上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。
GSK143
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。
GSK143 Chemical Structure
CAS No. : 1240390-27-5
| 规格 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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* Please select Quantity before adding items.
| 生物活性 |
GSK143 is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.5. GSK143 inhibits phosphorylated Erk (pErk: pIC50=7.1)[1]. GSK143 reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice[2][3].
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IC50 & Target |
pIC50: 7.5 (SYK) and 7.1 (pErk)[1]
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体外研究
(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)[1].
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[2].
GSK143 (0.1-10 μM; for 30 min) reduces cytokine expression in bone marrow derived macrophages in a concentration-dependent manner[3].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[2]
| Cell Line: |
Chronic lymphocytic leukaemia (CLL) cells |
| Concentration: |
10, 100, 1000, 10000 nM |
| Incubation Time: |
Every 24 h for 3 days |
| Result: |
Had an IC50 of 323 nM. |
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体内研究
(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[3].
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[2].
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[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: |
Wild type C57NL/BL6 mice, 10-12 weeks old[3] |
| Dosage: |
0.1, 1, 3, 10 mg/kg |
| Administration: |
Orally; 1.5 hours before intestinal manipulation (IM) |
| Result: |
Reduced inflammation and prevented recruitment of immune cells in the intestinal muscularis. |
| Animal Model: |
Male CD rats (175-200 g)[1] |
| Dosage: |
1 mg/kg of iv; 3 mg/kg of po (Pharmacokinetic Analysis) |
| Administration: |
IV or PO |
| Result: |
Had 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. |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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[1]. John Liddle, et al. Discovery of GSK143, a Highly Potent, Selective and Orally Efficacious Spleen Tyrosine Kinase Inhibitor. Bioorg Med Chem Lett. 2011 Oct 15;21(20):6188-94.
[2]. Abraham M Varghese, et al. Highly Selective SYK Inhibitor, GSK143, Abrogates Survival Signals in Chronic Lymphocytic Leukaemia. Br J Haematol. 2018 Sep;182(6):927-930.
[3]. Sjoerd H W van Bree, et al. Inhibition of Spleen Tyrosine Kinase as Treatment of Postoperative Ileus. Gut. 2013 Nov;62(11):1581-90.
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