iCRT5, b-catenin inhibitor (TBI1371)

Description

Product Details

Formal Name: 2-[[5-Chloro-2-[4-[(4-methylpiperazine-1-yl)methyl]pyrimidine-4-yl]amino]-N,N-dimethylbenzenesulfonamide

Molecular Formula: C₁₆H₁₇NO₅S₂

Formula Weight: 367.44

CAS Number: 18623-44-4

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to 30 mg/ml)

Storage: -20°C

Stability: ≥ 1 year.

Applications

b-catenin inhibitor

Functions

A selective CRT (β-catenin-responsive transcription) inhibitor. IC50=18 nM for Wnt responsive STF16 luciferase. Acts via interfering with the β-catenin, TCF4 interaction. Displays poor inhibition of cell proliferation in triple-negative breast cancer cells. Increases the surface expression of MHCII, CD80 and CD86 on unstimulated dendritic cells (DCs) with no detrimental effects on immune-phenotype of stimulated DCs. Modulators of Wnt signaling show great promise in animal models of several cancers. Cell permeable.

Application Procedures

First dissolved in DMSO (up to 30 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 2 months.