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MKK7-COV-9

Catalog No. T60857 CAS 2283355-59-7

MKK7-COV-9 is a selective and potent covalent inhibitor of MKK7 with inhibitory effects on MKK7-induced protein-protein interactions.MKK7-COV-9 interrupts the activation of primary B-cells in response to LPS.MKK7-COV-9 shows low cytotoxicity at high concentrations.

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MKK7-COV-9, CAS 2283355-59-7

Pack Size	Availability	Price/USD
5 mg	In stock	$ 247.00
10 mg	In stock	$ 396.00
25 mg	In stock	$ 787.00
50 mg	In stock	$ 1,180.00
100 mg	In stock	$ 1,860.00
1 mL * 10 mM (in DMSO)	In stock	$ 272.00

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Purity: 99.55%

Purity: 98.38%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	MKK7-COV-9 is a selective and potent covalent inhibitor of MKK7 with inhibitory effects on MKK7-induced protein-protein interactions.MKK7-COV-9 interrupts the activation of primary B-cells in response to LPS.MKK7-COV-9 shows low cytotoxicity at high concentrations.
Targets&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[1]. 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[1].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[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)[1].

Molecular Weight	320.35
Formula	C18H16N4O2
CAS No.	2283355-59-7

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 10 mg/mL (31.22 mM), Sonication is recommended.

References and Literature

1. Amit Shraga, et al. Covalent Docking Identifies a Potent and Selective MKK7 Inhibitor. Cell Chem Biol. 2019 Jan 17;26(1):98-108.e5.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

MKK7-COV-9 2283355-59-7 Others inhibitor inhibit

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