MK2-IN-1 structure
|
Common Name | MK2-IN-1 | ||
|---|---|---|---|---|
| CAS Number | 1314118-92-7 | Molecular Weight | 472.966 | |
| Density | 1.3±0.1 g/cm3 | Boiling Point | 699.2±55.0 °C at 760 mmHg | |
| Molecular Formula | C27H25ClN4O2 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | 376.7±31.5 °C | |
Use of MK2-IN-1MK2-IN-1 is a potent and selecitve MAPKAPK2(MK2) inhibitor(IC50=0.11 uM) with a non-ATP competitive binding mode.IC50 value: 0.11 uM [1]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 [3]. |
| Name | MK2-IN-1 |
|---|---|
| Synonym | More Synonyms |
| Description | MK2-IN-1 is a potent and selecitve MAPKAPK2(MK2) inhibitor(IC50=0.11 uM) with a non-ATP competitive binding mode.IC50 value: 0.11 uM [1]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 [3]. |
|---|---|
| Related Catalog | |
| References |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Boiling Point | 699.2±55.0 °C at 760 mmHg |
| Molecular Formula | C27H25ClN4O2 |
| Molecular Weight | 472.966 |
| Flash Point | 376.7±31.5 °C |
| Exact Mass | 472.166595 |
| LogP | 2.69 |
| Vapour Pressure | 0.0±2.2 mmHg at 25°C |
| Index of Refraction | 1.643 |
| Storage condition | 2-8℃ |
| 5-(4-Chlorophenyl)-N-[4-(1-piperazinyl)phenyl]-N-(2-pyridinylmethyl)-2-furamide |
| 2-Furancarboxamide, 5-(4-chlorophenyl)-N-[4-(1-piperazinyl)phenyl]-N-(2-pyridinylmethyl)- |