LGK974, Porcupine inhibitor (TBI4381)

Description

Product Details

Formal Name: 2-[5-Methyl-6-(2-methyl-4-pyridinyl)-3-pyridinyl]-N-(5-pyrazin-2-yl-2-pyridinyl)acetamide

Alternate Names: WNT974

Molecular Formula: C₂₃H₂₀N₆O

Formula Weight: 396.4

CAS Number: 1243244-14-5

Purity: >98%

Formulation: Powder

Solubility: Soluble in DMSO (> 25 mg/ml)

Storage: -20°C

Stability: ≥ 2 years.

Applications

Porcupine inhibitor

Functions

Potent and selective inhibitor of Porcupine (IC₅₀ = 1 nM). Inhibits Wnt signaling (IC₅₀ = 0.4 nM) in vitro and in vivo. It displays efficacy in several cancer models including glioblastoma, squamous cell, renal cell carcinoma, and non-small cell lung. Reprogrammed the immune suppressive tumor microenvironment in a mouse model of glioblastoma to increase antitumor immune responses. It also potentiated anti-PD1 therapy by increasing DC3-like dendritic cells and decreasing myeloid suppressor cells. LGK974 attenuated myocardial ischemia-reperfusion injury by reducing inflammatory responses.

Application Procedures

First dissolved in DMSO (> 25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.

Research use only.

Additional information

Datasheet:

TBI4381_LGK974_datasheet

MSDS:

TBI4381_LGK974_MSDS

Research use only.