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货期:1-2天
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1 mg/5 mg/10 mg/25 mg/50 mg
| 规格: | 1 mg | 产品价格: | ¥681.0 |
|---|---|---|---|
| 规格: | 5 mg | 产品价格: | ¥1500.0 |
| 规格: | 10 mg | 产品价格: | ¥2500.0 |
| 规格: | 25 mg | 产品价格: | ¥5400.0 |
| 规格: | 50 mg | 产品价格: | ¥9200.0 |
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GSK143 dihydrochloride
CAS No. : 2341796-81-2
MCE 国际站:GSK143 dihydrochloride
产品活性:GSK143 dihydrochloride 是一种具有口服活性,高选择性的脾酪氨酸激酶 (SYK) 抑制剂,pIC50 为 7.5。GSK143 dihydrochloride 抑制 Erk 磷酸化 (pErk: pIC50=7.1)。GSK143 dihydrochloride 可以减轻炎症,并防止小鼠肠道肌层中免疫细胞的募集。
研究领域:Protein Tyrosine Kinase/RTK | Cell Cycle/DNA Damage
In Vitro: GSK143 dihydrochloride (compound 20) inhibits ZAP-70 (pIC50=4.7), LCK (pIC50=5.3), LYN (pIC50=5.4), JAK1/2/3 (pIC50=5.8/5.8/5.7), Aurora B (pIC50=4.8), hWB (pIC50=6.6), hERG (pIC50=4.7).
GSK143 dihydrochloride (10-10000 nM; every 24 hours for 3 days) has an IC50 of 323 nM in CLL cells. GSK 143 dihydrochloride (1 μM; 30 mins) abrogates early signalling events including SYK phosphorylation and calcium flux.
GSK143 dihydrochloride (0.1-10 μM; for 30 min) reduces cytokine expression in bone marrow derived macrophages in a concentration-dependent manner.
In Vivo: GSK143 (0.1-10 mg/kg; orally; 1.5 hours) reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis of 1 mg/kg.
GSK143 (3, 10, 30, 100 mg/kg; oral; 1 hour before ovalbumin challenge) reduces the cutaneous reverse passive Arthus reaction in a dose dependent manner by approximately 50% and 70% at 10 mg/kg and 30 mg/kg, respectively.
GSK143 (iv of 1 mg/kg; po of 3 mg/kg) has a T1/2 of 4.2 hours, low clearance (16 mL/min/kg), moderate bioavailability of 30% and a Vss of 4.1 L/kg in rats.
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文献和实验真爱满行囊 我最近在体外细胞做的关于gsk3-beta功能问题,发现药物处理以后,gsk-3-beta的总表达量下调,如果是这样的话 1、我是否能够得出gsk-3-beta的活性下调的结论? 2、是否还有必要做非活性形式的表达量?我的理解是,基础状态下,gsk-3beta维持的是低活性状态,如果总量都下调了,那应该能够得出活性降低的结论了吧? 3、另外,在这种情况下我是否有必要去做gsk-3-beta的216位点的活性形式的表达
【求助】如何证明GSK-3beta的抑制是由Wnt通路引起的?
magichunter 我现在能够证明GSK-3beta的活性受到了抑制,同时也证明了b-catenin在核内和胞浆内的表达都升高了,同时胞浆内的磷酸化b-catenin含量降低(Wnt通路被激活了吗)。另外Akt的磷酸化增高(应该是PI3K/Akt通路被激活了)。因为Wnt和PI3K/Akt两条通路都可以抑制GSK的活性。 请问能否判断GSK的抑制是由Wnt通路的激活引起的,还是有PI3K/Akt的激活引起的?还是两条通路都激活了? (暂时我还不能进行
lizzy514 请问细胞中总的GSK-3β应该包括磷酸化的GSK-3β蛋白吧? 做WB检测细胞中GSK-3β和9位点磷酸化的GSK-3β(活性受抑制的形式)蛋白表达的变化,提取的是细胞总蛋白,那用GSK-3β抗体检测的GSK-3β的表达不仅仅只是非磷酸化的蛋白(活性形式)吧? 万分感谢!!! 坏坏的真心爱 有人回答吗?我也想知道 zhanglin1229 不是,GSK-3β
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