MKK7-COV-9 - 10mM in DMSO , CAS No.2283355-59-7

CAS: 2283355-59-7 Cat. No.: M654588 Molecular Weight: 320.35 PubChem CID: 137796287

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

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 EC 50 of 4.98 μM

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 (EC 50 =4.06 μM) and furthermore now provides a new vector for further derivatization. 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 (LD 50 )<10 μM for these two compounds. 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. 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 EC 50 value of 4.98 μM.(EC 50 =4.98 μM for MKK7-COV-12; EC 50 >10 μM for MKK7-COV-7; EC 50 =2.23 μM for JNK-IN-8). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell 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.

IC50& Target:p38 MAP kinase

Specifications

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

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 EC 50 of 4.98 μM.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

INHIBITOR

Names and Identifiers

• PubChem CID: 137796287
• Molecular Weight: 320.35