LY 364947
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- CAS号:
- 396129-53-6
- 英文名:
- LY-364947
- 英文别名:
- CS-576;Y364947;E 616451;LY-364947;HTS 466284;LY-364947, >=98%;LY 364947;LY-364947;LY-364947 USP/EP/BP;LY364947(HTS 466284);LY-364947, 396129-53-6
- 中文名:
- LY 364947
- 中文别名:
- LY364947游离;LY364947,TGFΒR-I抑制剂;TGFΒR-I抑制剂(LY-364947);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;4-[3-(2-吡啶基)-1H-吡唑-4-基]喹啉 英文名称:LY-364947
- CBNumber:
- CB3972214
- 分子式:
- C17H12N4
- 分子量:
- 272.3
- MOL File:
- 396129-53-6.mol
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LY 364947化学性质
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熔点:
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>230℃ (dec.)
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沸点:
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490.8±45.0 °C(Predicted)
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密度:
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1.283±0.06 g/cm3(Predicted)
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储存条件:
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2-8°C
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溶解度:
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DMSO: soluble2mg/mL, clear
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酸度系数(pKa):
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8.94±0.50(Predicted)
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形态:
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powder
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颜色:
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white to beige
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稳定性:
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Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
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InChIKey:
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IBCXZJCWDGCXQT-UHFFFAOYSA-N
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LY 364947性质、用途与生产工艺
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。
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.
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.
LY364947 (HTS 466284)是一种有效的ATP竞争性TGFβR-I抑制剂，无细胞试验中IC50为59 nM，比作用于TGFβR-II选择性高7倍。
| Target | Value |
TGFβRI
(Cell-free assay)
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59 nM
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RIPK2
(Cell-free assay)
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0.11 μM
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CK1δ
(Cell-free assay)
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0.22 μM
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TGFβRII
(Cell-free assay)
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0.4 μM
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MLK-7K
(Cell-free assay)
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1.4 μM
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LY364947是一种ATP竞争性，紧密结合抑制剂，通过TGFβR-I激酶抑制P-Smad3磷酸化，Ki为28 nM。LY364947抑制体内Smad2磷酸化，NMuMg细胞中IC50 为135 nM。LY364947逆转NMuMg细胞中TGF-β介导的生长抑制，IC50为0.218 μM。LY364947在0.25 μM的低浓度下，使NMuMg细胞中的xVent2-lux BMP4响应增强30%。LY364947 (2 μM)防止NMuMg 细胞中TGF-β诱导的上皮间叶细胞转化。 LY364947 (3 μM)处理24小时后，几乎在所有HDLECs中诱导Prox1和 LYVE-1表达。 LY364947促进Foxo3a的核输出，在白血病阳性细胞中具有低Smad2/3和高Akt磷酸化水平。与OP-9基质细胞共培养后，LY364947 (< 20 μM)抑制白血病阳性细胞的集落形成能力。
在慢性腹膜炎小鼠模型中，显著增加的LYVE-1-阳性区域表明，LY364947(1 mg/kg i.p.)加速淋巴管生成。BxPC3胰腺癌细胞的肿瘤异种移植模型中，LY364947 (1 mg/kg i.p.)显著增加肿瘤组织中LYVE-1-阳性区域。在感染CML的小鼠体内白血病阳性细胞中，LY364947 (25 mg /kg)增加p-Akt，并减少细胞核Foxo3a。
LY 364947
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-13462 | LY 364947
LY-364947 | 396129-53-6 | 5mg | 550元 |
| 2024/04/30 | HY-13462 | LY 364947
LY-364947 | 396129-53-6 | 10mg | 760元 |
396129-53-6, LY 364947 相关搜索:
- TGF-beta
- Smad
- Inhibitors
- API
- 合成有机化合物配体
- 试剂盒-细胞分析试剂盒
- 细胞生物学试剂
- 小分子抑制剂，天然产物
- 小分子抑制剂
- C17H12N4
- 6129-53-6
- LY364947,TGFΒR-I抑制剂
- LY364947游离
- TGFΒR-I抑制剂(LY-364947)
- 4-[3-(2-吡啶基)-1H-吡唑-4-基]喹啉
- 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 英文名称:LY-364947
- 396129-53-6
- LY-364947 LY364947 TGF-β RI Kinase Inhibitor
- LY-364947 USP/EP/BP
- Y364947
- LY 364947;LY364947;HTS466284
- 4-[(3-Pyridin-2-yl)-1H-pyrazol-4-yl)]quinoline 95+%
- TGF-β RI Kinase Inhibitor - CAS 396129-53-6 - Calbiochem
- LY-364947?,HTS 466284, >98%
- LY 364947;LY-364947
- CS-576
- 4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]quinoline E 616451
- Quinoline, 4-[3-(2-pyridinyl)-1H-pyrazol-4-yl]-
- 2-[4-(Quinolin-4-yl)-1H-pyrazol-3-yl]pyridine, 3-(Pyridin-2-yl)-4-(quinolin-4-yl)-1H-pyrazole
- HTS 466284
- E 616451
- LY364947(HTS 466284)
- 4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]-quinoline
- [3-(Pyridin-2-yl)-4-(4-quinonyl)]-1H-pyrazole
- TGF-β RI Kinase Inhibitor
- LY364947;HTS466284; LY-364947
- LY-364947, >=98%
- LY-364947
- Transforming Growth Factor-β Type I Receptor Kinase Inhibitor
- LY-364947, 396129-53-6
- LY 364947 4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]quinoline