| SKU | Size | Availability | Price | Qty |
|---|---|---|---|---|
| M656517-1ml | 1ml | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $73.90 |
| Specifications & Purity | 10mM in DMSO |
|---|---|
| Storage Temp | Argon charged,Store at -80°C |
| Shipped In | Ice chest + Ice pads |
| Product Description | 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) inhibitorMK2-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 . |
| Canonical SMILES | C1CN(CCN1)C2=CC=C(C=C2)N(CC3=CC=CC=N3)C(=O)C4=CC=C(O4)C5=CC=C(C=C5)Cl.Cl |
|---|---|
| Molecular Weight | 509.4 |
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