MKK7-COV-9 - ≥97% , CAS No.2283355-59-7

CAS: 2283355-59-7 Cat. No.: M646456 Molecular Weight: 320.35 PubChem CID: 137796287

GRADE & PURITY ≥97%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

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.

Form:Solid

IC50& Target:p38 MAP kinase

Specifications

Specifications & Purity

≥97%

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 -20°C

Shipped In

Ice chest + Ice pads

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

Action Type

INHIBITOR

Purity

≥97%

Names and Identifiers

• Canonical Smiles: CNC(=O)C1=CC(=CC(=C1)C2=NNC3=CC=CC=C32)NC(=O)C=C
• IUPAC Name: 3-(1H-indazol-3-yl)-N-methyl-5-(prop-2-enoylamino)benzamide
• InChIKey: OIVBYXJDKPKZFE-UHFFFAOYSA-N
• INCHI: 1S/C18H16N4O2/c1-3-16(23)20-13-9-11(8-12(10-13)18(24)19-2)17-14-6-4-5-7-15(14)21-22-17/h3-10H,1H2,2H3,(H,19,24)(H,20,23)(H,21,22)
• PubChem CID: 137796287
• Molecular Weight: 320.35

Chemical and Physical Properties

• Solubility: DMSO : 50 mg/mL (156.08 mM; Need ultrasonic)