生物活性 | |||
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描述 | SMYD3 is a lysine methyltransferase implicated as an oncogene in human malignancies, which is found to be overexpressed in colorectal, breast, prostate, and hepatocellular tumors. Methylation of its target, MEKK2, is important for regulation of the MEK/ERK pathway. GSK2807 Trifluoroacetate is the trifluoroacetate form of GSK2807. GSK2807 is a potent and selective, SAM-competitive inhibitor of SMYD3 with Ki value of 14nM, with selectivity to SMYD3 over a panel of protein methyltransferases including SMYD2, PRMT1, PRMT4, PRMT5, NSD2, NSD3, DOT1L, G9a and ASH1L. GSK2807 could form a dead-end ternary complex with SMYD3 and MEKK2. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.77mL 0.35mL 0.18mL |
8.83mL 1.77mL 0.88mL |
17.65mL 3.53mL 1.77mL |