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LY-364947

CAS No. : 396129-53-6

MCE 站：LY-364947

产品活性：LY-364947 (HTS466284) 是一种有效的，ATP 竞争性的 TGFβR-I 抑制剂，IC₅₀ 值为 59 nM，是对 TGFβR-II 选择性的 7 倍。

研究领域：TGF-beta/Smad

作用靶点：TGF-β Receptor

In Vitro: LY-364947 is an ATP competitive and tight-binding inhibitor, inhibiting phosphorylation of P-Smad3 by TGFβR-I Kinase with K_i of 28 nM. LY-364947 inhibits in vivo Smad2 phosphorylation within the NMuMg cells with IC₅₀ of 135 nM. LY-364947 reverses TGF-β-mediated growth inhibition in NMuMg cells with IC₅₀ of 0.218 μM. LY-364947 potentiates the xVent2-lux BMP4 response in NMuMg cells by 30% at concentrations as low as 0.25 μM. LY-364947 (2 μM) prevents TGF-β-induced epithelial?mesenchymal transition in NMuMg cells. LY-364947 (3 μM) induces expression of Prox1 and LYVE-1 in almost all HDLECs after 24 hours. LY-364947 promotes nuclear export of Foxo3a, with low Smad2/3 and high Akt phosphorylation levels in leukaemia-initiating cells. LY-364947 (< 20 μM) suppresses leukaemia-initiating cells colony-forming ability after co-culture with OP-9 stromal cells.

In Vivo: LY-364947 (1 mg/kg, i.p.) accelerates lymphangiogenesis, as evidence by significantly increasing the LYVE-1-positive areas in a mouse model of chronic peritonitis. LY-364947 (1 mg/kg, i.p.) significantly increases the LYVE-1-positive areas in tumor tissues in tumor xenograft models using BxPC3 pancreatic adenocarcinoma cells. LY-364947 (25 mg/kg) increases p-Akt and decreases nuclear Foxo3a in leukaemia-initiating cells in CML-affected mice.

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