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MKK7-COV-9
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MKK7-COV-9图片
CAS NO:2283355-59-7
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
MKK7-COV-9 是一种有效的、选择性的 MKK7 共价抑制剂,靶向 MKK7 的一种特异性蛋白-蛋白相互作用。MKK7-COV-9 阻断了原代 B 细胞应对 LPS 的激活的 EC50 值为 4.98 μM.
Cas No.2283355-59-7
分子式C18H16N4O2
分子量320.35
溶解度DMSO : 50 mg/mL (156.08 mM; Need ultrasonic)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.