2 years -20°C powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Biological activity
Description
CAS NO.：396129-53-6 Product Name：4-(3-Pyridin-2-YL-1H-pyrazol-4-YL)quinoline Synonyms：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 EINEC: Molecular Formula：C17N4H12 Molecular Weight：272.304
Target:
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[2]. LY-364947 (25 mg/kg) increases p-Akt and decreases nuclear Foxo3a in leukaemia-initiating cells in CML-affected mice[3].
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[1]. LY-364947 (3 μM) induces expression of Prox1 and LYVE-1 in almost all HDLECs after 24 hours[2]. 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[3].
Kinase Assay
Cell Assay
Animal Administration
References
Return Policy
If you are in any way unsatisfied with your purchase, you may return any item(s) within 365 days of its original purchase date.
Please provide your Order Number in the email. We strive to reply to all email inquiries within one business day.
