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目录:MedChemExpress LLC>>生化试剂>> MKK7-COV-9 | MCE

MKK7-COV-9 | MCE
  • MKK7-COV-9 | MCE
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参考价 3000
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更新时间:2023-06-26 11:25:38浏览次数:196评价

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CAS 2283355-59-7 分子量 320.35
分子式 C₁₈H₁₆N₄O₂ 供货周期 现货
规格 5 mg 货号 HY-122872
应用领域 医疗卫生,化工,生物产业,制药/生物制药
MKK7-COV-9 | MCEMKK7-COV-9 is a potent and selective covalent inhibitor of <b>MKK7</b> and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an <b>EC<sub>50</sub></b> of 4.98 μM<sup>[1]</sup>.</br>

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MKK7-COV-9

CAS No. : 2283355-59-7

产品活性: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.

研究领域:MAPK/ERK Pathway

作用靶点:p38 MAPK

In Vitro: 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).

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