LY364947

Tumor xenograft models with BxPC3 pancreatic adenocarcinoma cells.

LY364947 is a potent ATP-competitive inhibitor of TGFbetaR-I with IC50 of 59 nM.

Dissolved in 5 mg/mL in DMSO and diluted with 100 uL PBS

LY364947 is an ATP competitive and tight-binding inhibitor, inhibiting phosphorylation of P-Smad3 by TGFbetaR-I kinase with Ki of 28 nM. LY364947 inhibits in vivo Smad2 phosphorylation within the NMuMg cells with IC50 of 135 nM. LY364947 reverses TGF-beta-mediated growth inhibition in NMuMg cells with IC50 of 0.218 uM. LY364947 potentiates the xVent2-lux BMP4 response in NMuMg cells by 30% at concentrations as low as 0.25 uM. LY364947 (2 uM) prevents TGF-beta-induced epithelial mesenchymal transition in NMuMg cells. [3] LY364947 (3 uM) induces expression of Prox1 and LYVE-1 in almost all HDLECs after 24 hours. [4] LY364947 promotes nuclear export of Foxo3a, with low Smad2/3 and high Akt phosphorylation levels in leukaemia-initiating cells. LY364947 (< 20 uM) suppresses leukaemia-initiating cells colony-forming ability after co-culture with OP-9 stromal cells. [5]

[3], Filter-binding assay, The IC50 of LY364947 at different enzyme concentrations are determined by the filter-binding assay. Typically, 40 uL reactions in 50 mM HEPES at pH 7.5, 1 mM NaF, 200 uM pKSmad3( 3), and 50 mM ATP containing a titration of each inhibitor with concentrations of 1600, 800, 400, 200, 100, 50, 25, and 0 nM are incubated at 30 C for 30 min. The IC50 is calculated using a nonlinear regression method with GraphPad Prism software. The binding type is determined by plotting the correlation between enzyme concentrations and IC50 values.

LY364947 Chemical Structure

2 years -20CPowder, 2 weeks4Cin DMSO, 2 months-80Cin DMSO