MilliporeSigma™ Calbiochem™ TGF-β RI Kinase Inhibitor IX

Description

A cell-permeable pyridinyloxypyridine compound that acts as a potent and highly selective inhibitor against TGFβ RI/ALK5 (IC₅₀ = 72 nM, [ATP] = 1 mM) by targeting both the ATP-binding site and the selectivity pocket, while exhibiting much reduced or little activity against a panel of 75 other kinases (IC₅₀ <1μM).

A cell-permeable pyridinyloxypyridine compound that acts as a potent and highly selective inhibitor against TGFβ RI/ALK5 (IC₅₀ = 72 nM, [ATP] = 1 mM) by targeting both the ATP-binding site and the selectivity pocket, while exhibiting much reduced or little activity against a panel of 75 other kinases (IC₅₀ <1μM). Shown to reduce TGFβ1-induced nuclear translocation of a GFP-Smad2 fusion reporter in MDA-MB-468 cells (IC₅₀ = 22nM) in vitro and exhibit excellent oral bioavailability (F = 75%, AUC = 4.95μM.h) with low clearance (12 ml/min/kg) in rats in vivo .

Specifications

• Color: Off-white
• Description: 95% by HPLC
• Molecular Formula: C₁₈H₁₈N₄O₃S
• Formula Weight: 370.4g/mol
• Solubility: DMSO
• Content And Storage: Protect from light
• Form: Powder
• Quantity: 10 mg