1314118-92-7

1314118-92-7 structure

Name: MK2-IN-1
Chemical Name: MK2-IN-1
CAS Number: 1314118-92-7
Molecular Formula: C₂₇H₂₅ClN₄O₂
Molecular Weight: 472.966
Catalog: Signaling Pathways MAPK/ERK Pathway MAPKAPK2 (MK2)
Create Date: 2018-04-12 02:27:32
Modify Date: 2024-01-11 18:18:13
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].

Name	MK2-IN-1
Synonyms	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)-

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	Signaling Pathways >> MAPK/ERK Pathway >> MAPKAPK2 (MK2) Research Areas >> Cancer
References	[1]. Rao AU, et al. Facile synthesis of tetracyclic azepine and oxazocine derivatives and their potential as MAPKAP-K2 (MK2) inhibitors. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1068-72. [2]. Huang X, et al. A three-step protocol for lead optimization: quick identification of key conformational features and functional groups in the SAR studies of non-ATP competitive MK2 (MAPKAPK2) inhibitors. Bioorg Med Chem Lett. 2012 Jan 1;22(1):65-70. [3]. Huang X, et al. Discovery and Hit-to-Lead Optimization of Non-ATP Competitive MK2 (MAPKAPK2) Inhibitors. ACS Med Chem Lett. 2011 Jun 24;2(8):632-7.

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℃

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