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MilliporeSigma™ Calbiochem™ TGF-β RI Kinase Inhibitor IX

Catalog No. 61646310MG Shop All MilliporeSigma Products
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61-646-310MG 10 mg
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Catalog No. 61-646-310MG Supplier MilliporeSigma™ Supplier No. 61646310MG

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 .
TRUSTED_SUSTAINABILITY

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
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