MKK7-COV-9 |
Catalog No.GC62315 |
MKK7-COV-9는 MKK7의 강력하고 선택적인 공유 억제제이며 MKK7의 특정 단백질-단백질 상호작용을 표적으로 합니다. MKK7-COV-9는 4.98μM의 EC50으로 LPS에 대한 반응으로 1차 B 세포 활성화를 차단합니다.
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Cas No.: 2283355-59-7
Sample solution is provided at 25 µL, 10mM.
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[1].
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[1].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)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[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)[1].
[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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