4-(3-(Pyridin-2-yl)-1H-pyrazol-4-yl)quinoline;LY-364947;4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]-quinoline;[3-(Pyridin-2-yl)-4-(4-quinonyl)]-1H-pyrazole;LY364947;4-(3-Pyridin-2-yl-1H-pyrazol-4-yl)quinoline;LY364947 (LY-364947, HTS 466284);4-(5-pyridin-2-yl-1H-pyrazol-4-yl)quinoline;HTS466284;Transforming Growth Factor-β Type I Receptor Kinase Inhibitor;E 616451;TGF-beta RI Kinase Inhibitor;HTS 466284;TbetaR-I Inhibitor;LY 364947;4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]quinoline;4-[5-(pyridin-2-yl)-1H-pyrazol-4-yl]quinoline;Quinoline, 4-[3-(2-pyridinyl)-1H-pyrazol-4-yl]-;Transforming Growth Factor-beta Type I Receptor Kinase Inhibitor;4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]quinoline;4-(3-pyridin-2-yl)(1h)-pyra
Cas No.
396129-53-6
分子式
C17N4H12
分子量
272.30
包装储存
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
生物活性
LY-364947 (HTS466284) is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM, and exhibits 7-fold selectivity over TGFβR-II.
性状
Solid
IC50 & Target[1][2]
IC50: 59 nM (TGFβR-I)
体外研究(In Vitro)
LY-364947 is an ATP competitive and tight-binding inhibitor, inhibiting phosphorylation of P-Smad3 by TGFβR-I Kinase with Ki 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.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.