MKK7-COV-9 B

Research use only, not for human use.

MKK7-COV-9 is a selective and potent covalent inhibitor of MKK7 with inhibitory effects on MKK7-induced protein-protein interactions.

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.

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).Cell Viability Assay Cell 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.

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Others

Other Targets

Others

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2283355-59-7

320.35

C18H16N4O2

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (156.08 mM; Ultrasonic )

CNC(=O)c1cc(NC(=O)C=C)cc(c1)-c1n[nH]c2ccccc12

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(-20℃)

With Ice Pack

≥ 2 years