LY364947
| CAS号 | 396129-53-6 | 货号 | BCP05350 |
| 中文名 | LY364947 | ||
| 英文名 | LY364947 | ||
| 中文别名 | |||
| 英文别名 | LY-364947;LY 364947; | ||
| 分子式 | C17H12N4 | 分子量 | 272.3 |
| 生物活性 | in vitro: LY364947 is an ATP competitive and tight-binding inhibitor, inhibiting phosphorylation of P-Smad3 by TGFβR-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-β-mediated growth inhibition in NMuMg cells with IC50 of 0.218 μM. LY364947 potentiates the xVent2-lux BMP4 response in NMuMg cells by 30% at concentrations as low as 0.25 μM. LY364947 (2 μM) prevents TGF-β-induced epithelial-mesenchymal transition in NMuMg cells . LY364947 (3 μM) induces expression of Prox1 and LYVE-1 in almost all HDLECs after 24 hours . LY364947 promotes nuclear export of Foxo3a, with low Smad2/3 and high Akt phosphorylation levels in leukaemia-initiating cells. LY364947 (< 20 μM) suppresses leukaemia-initiating cells colony-forming ability after co-culture with OP-9 stromal cells. in vivo: LY364947 (1 mg/kg i.p.) accelerates lymphangiogenesis, as evidence by significantly increased the LYVE-1-positive areas, in | ||
| 信号通路 | TGF beta/Smad | ||
| 靶 点 | BMP/TGF beta Receptor | ||
结构式
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