LY-364947

Min.Order / FOB Price:Get Latest Price

100 Gram	FOB Price: USD 1.0000

100 Gram

FOB Price: USD 1.0000

Min.Order :100 Gram
Purity: 98%
Payment Terms : L/C

Keywords

LY-364947 LY-364947;[3-(Pyridin-2-yl)-4-(4-quinonyl)]-1H-pyrazole;4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]-quinoline;LY364947(HTS 466284);E 616451;HTS 466284;2-[4-(Quinolin-4-yl)-1H-pyrazol-3-yl]pyridine, 3-(Pyridin 396129-53-6

Quick Details

Appearance:close to white solid
Application:CAS:396129-53-6; Small molecule inhibitors
PackAge:100g,500g,1kg,25kg/drum
ProductionCapacity:1000|Gram|Week
Storage:Dry seal
Transportation:shipping

Superiority:

We are specialized in custom synthesis, chemical/pharmaceutical/ pesticides outsourcing and contract research.

We are committed to provide excellence in researching, manufacturing and drug discovery process.

Our research team of scientists consists of western-trained Ph.D.s with experience and capabilities in drug R&D methodologies and medicinal chemistry.

Details:

LY 364947 用途与合成方法

生物活性	LY364947是一种有效的，ATP竞争性的TGFβR-I抑制剂，IC50为59 nM，比作用于TGFβR-II选择性高7倍。
体外研究	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.
体内研究	LY364947 (1 mg/kg i.p.) accelerates lymphangiogenesis, as evidence by significantly increased the LYVE-1-positive areas, in a mouse model of chronic peritonitis. LY364947 (1 mg/kg i.p.) significantly increases the LYVE-1-positive areas in tumor tissues in tumor xenograft models using BxPC3 pancreatic adenocarcinoma cells. LY364947 (25 mg /kg) increases p-Akt and decreases nuclear Foxo3a in leukaemia-initiating cells in CML-affected mice.