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GSK143
CAS No. : 1240390-27-5
MCE 国际站：GSK143
产品活性：GSK143 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 抑制 Erk 磷酸化 (pErk: pIC50=7.1)。GSK143 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 (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 (10-10000 nM; every 24 h for 3 days) has an IC50 of 323 nM in CLL cells. GSK 143 (1 μM; 30 mins) abrogates early signalling events including SYK phosphorylation and calcium flux.
GSK143 (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1.103.90±0.95(1.20-5.00)138±2.90134_2.60(128-145)5.25±0.135.40±0.15(4.85-5.85)108±0.60107±0.55(105-110)26.2±2.1024.8±2.30(20.2-31.5)5.60±1.616.55±1.30(2.30-9.20)5.60±0.407.40±0.50(3.20-8.50)3.11±0.371.38±0.28(0.80-3.90)大鼠0.35±0.020.24±0.07(0.00-0.55)28
1,763 8,748 3.96*** 2,123 8,945 3.21*** 2,000 8,984 3.49*** 2,129 8,258 2.88*** hsa-miR-200b 1,934 7,551 2.90*** 1,692 9,633 4.69*** 1,705 9,393 4.51*** 1,911 10,855 4.68*** hsa-miR-143 1,355 5,087
[资源] 所有的看家基因(housekeeping genes)列表+引物设计服务
LIM domain only 1 (rhombotin 1) (LMO1), mRNA 469 NM_000884 Homo sapiens IMP (inosine monophosphate) dehydrogenase 2 (IMPDH2), mRNA 1288 NM_003641 Homo sapiens interferon induced transmembrane protein 1 (9-27) (IFITM1), mRNA 4898 NM_000841 Homo
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