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Lck Inhibitor

CAS No. : 847950-09-8

MCE 站：Lck Inhibitor

产品活性：Lck Inhibitor 是一种有效的口服活性淋巴细胞特异性激酶 (Lck) 抑制剂，对 Lck，Lyn，Src 和 Syk 激酶的 IC₅₀ 分别为 7、2.1、4.2 和 200 nM。与 MAPK，CDK 和 RSK 家族代表相比，Lck Inhibitor 对 Lck 的选择性高出 1000 倍以上。Lck Inhibitor 抑制 T 细胞增殖和关节炎模型。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：Src

In Vitro: Lck Inhibitor (compound 25) exhibits good potency in the T-cell receptor-induced IL-2 secretion assay (IL-2, IC₅₀=0.46 μM) and also inhibits subsequent T-cell proliferation (T-cell prolif, IC₅₀=0.53 μM) in the same human T-cells. Lck Inhibitor also inhibits a human mixed lymphocyte reaction (huMLR) with a 10-fold increase in potency as compared to the other invitro cell assays utilizing purified human cells. Lck Inhibitor also displays inhibition of a mechanism-based biochemical cell assay probing Lck-dependent TCR-chain phosphorylation (TCR-chain). Lck Inhibitor shows a 10-fold reduction in potency when IL-2 is induced in a receptor-independent fashion by stimulating with phorbo lester and calcium ionophore (PMA/iono). Lck Inhibitor exhibits a similar level of potency when tested in a general proliferation assay using the human T-cell line, Jurkat (JKT).

In Vivo: Lck Inhibitor (0-60 mg/kg; p.o.; once daily; from day 9 today 17) shows a dose-dependent inhibition of arthritis.
Lck Inhibitor (p.o.; 5 mg/kg) treatment shows the C_max, AUC_0-∞, t_max and F% are 82 ng/mL, 862 ng h/mL, and 17%, respectively.

相关产品：Bioactive Compound Library Plus  |  Immunology/Inflammation Compound Library  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Reprogramming Compound Library  |  Orally Active Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Bosutinib  |  PP2  |  SU6656  |  Src Inhibitor 1  |  WH-4-023  |  Pelitinib  |  Scutellarein  |  PP1  |  1-Naphthyl PP1  |  1-NM-PP1  |  RK-24466  |  Tolimidone  |  A-770041  |  PP121  |  PP58  |  PD173955  |  MNS  |  AZM475271  |  7-Hydroxy-4H-chromen-4-one  |  Lck inhibitor 2  |  β-Hydroxyisovalerylshikonin  |  PD-161570  |  UM-164  |  CGP77675  |  Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH  |  Caffeic acid-pYEEIE TFA  |  Damnacanthal

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