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编 号:F074170
分子式:C7H6O4
分子量:154.12
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生物活性:
Terreic acid, a quinone epoxide antibiotic, acts as an effective Btk inhibitor. Terreic acid blocks the interaction between PKC and the pleckstrin homology domain of Btk. Terreic acid inhibits the binding of GST-BtkPH to PKC in lysates of HMC-1 human mast cells with an IC50 of approximately 100 μM.

体内研究:
Terreic acid inhibits the late-phase response of in vivo allergic cutaneous reactions.Animal Model:BALB/c mice
Dosage:0, 0.15, 1.5, and 15 mg/kg
Administration:Injected i.p. 1 hr before antigen challenge. Ear thicknesses were measured at 1 hr and 24 hr
Result:The early response, as examined 1 hr after antigen challenge, was not affected by TA. In contrast, TA inhibited the late-phase (24 hr) response in a dose-dependent manner.

体外研究:
Terreic acid inhibits the association of Btk with PKCβII in mouse mast cells at lower concentrations (IC50 of ≈30 μM). Terreic acid inhibits the catalytic activity of Btk but not PKC.Terreic acid (pretreatment for 30 min before stimulation by antigen for 3 min) inhibits both the basal and activation levels of Btk autophosphorylating activity with IC50s of 10 μM and 3 μM, respectively.Terreic acid inhibits the autophosphorylating activity of Btk purified partially from recombinant baculovirus-infected Sf9 insect cells in a dose-dependent manner.
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