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.

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 EC 50 of 4.98 μM.

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p38 MAP kinase

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 lipopolysa

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Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : 50 mg/mL (156.08 mM; Need ultrasonic)配制储备液