1314118-94-9
1314118-94-9 structure
- Name: MK2-IN-1 (hydrochloride)
- Chemical Name: MK 25 (hydrochloride)
- CAS Number: 1314118-94-9
- Molecular Formula: C27H26Cl2N4O2
- Molecular Weight: 509.427
- Catalog: Signaling Pathways MAPK/ERK Pathway MAPKAPK2 (MK2)
- Create Date: 2017-03-23 15:42:49
- Modify Date: 2025-08-26 13:43:30
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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 [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 | MK 25 (hydrochloride) |
|---|---|
| Synonyms |
2-Furancarboxamide, 5-(4-chlorophenyl)-N-[4-(1-piperazinyl)phenyl]-N-(2-pyridinylmethyl)-, hydrochloride (1:1)
5-(4-Chlorophenyl)-N-[4-(1-piperazinyl)phenyl]-N-(2-pyridinylmethyl)-2-furamide hydrochloride (1:1) MK2-IN-1 (hydrochloride) |
| 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 [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]. |
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| Related Catalog | |
| References |
| Molecular Formula | C27H26Cl2N4O2 |
|---|---|
| Molecular Weight | 509.427 |
| Exact Mass | 508.143280 |
| PSA | 61.61000 |
| LogP | 6.44740 |
| Storage condition | 2-8℃ |
| Precursor 3 | |
|---|---|
| DownStream 0 | |
