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Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $1,520 | 1-2 weeks | |
50 mg | $1,980 | 1-2 weeks | |
100 mg | $2,500 | 1-2 weeks |
Description | MK2-IN-1 is a potent and selecitve MAPKAPK2(MK2) inhibitor(IC50=0.11 uM) with a non-ATP competitive binding mode. |
In vitro | 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 [3]. |
Alias | MK2-IN-1 (MK2 Inhibitor) |
Molecular Weight | 472.97 |
Formula | C27H25ClN4O2 |
Cas No. | 1314118-92-7 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
Solubility Information | DMSO: Soluble |
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