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LY 364947

LY 364947 更多供应商
公司名称:上海技毅生物科技有限公司  黄金产品
联系电话:13621943973
产品介绍:中文名称:LY 364947
英文名称:LY-364947
CAS:396129-53-6
纯度:>98% 包装信息:1g,10g,100g,1kg 备注:仅供实验室使用
公司名称:上海波以尔化工有限公司  
联系电话:86-15221043597
产品介绍:英文名称:LY364947
CAS:396129-53-6
公司名称:百灵威科技有限公司  
联系电话:400-666-7788 +86-10-82848833
产品介绍:中文名称:4-(3-吡啶-2-基-1H-吡唑-4-基)喹啉
英文名称:4-(3-Pyridin-2-yl-1H-pyrazol-4-yl)quinoline
CAS:396129-53-6
纯度:97% 包装信息:1g 备注:化学试剂、精细化学品、医药中间体、材料中间体
公司名称:武汉易泰科技有限公司上海分公司  
联系电话:86-21-50328103 * 801、802、803、804 Mobile:18930552037
产品介绍:英文名称:LY 364947;4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]-quinoline
CAS:396129-53-6
纯度:99% HPLC 包装信息:1Mg ; 5Mg;10Mg ;100Mg;250Mg ;500Mg ;1g;2.5g ;5g ;10g
公司名称:上海佰世凯化学科技有限公司  
联系电话:+86(0)21-20908456
产品介绍:英文名称:LY364947(HTS 466284)
CAS:396129-53-6
备注:C13851
LY 364947
生物活性 体外研究 体内研究
中文名称:LY 364947
中文同义词:4-(3-吡啶-2-基-1H-吡唑-4-基)喹啉;4-[3-(2-吡啶基)-1H-吡唑-4-基]喹啉;LY364947;HTS466284; LY-364947;4-[3-(2-吡啶基)-1H-吡唑-4-基]喹啉 英文名称:LY-364947
英文名称:LY-364947
英文同义词: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-2-yl)-4-(quinolin-4-yl)-1H-pyrazole;Quinoline, 4-[3-(2-pyridinyl)-1H-pyrazol-4-yl]-
CAS号:396129-53-6
分子式:C17H12N4
分子量:272.31
EINECS号:
相关类别:API;小分子抑制剂;Inhibitors;小分子抑制剂,天然产物;Smad;TGF-beta
Mol文件:396129-53-6.mol
LY 364947
LY 364947 性质
储存条件 Store at RT
溶解度 DMSO: soluble2mg/mL, clear
颜色white to beige
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.
安全信息
危险品标志 T,N
危险类别码 25-36/37/38-50/53
安全说明 26-45-60-61
危险品运输编号 UN 2811 6.1/PG 3
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