AMG-47a is a highly potent and orally bioavailable inhibitor of lymphocyte-specific protein tyrosine kinase (Lck), with an exceptionally low IC50 of 0.2 nM. Beyond its primary target, AMG-47a also effectively inhibits several other kinases, including VEGF2, p38α, Jak3, alongside mixed lymphocyte reaction (MLR) and interleukin-2 (IL-2) production, with IC50 values ranging from 1 nM to 72 nM. These properties equip AMG-47a with significant anti-inflammatory capabilities, marking it as a compound of interest for inflammatory disease research and potential therapeutic development[1].
AMG-47a 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Murine RAW cells
0.25–0.5 µM
24 h
AMG-47a inhibited TSI-induced necroptosis at 0.25–0.5 µM but showed toxicity at doses >1 µM.
Cell Death Dis. 2022 Apr 1;13(4):291.
Murine dermal fibroblasts (MDFs)
1 µM
6 h or 24 h
Assessed the ability of AMG-47a to protect against necroptotic cell death induced by TSQ or TSI, showing significant protection against TSQ-induced cell death.
Cell Death Dis. 2022 Apr 1;13(4):291.
Human THP-1 cells
~100 nM to ~2.5 µM
24 h or 48 h
AMG-47a robustly protected THP-1 cells from TSI-induced cell death with IC50 values of ~100 nM to ~2.5 µM.
Cell Death Dis. 2022 Apr 1;13(4):291.
Human HT29 cells
~100 nM to ~2.5 µM
24 h or 48 h
AMG-47a robustly protected HT29 cells from TSQ- and TSI-induced cell death with IC50 values of ~100 nM to ~2.5 µM.
Cell Death Dis. 2022 Apr 1;13(4):291.
Human U937 cells
~100 nM to ~2.5 µM
24 h or 48 h
AMG-47a robustly protected U937 cells from TSQ- and TSI-induced cell death with IC50 values of ~100 nM to ~2.5 µM.
Cell Death Dis. 2022 Apr 1;13(4):291.
HoxA9-Meis1 AML cells
125 nM to 1 µM
24 h
AMG-47a provided substantial protection against necroptotic cell death in HoxA9-Meis1 AML cells at 125 nM to 1 µM.
Cell Death Dis. 2022 Apr 1;13(4):291.
A375 cells
1μM
24 hours
Evaluate the inhibitory effect of AMG-47a on ERK1/2 phosphorylation
搜索
