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编 号:F763004
分子式:C31H29ClN4O6
分子量:589.04
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生物活性:
MLKL-IN-3 (compound 66) is a potent MLKL (Mixed lineage kinase domain-like protein) inhibitor. MLKL-IN-3 inhibits necroptosis in HT-29 cells and acts downstream of MLKL phosphorylation, with EC50 of 31 nM. MLKL-IN-3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

体内研究:
MLKL-IN-3 (compound 66) shows T1/2 over 48 h and more than 150-fold lower reaction rates with glutathione (GSH), which potentially decreased their off-target effects and cell toxicity.

体外研究:
MLKL-IN-3 (compound 66) (1 μM, 24 h) inhibits the translocation of MLKL to cell membranes in HT-29 cells.MLKL-IN-3 does not affect the phosphorylation status of RIPK1 and MLKL.
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