| Bioactivity | MK2-IN-3 hydrate (compound 16) is an orally active, selective, and ATP-competitive MAPKAP-K2 (MK-2) inhibitor with an IC50 of 0.85 nM.MK2-IN-3 hydrate is 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[1]. | |||||||||
| Target | IC50: 0.85 nM (MK-2), 0.21 μM (MK-3), 0.081 μM (MK-5), 3.44 μM (ERK2), 5.7 μM (MNK1) | |||||||||
| Invitro | MK2-IN-3 hydrate suppresses TNFα production in U397 cells with an IC50 of 4.4 μM[1]. | |||||||||
| Name | MK2-IN-3 hydrate | |||||||||
| CAS | 1186648-22-5 | |||||||||
| Formula | C21H18N4O2 | |||||||||
| Molar Mass | 358.39 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. Anderson DR, et al. Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2). J Med Chem. 2007 May 31;50(11):2647-54. |
MK2-IN-3 hydrate
CAS: 1186648-22-5 F: C21H18N4O2 W: 358.39
MK2-IN-3 hydrate (compound 16) is an orally active, selective, and ATP-competitive MAPKAP-K2 (MK-2) inhibitor with an IC
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