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

CAS: 2283355-59-7 Cat. No.: M646456 Formula: C₁₈H₁₆N₄O₂ 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)

Frequently Asked Questions

What is the purity of this product?

This product is supplied at ≥97% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.

How should this product be stored?

Store at ?20 °C. Freezer storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships in an insulated container with ice pads. Unpack on arrival and transfer it to the storage condition stated above.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 2283355-59-7, the molecular formula is C18H16N4O2, and the molecular weight is 320.35 g/mol. InChIKey OIVBYXJDKPKZFE-UHFFFAOYSA-N.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.