产品英文名称:LY364947
产品中文名称:ATP 竞争性TGFβR-I 抑制剂
LY364947 ATP 竞争性TGFβR-I 抑制剂生物活性:
产品描述 |
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。 |
靶点 |
TGFβRI |
RIPK2 |
CK1δ |
TGFβRII |
MLK-7K |
IC50 |
59 nM |
0.11 μM |
0.22 μM |
0.4 μM |
1.4 μM |
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.
|
LY364947 ATP 竞争性TGFβR-I 抑制剂化学特性:
溶解性 (25°C) * |
体外 |
DMSO |
1 mg/mL (3 mM) |
水 |
<1 mg/mL (<1 mM) |
乙醇 |
<1 mg/mL (<1 mM) |
* <1 mg/ml 指产品微溶或不溶
* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。 |
Chemical Name |
Quinoline, 4-[3-(2-pyridinyl)-1H-pyrazol-4-yl]- |
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LY2109761
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Ibrutinib (PCI-32765)
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GW788388
GW788388是一种有效的,选择性的ALK5抑制剂,IC50为18 nM,也抑制其他TGF-βI型和II型受体激酶活性,但不抑制BMP II型受体。
Rigosertib (ON-01910)
Rigosertib (ON-01910)是一种非ATP竞争性的PLK1抑制剂,IC50为9 nM,比作用于Plk2选择性高30倍,对Plk3没有抑制活性。Phase 3。
特征: Rigosertib是作用于Polo样激酶(PLK1)的非ATP竞争性抑制剂。
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