SB-525334, ALK5 (TGF bR1) inhibitor (TBI2983)

Description

Product Details

Formal Name: 6-[2-(1,1-Dimethylethyl)-5-(6-methyl-2-pyridinyl)-1H-imidazol-4-yl]quinoxaline

Molecular Formula: C₂₁H₂₁N₅

Formula Weight: 343.42

CAS Number: 356559-20-1

Purity: >98%

Formulation: powder

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

Storage: -20°C

Stability: ≥ 2 years.

Applications

ALK5 (TGF bR1) inhibitor

Functions

Potent and selective inhibitor of the transforming growth factor beta 1 receptor, activin receptor-like kinase (ALK5), IC50 = 14.3 nM and ALK4 (IC50 = 58.5 nM) with no activity at ALK2, 3 and 61. Blocks fibrosis markers and renal injury in the puromycin-induced nephritis model. It causes significant attenuation in Smad2/3 nuclear translocation, decrease in CTGF-expressing cells, myofibroblast proliferation and type 1 collagen deposition resulting in an overall attenuation in bleomycin-induced pulmonary fibrosis. Sensitizes drug-resistant pancreatic cancer cells to gemcitabine. Cell permeable and active in vivo.

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 3 months.