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MK2-IN-3 hydrate是一种口服活性、选择性、ATP 竞争性的 MAPKAP-K2 (MK-2) 抑制剂,IC50 值为 0.85 nM,对 MK-3 (IC50=0.21 μM), MK-5 (IC50=0.081 μM), ERK2 (IC50=3.44 μM), MNK1(IC50=5.7 μM) 以及 CDK2, JNK2, IKK2, MSK1, 和 MSK2 也有选择性。
BMS-754807 is a potent and reversible inhibitor of IGF-1R/InsR with IC50 of 1.8 nM/1.7 nM, less potent to Met, Aurora A/B, TrkA/B and Ron, and shows little activity to Flt3, Lck, MK2, PKA, PKC etc.
Gamcemetinib (CC-99677) 是一种有效的、共价的和不可逆的丝裂原活化蛋白激酶活化蛋白激酶-2 (MK2) 通路抑制剂,在生化 (IC50 = 156.3 nM) 和细胞 (EC50 = 89 nM) 实验中均表现出活性。
Tpl2 Kinase Inhibitor 1 (Compound 1) is a potent and selective Tpl2 (COT kinase, MAP3K8) inhibitor that plays an important role in the regulation of the inflammatory response and the progression of some cancers[1].
Norartocarpetin 是一种酪氨酸酶抑制剂,具有较强的抑制活性,IC50 为 0.47 μM。它作为一种抗褐变剂可用于食品体系的研究,对肺癌细胞 (NCI-H460) 也具有显著的抗癌活性,IC50 为 22 μM。
CMPD1 is a selective inhibitor of non-ATP-competitive p38 MAPK-mediated MK2 phosphorylation with apparent Ki (Kiapp) of 330 nM.
PF-3644022 is a potent, ATP-competitive inhibitor of mitogen-activated protein kinase (MAPK)-activated protein kinase-2 (MK2) (IC50 = 5.2 nM and Ki = 3 nM). It inhibits tumor necrosis factor α (TNFα) production in U937 monocytic cells and peripheral blood mononuclear cells (PBMCs) (IC50 = 160 nM) and exhibits oral efficacy in acute and chronic inflammatory models.
MK2-IN-1 is a potent and selecitve MAPKAPK2 (MK2) inhibitor (IC50=0.11 μM) with a non-ATP competitive binding mode.
Tags: MK2 | MAPK/ERK Pathway | MK2 相关产品
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