Wnt-C59 (C59) - Moligand™, 10mM in DMSO , Inhibitor of porcupine O-acyltransferase, CAS No.1243243-89-1, Inhibitor of porcupine O-acyltransferase

CAS: 1243243-89-1 Cat. No.: W407881 Summenformel: C₂₅H₂₁N₃O Molekulargewicht: 379.45 PubChem CID: 57519544

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

2-(4-(2-methylpyridin-4-yl)phenyl)-N-(4-(pyridin-3-yl)phenyl)acetamide

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Übersicht

Information

Wnt-C59 (C59) Wnt-C59 (C59) is a PORCN inhibitor for Wnt3A-mediated activation of a multimerized TCF-binding site driving luciferase with IC50 of 74 pM in HEK293 cells.
In vitro

Wnt-C59 (C59) is claimed to inhibit PORCN enzyme activity at nanomolar concentrations. Wnt-C59 (10 nM) blocks the palmitoylation-dependent Wnt–WLS interaction in HeLa cells transfected with either WNT3A-V5 or WNT8A-V5 plasmids. Wnt-C59 (100 nM) prevents incorporation of palmitate into WNT3A in HeLa cells transfected with WNT3A-V5, consistent with inhibition of PORCN activity. Wnt-C59 (100 nM) inhibits the activity of all splice variants of murine PORCN in PORCN- HT1080 cells transfected with PORCN. Wnt-C59 is a nanomolar inhibitor of mammalian PORCN acyltransferase activity and blocks activation of all evaluated human Wnts. Wnt-C59 does not significantly inhibit the proliferation of any of 46 tested cancer cell lines in vitro at concentrations that completely inhibit PORCN. Wnt-C59 is capable to significantly inhibit proliferation and comparable to the ICG-001 treated NMuMG (NMG) cells. Wnt-C59 inhibits sphere formation by threefold in NMuMG (NMG) cells, which is dependent on Wnt10b-secretion. Wnt-C59 inhibits proliferation of human MDA-MB 231 cells by >50%. Wnt-C59 (a Porcupine inhibitor) blocks radiolabel incorporation of [¹²⁵I]iodo-pentadecanoate in mouse L-Wnt3a cells transfected with Flag-Porcupine.

In vivo

Wnt-C59 concentration remains greater than 10-fold above the in vitro IC50 for at least 16 hours following a single oral dose (5 mg/kg) in mice. Wnt-C59 (10 mg/kg) prevents growth of MMTV-WNT1 tumors in female nude mice orthotopically transplanted with independent MMTV-WNT1 tumors. Wnt-C59 (10 mg/kg) decreases Wnt pathway activity and decreased proliferation in MMTV-WNT1 tumors in female nude mice orthotopically transplanted with independent MMTV-WNT1 tumors as evident by decreased expression of β-catenin target gene expression. Wnt-C59 (10%) topically administered 4 weeks decreases the size of dysplasia of SmoM2-expressing cells in adult K14CREER/Rosa–SmoM2 mice.
Cell Data

cell lines：

Concentrations：--

Incubation Time：48 hours

Powder Purity:≥98%

Specifications

Synonyme

2-(4-(2-methylpyridin-4-yl)phenyl)-N-(4-(pyridin-3-yl)phenyl)acetamide

Spezifikationen & Reinheit

Moligand™, 10mM in DMSO

Biochemische und physiologische Mechanismen

Wnt-C59 (C59) is a PORCN inhibitor for Wnt3A-mediated activation of a multimerized TCF-binding site driving luciferase with IC50 of 74 pM in HEK293 cells.

Storage

Store at -80°C

Verschickt in

Dry ice packs + Cold packs

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Note

Moligand™

Aktionsart

INHIBITOR

Mechanismus der Wirkung

Inhibitor of porcupine O-acyltransferase

Namen und Kennungen

Isomere SMILES

CC1=NC=CC(=C1)C2=CC=C(C=C2)CC(=O)NC3=CC=C(C=C3)C4=CN=CC=C4

PubChem CID

57519544

Molekulargewicht

379.45

Zugehörige Ziele (menschlich)

PORCN Tchem Protein-serine O-palmitoleoyltransferase porcupine (1 Activities)

Discover Target: PORCN

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)