1. MAPK/ERK Pathway
  2. p38 MAPK
  3. MKK7-COV-9

MKK7-COV-9 

Cat. No.: HY-122872
Handling Instructions

MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC50 of 4.98 μM.

For research use only. We do not sell to patients.

MKK7-COV-9 Chemical Structure

MKK7-COV-9 Chemical Structure

CAS No. : 2283355-59-7

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Description

MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC50 of 4.98 μM[1].

IC50 & Target[1]

p38 MAP kinase

 

In Vitro

Due to poor permeability, the piperidine analogs MKK7-COV-10 and MKK7-COV-11 proves to be inactive in ICW in 3T3 cells, as well as the carboxylic acid MKK7-COV-8. In contrast, as an amide counterpart , MKK7-COV-9, retains activity (EC50=4.06 μM) and furthermore now provides a new vector for further derivatization[1].
MKK7-COV-9 (10 μM; 48 hours) shows limited cytotoxic effect only at the highest tested concentration. Only one cell line, HCT116, displayed half-maximal lethal dose (LD50)<10 μM for these two compounds[1].
MKK7-COV-9 (10 μM; 2 hr pre-incubation) is able to inhibit 60% of the CD86+ response in response to LPS stimulation, in primary mouse B cells , except the negative control MKK7-NEG-1[1].
JNK is known to mediate activation of B cells in response to lipopolysaccharide (LPS; HY-D1056) through the TLR4 signaling pathway.
MKK7-COV-9 (0-10 μM; 2 hr pre-incubation) is able to mediate activation of B cells in response to LPS through the TLR4 signaling pathway, it shows a dose-response curves for inhibition of LPS induced activation and exhibits an EC50 value of 4.98 μM.(EC50=4.98 μM for MKK7-COV-12; EC50>10 μM for MKK7-COV-7; EC50=2.23 μM for JNK-IN-8)[1].

Cell Viability Assay[1]

Cell Line: MDAMB231, HCT116, HT29,COLO205, HELA,Z93T, PC3,4T1,A549, PC9, MDAMB468
Concentration: 0-10 μM
Incubation Time: 48 hours
Result: Showed little cytotoxic effect except for HCT116 cells.
Molecular Weight

320.35

Formula

C₁₈H₁₆N₄O₂

CAS No.

2283355-59-7

SMILES

O=C(NC)C1=CC(NC(C=C)=O)=CC(C2=NNC3=C2C=CC=C3)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

MKK7-COV-9p38 MAPKMDAMB231HCT116HT29,COLO205HELA,Z93TPC3,4T1,A549PC9MDAMB468cancerjnklps covalent inhibitorInhibitorinhibitorinhibit

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