MK2-IN-3 hydrate (compound 16) is an orally active, selective, and ATP-competitive MAPKAP-K2 (MK-2) inhibitor with an IC50 of 8.5 nM. It exhibits exceptional selectivity against MK-3 (IC50=0.21 μM), MK-5 (IC50=0.081 μM), ERK2 (IC50=3.44 μM), MNK1(IC50=5.7 μM), as well as CDK2, JNK2, IKK2, MSK1, and MSK2. It suppresses TNFα production in U397 cells with an IC50 of 4.4 μM.
- Orally active.
- Selective and ATP-competitive MAPKAP-K2 (MK-2) inhibitor.
- Exceptional selectivity against MK-3, MK-5, ERK2, MNK1, CDK2, JNK2, IKK2, MSK1, and MSK2.
- Suppresses TNFα production in U397 cells with an IC50 of 4.4 μM.