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产品介绍
产品信息
商品描述
MKK7-COV-9 is a potent and selective MKK7 covalent inhibitor targeting a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks the activation of primary B cell in response to LPS with an EC 50 of 4.98 μM [1].
分子量
320.352
纯度
98%
In vitro(体外研究)
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 (EC 50 =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 (LD 50 )<10 μM for these two compounds [1].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) 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 EC 50 value of 4.98 μM.(EC 50 =4.98 μM for MKK7-COV-12; EC 50 >10 μM for MKK7-COV-7; EC 50 =2.23 μM for JNK-IN-8) [1]. Cell Viability Assay [1] 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.
背景
分子式
C18H16N4O2
CAS号
2283355-59-7
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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