LGK-974 - Moligand™, 10mM in DMSO , Probable protein-cysteine N-palmitoyltransferase porcupine inhibitor, CAS No.1243244-14-5, Probable protein-cysteine N-palmitoyltransferase porcupine inhibitor

CAS: 1243244-14-5 Cat. No.: L409002 Molecular Weight: 396.4

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

NVP-LGK974, WNT974 | [2,4'-Bipyridine]-5-acetamide, 2',3-dimethyl-N-[5-(2-pyrazinyl)-2-pyridinyl]-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

LGK-974 LGK-974 (NVP-LGK974, WNT974) is a potent and specific PORCN inhibitor, and inhibits Wnt signaling with IC50 of 0.4 nM in TM3 cells. Phase 1.
In vitro

LGK974 effectively displaces [³H]-GNF-1331 with IC50 of 1 nM in the PORCN radioligand binding assay, and shows no major cytotoxicity in cells up to 20 µM. LGK974 shows comparable inhibitory activities against all tested Wnts with IC50 ranging from 0.05 to 2.4 nM, which is consistent with the genetic loss of PORCN phenotype. LGK974 specifically inhibits the growth of three RNF43-mutant cell lines, HPAF-II, PaTu 8988S, and Capan-2.

In vivo

In a murine MMTV-Wnt1 tumor model and a human head and neck squamous cell carcinoma model (HN30), LGK974 (3 mg/kg) inhibits Wnt signaling in vivo and induces tumor regression without significant body weight loss in the mice. LGK974 (5 mg/kg, p.o., BID) also inhibits tumor growth of RNF43-mutant pancreatic tumors (HPAF-II and Capan-2) in vivo.
Cell Data

cell lines：

Concentrations：~1 μM

Incubation Time：3 days

Powder Purity:≥99%

Specifications

Synonyms

NVP-LGK974, WNT974 | [2, 4'-Bipyridine]-5-acetamide, 2', 3-dimethyl-N-[5-(2-pyrazinyl)-2-pyridinyl]-

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

LGK-974 (NVP-LGK974, WNT974) is a potent and specific PORCN inhibitor, and inhibits Wnt signaling with IC50 of 0.4 nM in TM3 cells. Phase 1.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

Probable protein-cysteine N-palmitoyltransferase porcupine inhibitor

Product Properties

• ALogP: 1.8

Names and Identifiers

• Isomeric SMILES: CC1=CC(=CN=C1C2=CC(=NC=C2)C)CC(=O)NC3=NC=C(C=C3)C4=NC=CN=C4
• Molecular Weight: 396.4
• Reaxy-Rn: 20663778
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=20663778&ln=

Associated Targets(Human)

PORCN Tchem Protein-serine O-palmitoleoyltransferase porcupine (2 Activities)

Discover Target: PORCN

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