Product Name :
MK2-IN-1
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 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 .
CAS:
1314118-92-7
Molecular Weight:
472.97
Formula:
C27H25ClN4O2
Chemical Name:
5-(4-chlorophenyl)-N-[4-(piperazin-1-yl)phenyl]-N-[(pyridin-2-yl)methyl]furan-2-carboxamide
Smiles :
O=C(C1=CC=C(O1)C1C=CC(Cl)=CC=1)N(CC1=CC=CC=N1)C1C=CC(=CC=1)N1CCNCC1
InChiKey:
LIPNXDIBECKOMJ-UHFFFAOYSA-N
InChi :
InChI=1S/C27H25ClN4O2/c28-21-6-4-20(5-7-21)25-12-13-26(34-25)27(33)32(19-22-3-1-2-14-30-22)24-10-8-23(9-11-24)31-17-15-29-16-18-31/h1-14,29H,15-19H2
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.{{SGI-1776} medchemexpress|{SGI-1776} Autophagy|{SGI-1776} Epigenetics|{SGI-1776} Protocol|{SGI-1776} Data Sheet|{SGI-1776} supplier}
Shelf Life:
≥12 months if stored properly.{{Abatacept} web|{Abatacept} CTLA-4|{Abatacept} Protocol|{Abatacept} Data Sheet|{Abatacept} manufacturer|{Abatacept} Autophagy}
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.PMID:23907521
Additional information:
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 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 .|Product information|CAS Number: 1314118-92-7|Molecular Weight: 472.97|Formula: C27H25ClN4O2|Synonym:|MK2 Inhibitor|Chemical Name: 5-(4-chlorophenyl)-N-[4-(piperazin-1-yl)phenyl]-N-[(pyridin-2-yl)methyl]furan-2-carboxamide|Smiles: O=C(C1=CC=C(O1)C1C=CC(Cl)=CC=1)N(CC1=CC=CC=N1)C1C=CC(=CC=1)N1CCNCC1|InChiKey: LIPNXDIBECKOMJ-UHFFFAOYSA-N|InChi: InChI=1S/C27H25ClN4O2/c28-21-6-4-20(5-7-21)25-12-13-26(34-25)27(33)32(19-22-3-1-2-14-30-22)24-10-8-23(9-11-24)31-17-15-29-16-18-31/h1-14,29H,15-19H2|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|Products are for research use only. Not for human use.|