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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

作用靶点：Syk  |  PERK

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 T_1/2 of 4.2 hours, low clearance (16 mL/min/kg), moderate bioavailability of 30% and a V_ss of 4.1 L/kg in rats.

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