MKK7-COV-9 B

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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 EC50 of 4.98 μM.

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).Cell Viability Assay 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.

——

——

Others

Other Targets

Others

——

——

2283355-59-7

320.35

C18H16N4O2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 50 mg/mL (156.08 mM; 超声助溶 )

CNC(=O)c1cc(NC(=O)C=C)cc(c1)-c1n[nH]c2ccccc12

——

(-20℃)

With Ice Pack

≥ 2 years