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MK2-IN-1 hydrochloride is a potent and selecitve MAPKAPK2(MK2) inhibitor(IC50=0.11 uM) with a non-ATP competitive binding mode. IC50 value: 0.11 uM Target: MAPKAPK2(MK2) inhibitor MK2-IN-1 was profiled for kinase selectivity by screening against a broad panel of 150 protein kinases at a concentration of 10 μM, and only CK1γ3 was significantly inhibited at greater than 50%. MK2-IN-1 inhibited pro-inflammatory cytokine secretion from the human THP1 acute monocytic leukemia cell line, causing dose-dependent inhibition of LPS-stimulated TNFα and IL6 secretion. MK2-IN-1 also dose dependently inhibited IL1β-stimulated matrixmetalloprotease (MMP)13 secretion from the SW1353 chondrosarcoma cell line and human primary chondrocyte cultures. Of note, given its high degree of selectivity, our data suggest that MK2-IN-1 may be an excellent pharmacologic tool for specifically exploring and validating MK2 biology.
| Molecular Weight | 509.43 |
| CAS Number | 1314118-94-9 |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage | 2-8°C, sealed |
[1] Mustafa Kemal Gmş. Green Formation of Novel Pyridinyltriazole-Salicylidene Schiff Bases
| Related MAPKAPK2/MAP3K/MAP4K Products |
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Takinib is a potent and selective TAK1 inhibitor with an IC50 of 9.5 nM, more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. |
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GNE-495 is a potent and selective MAP4K4 inhibitor with an IC50 of 3.7 nM. |
| NG25
NG25 is a potent dual TAK1 and MAP4K2 inhibitor with IC50s of 149 nM and 21.7 nM, respectively. |
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PF-06260933 is a potent inhibitor of MAP4K4 with an IC50 of 3.7 nM, possessing excellent kinome selectivity. |
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MAP4K4-IN-3 is a potent and selective MAP4K4 inhibitor with an IC50 of 14.9 nM in kinase assay, and an IC50 of 470 nM in cell assay. |
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