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LY-364947 (HTS466284) 是有效的、ATP 竞争性的TGFβR-I 抑制剂(IC50:59 nM),是对 TGFβR-II 选择性的 7 倍。


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LY-364947 (HTS466284) 是有效的、ATP 竞争性的TGFβR-I 抑制剂(IC50:59 nM),是对 TGFβR-II 选择性的 7 倍。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 196 | In stock | |
| 5 mg | ¥ 455 | In stock | |
| 10 mg | ¥ 628 | In stock | |
| 25 mg | ¥ 1,230 | In stock | |
| 50 mg | ¥ 2,280 | In stock | |
| 100 mg | ¥ 2,990 | In stock | |
| 200 mg | ¥ 4,420 | In stock | |
| 500 mg | ¥ 6,910 | In stock | |
| 1 mL x 10 mM (in DMSO) | ¥ 490 | In stock |
LY-364947 相关产品
| 产品描述 | LY-364947 (HTS466284) is a potent ATP-competitive inhibitor of TGFβR-I. |
| 靶点活性 | CK1δ:0.22 μM, RIPK2:0.11 μM, MLK7K:1.4 μM, TGFβRI:59 nM, TGFβRII:0.4 μM |
| 体外活性 | 1 mg/kg i.p. LY364947在BxPC3胰腺癌细胞的肿瘤异种移植模型中,明显增加肿瘤组织中LYVE-1-阳性区域.25 mg/kg i.p. LY364947在慢性腹膜炎小鼠模型中,明显增加的LYVE-1-阳性区域表明其加速淋巴管生成.Y364947(25 mg/kg)可增加CML感染小鼠中白血病起始细胞中的p-Akt和减少核Foxo3a. |
| 体内活性 | 在浓度低至0.25 μM时,LY364947使NMuMg细胞中的xVent2-lux BMP4响应增强30%。2 μM LY364947防止NMuMg细胞中TGF-β诱导的上皮 - 间质转化。3 μM LY364947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)抑制白血病起始细胞集落形成能力。LY364947作为一种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抑制NMuMg细胞内的体内Smad2磷酸化,IC50为135 nM。 |
| 激酶实验 | The IC50 of LY-364947 at different enzyme concentrations are determined by the filter-binding assay. Typically, 40 μL reactions in 50 mM HEPES at pH 7.5, 1 mM NaF, 200 μM pKSmad3(-3), and 50 mM ATP containing a titration of each inhibitor with concentrations of 1600, 800, 400, 200, 100, 50, 25, and 0 nM are incubated at 30°C for 30 min. The IC50 is calculated using a nonlinear regression method with GraphPad Prism software. The binding type is determined by plotting the correlation between enzyme concentrations and IC50 values. |
| 别名 | LY 364947, HTS466284 |
| 分子量 | 272.3 |
| 分子式 | C17H12N4 |
| CAS No. | 396129-53-6 |
| Smiles | N1C=C(C(=N1)C1=NC=CC=C1)C1=CC=NC2=CC=CC=C12 |
| 密度 | 1.283 g/cm3 (Predicted) |
| 颜色 | Yellow |
| 物理性状 | Solid |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| 溶解度信息 | DMSO: 7.5 mg/mL (27.54 mM), Sonication is recommended. | |||||||||||||||||||||||||
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