LY2109761

LY2109761

Application

LY2109761 has been used as an inhibitor of type I and II transforming growth factor-beta (TGF?) receptors to reduce the phosphorylation of SMAD2 (mothers against decapentaplegic homolog) in HepG2 cells.

Biochem/physiol Actions

LY2109761 is a potent and orally active TGF-β receptor (TGFβR) type I & II dual inhibitor (IC50 = 70 and 322 nM against TGFβRI/ALK5 and TGFβRII autophosphorylation, respectively, with 4 µM ATP), inhibiting Fyn/JNK3/Lck/MKK6/SAPK2α only at much higher concentrations (58-89% inhibition at 20 µM) and exhibiting little or no potency against 37 other kinases (IC50 >20 µM). LY2109761 inhibits 0.25 ng/mL TGFβ-induced NIH/3T3 proliferation in cultures (IC50 = 210 nM; 2-hr pretreatment prior to TGFβ for 24 hrs) and suppresses human MX1 breast carcinoma xenograft tumor growth in mice in vivo (by ~80% on day 37; 75 mg/kg p.o. bid from day 7 to 20). When administered in combination with gemcitabine (25 mg/kg/day i.p.), LY2109761 (50 mg/kg p.o. bid) is shown to significantly reduce tumor burden and spontaneous abdominal metastases in a murine model of metastatic pancreatic cancer.

LY2109761 suppresses transforming growth factor (TGF)-?1-induced fibroblasts proliferation and collagen synthesis in hypertrophic scar fibroblasts. Therefore, it is used in treating hypertrophic scars.

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Code Description Colour Manufacturer Storage Temp. Solubility Form Assay Price Quantity
3575751 LY2109761 white to beige SIGMA-ALDRICH −20°C DMSO: 2 mg/mL, clear
£449.89 (exc VAT) per 25MG
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3575752 LY2109761 white to beige SIGMA-ALDRICH −20°C DMSO: 2 mg/mL, clear
£111.71 (exc VAT) per 5MG
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