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编 号:F763022
分子式:C30H27ClN4O5
分子量:559.01
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生物活性:
MLKL-IN-4 (compound 56) is a potent MLKL (Mixed lineage kinase domain-like protein) inhibitor. MLKL-IN-4 inhibits necroptosis in HT-29 cells and acts downstream of MLKL phosphorylation, with EC50 of 82 nM. MLKL-IN-4 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-4 (compound 56) 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-4 (compound 56) (10 μM) slightly inhibits RIPK1, does not affect the phosphorylation status of RIPK1 and MLKL.MLKL-IN-4 (1 μM, 24 h) inhibits the translocation of MLKL to cell membranes in HT-29 cells.
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