LY 364947
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- CAS號:
- 396129-53-6
- 英文名:
- LY-364947
- 英文別名:
- 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
- 中文別名:
- LY364947游離;LY364947,TGFΒR-I抑制劑;TGFΒR-I抑制劑(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;化合物L(fēng)Y-364947,10 MM DMSO 溶液;4-[3-(2-吡啶基)-1H-吡唑-4-基]喹啉 英文名稱:LY-364947;LY 364947,ATP-COMPETITIVE TGFBETA RECEPTOR KINASE I抑制劑
- CBNumber:
- CB3972214
- 分子式:
- C17H12N4
- 分子量:
- 272.3
- MOL File:
- 396129-53-6.mol
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LY 364947化學(xué)性質(zhì)
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熔點:
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>230℃ (dec.)
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沸點:
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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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儲存條件:
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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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酸度系數(shù)(pKa):
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8.94±0.50(Predicted)
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形態(tài):
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powder
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顏色:
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white to beige
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穩(wěn)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性質(zhì)、用途與生產(chǎn)工藝
LY364947是一種有效的，ATP競爭性的TGFβR-I抑制劑，IC50為59 nM，比作用于TGFβR-II選擇性高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)是一種有效的ATP競爭性TGFβR-I抑制劑，無細(xì)胞試驗中IC50為59 nM，比作用于TGFβR-II選擇性高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是一種ATP競爭性，緊密結(jié)合抑制劑，通過TGFβR-I激酶抑制P-Smad3磷酸化，Ki為28 nM。LY364947抑制體內(nèi)Smad2磷酸化，NMuMg細(xì)胞中IC50 為135 nM。LY364947逆轉(zhuǎn)NMuMg細(xì)胞中TGF-β介導(dǎo)的生長抑制，IC50為0.218 μM。LY364947在0.25 μM的低濃度下，使NMuMg細(xì)胞中的xVent2-lux BMP4響應(yīng)增強(qiáng)30%。LY364947 (2 μM)防止NMuMg 細(xì)胞中TGF-β誘導(dǎo)的上皮間葉細(xì)胞轉(zhuǎn)化。 LY364947 (3 μM)處理24小時后，幾乎在所有HDLECs中誘導(dǎo)Prox1和 LYVE-1表達(dá)。 LY364947促進(jìn)Foxo3a的核輸出，在白血病陽性細(xì)胞中具有低Smad2/3和高Akt磷酸化水平。與OP-9基質(zhì)細(xì)胞共培養(yǎng)后，LY364947 (< 20 μM)抑制白血病陽性細(xì)胞的集落形成能力。
在慢性腹膜炎小鼠模型中，顯著增加的LYVE-1-陽性區(qū)域表明，LY364947(1 mg/kg i.p.)加速淋巴管生成。BxPC3胰腺癌細(xì)胞的腫瘤異種移植模型中，LY364947 (1 mg/kg i.p.)顯著增加腫瘤組織中LYVE-1-陽性區(qū)域。在感染CML的小鼠體內(nèi)白血病陽性細(xì)胞中，LY364947 (25?mg?/kg)增加p-Akt，并減少細(xì)胞核Foxo3a。
LY 364947
上下游產(chǎn)品信息
上游原料
下游產(chǎn)品
| 更新日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS編號 | 包裝 | 價格 |
|---|
| 2025/02/08 | HY-13462 | LY 364947
LY-364947 | 396129-53-6 | 5mg | 550元 |
| 2025/02/08 | HY-13462 | LY 364947
LY-364947 | 396129-53-6 | 10mM * 1mLin DMSO | 605元 |
396129-53-6, LY 364947 相關(guān)搜索:
- TGF-beta
- Smad
- Inhibitors
- API
- 抑制劑
- 合成有機(jī)化合物配體
- 試劑盒-細(xì)胞分析試劑盒
- 細(xì)胞生物學(xué)試劑
- 小分子抑制劑，天然產(chǎn)物
- 小分子抑制劑
- C17H12N4
- 6129-53-6
- 化合物L(fēng)Y-364947,10 MM DMSO 溶液
- LY 364947,ATP-COMPETITIVE TGFBETA RECEPTOR KINASE I抑制劑
- LY364947,TGFΒR-I抑制劑
- LY364947游離
- TGFΒR-I抑制劑(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 英文名稱:LY-364947
- 396129-53-6
- TGF-β RI Kinase Inhibitor
- LY-364947, 10 mM in DMSO
- LY 364947, ATP-competitive TGFbeta receptor kinase I inhibitor
- 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