MKK7-COV-9

SKU: orb1689176

Description

MKK7-COV-9 is a selective, covalent MKK7 inhibitor that potently disrupts MKK7-mediated protein-protein interactions. It effectively suppresses LPS-induced primary B-cell activation in vitro and demonstrates low cytotoxicity at high concentrations, making it a valuable tool for studying JNK signaling pathways in immunology and inflammation research.

Research Area

Infectious Disease & Virology; Cell Biology

Key Properties

• CAS Number: 2283355-59-7
• MW: 320.35
• Purity: 99.83% (May vary between batches)
• Formula: C₁₈H₁₆N₄O₂
• SMILES: CNC(=O)c1cc(NC(=O)C=C)cc(c1)-c1n[nH]c2ccccc12
• Target: Others,p38 MAPK
• Solubility: DMSO:10 mg/mL (31.22 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (3.12 mM)

Bioactivity

• Target IC50:
  3T3 cells:4.06 μM (EC50)
• In Vitro:
  Due to poor permeability, the piperidine analogs MKK7-COV-10 and MKK7-COV-11, as well as the carboxylic acid MKK7-COV-8, prove to be inactive in ICW in 3T3 cells. In contrast, the amide counterpart, MKK7-COV-9, retains activity (EC50=4.06 μM) and provides a new vector for further derivatization. MKK7-COV-9 (10 μM; 48 hours) shows a limited cytotoxic effect only at the highest tested concentration. Only one cell line, HCT116, displayed a half-maximal lethal dose (LD50) < 10 μM for these two compounds.With a 2-hour pre-incubation at 10 μM, MKK7-COV-9 is able to inhibit 60% of the CD86+ response to LPS stimulation in primary mouse B cells, except the negative control MKK7-NEG-1.JNK is known to mediate the activation of B cells in response to lipopolysaccharide through the TLR4 signaling pathway.MKK7-COV-9 (0-10 μM; 2 hr pre-incubation) is able to mediate the activation of B cells in response to LPS through the TLR4 signaling pathway. It shows a dose-response curve for the 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).

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GADD45β/MKK7

Compound Identifiers

PubChem CID

137796287