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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.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $148 | In Stock | In Stock | |
| 5 mg | $247 | In Stock | In Stock | |
| 10 mg | $396 | In Stock | In Stock | |
| 25 mg | $787 | In Stock | In Stock | |
| 50 mg | $1,180 | - | In Stock | |
| 100 mg | $1,860 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $272 | In Stock | In Stock |
| 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 |
| Smiles | CNC(=O)c1cc(NC(=O)C=C)cc(c1)-c1n[nH]c2ccccc12 |
| 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. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 10 mg/mL (31.22 mM), Sonication is recommended. | |||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (3.12 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
| ||||||||||||||||||||||||||
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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