/C19H17N7O3/c1-24-17-16(18(28)25(2)19(24)29)26(11-20-17)10-15(27)21-14-9-8-13(22-23-14)12-6-4-3-5-7-12/h3-9,11H,10H2,1-2H3,(H,21,23,27)

InChi Key: QTRXIFVSTWXRJJ-UHFFFAOYSA-N