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.
Product information
CAS Number: 2283355-59-7
Molecular Weight: 320.35
Formula: C18H16N4O2
Chemical Name: 3-(1H-indazol-3-yl)-N-methyl-5-(prop-2-enamido)benzamide
Smiles: CNC(=O)C1=CC(=CC(=C1)C1=NNC2=CC=CC=C21)NC(=O)C=C
InChiKey: OIVBYXJDKPKZFE-UHFFFAOYSA-N
InChi: 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)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 50 mg/mL (156.08 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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. 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. 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 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).
Products are for research use only. Not for human use.
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