TQ416
TQ416 is a non-competitive inhibitor of paraoxonase 2 (PON2) with an IC50 of 0.775 μM for PON2. TQ416 inhibits PON2 lactonase activity, blocking PON2-dependent 3OC12HSL hydrolysis and intracellular acidification, thereby modulating mitochondrial function, Ca2+, apoptosis, and cell cycle-related responses. TQ416 is useful for research on PON2 biology and bacterial quorum sensing-related host responses.
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- No. CAS: 950388-70-2
- Fòrmula: C21H21N3OS
- Peso molecular:363.48
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
PON2 0.775 μM (IC50) |
In Vitro
TQ416 (compound 1) binds to recombinant human PON2 with Kd1 and Kd2 values of 0.042 μM and 5.70 μM, respectively[1].
TQ416 inhibits the 3OC12HSL lactonase activity of recombinant human PON2 with an IC50 of 0.775 μM[1].
TQ416 (0.25-1.25 μM) progressively decreases the Vmax of recombinant PON2 with increasing concentration while KM remains essentially unchanged, exhibiting non-competitive inhibition characteristics[1].
TQ416 (1 μM; 4 h; 100 μM C12-HSL) reduces the C12-HSL-related relative intracellular Ca2+ fluorescence intensity from 128.0254% to 110.1271% in LS174T cells[2].
TQ416 (1 μM; 4 h; 100 μM C12-HSL) restores the relative mRNA expression levels of CCND1 and CCND2 from 0.4262 and 0.4706 to 0.7975 and 1.0444, respectively, in LS174T cells[2].
TQ416 inhibits 3OC12 hydrolysis activity in purified recombinant PON2 and HEK PON2 cell lysates in a concentration-dependent manner[3].
TQ416 (0.5-1 μM; 50 μM 3OC12) inhibits PON2-dependent 3OC12-induced cytoplasmic acidification in EA.hy PON2 cells[3].
TQ416 (1 μM; 2 h or 4 h) increases endogenous PON2 protein levels by approximately 20% and 40-50%, respectively, in HeLa cells[1].
TQ416 (1 μM; 2 h or 4 h) reduces normalized PON2 lactonase activity to approximately 40% and 35% of control, respectively, in HeLa cells[1].
TQ416 (1 μM; 2 h or 4 h) increases endogenous PON2 protein levels by approximately 15% and 45-60% in A549 cells, respectively[1].
TQ416 (1 μM; 2 h or 4 h) reduces normalized PON2 lactonase activity to 45-50% of the control in A549 cells[1].
TQ416 (1 μM; 4 h; 100 μM C12-HSL (HY-118697)) reduces C12-HSL-related mitochondrial respiratory chain complex IV activity from 115.4910 to 48.6712 nmol/min/μg protein in LS174T cells[2].
TQ416 (1 μM; 4 h; 100 μM C12-HSL) reduces C12-HSL-related mitochondrial respiratory chain complex V activity from 17.3764 to 9.7317 nmol/min/μg protein in LS174T cells[2].
TQ416 (1 μM; 4 h; 100 μM C12-HSL) reduces C12-HSL-associated intracellular ATP levels from 1.2380 to 1.0006 nmol/mg protein in LS174T cells[2].
TQ416 (1 μM; 4 h; 100 μM C12-HSL) restores the relative fluorescence intensity of C12-HSL-associated mitochondrial activity from 49.0322% to 102.3002% in LS174T cells[2].
TQ416 (1 μM; 4 h; 100 μM C12-HSL) decreases the relative mRNA expression levels of caspase-6, caspase-8, caspase-9, and caspase-10 from 1.6745, 2.0977, 3.3133, and 2.9879 to 0.9539, 1.0949, 1.3402, and 1.3909, respectively, in LS174T cells[2].
TQ416 (1 μM; 4 h; 100 μM C12-HSL) restores the G0/G1 phase proportion of LS174T cells from 78.1133% to 67.5267% and restores the S+G2/M phase proportion from 21.8867% to 32.4733%[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa and A549 human cell lines
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Concentration:1 μM
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Incubation Time:2 h; 4 h
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Result:Induced a time-dependent increase in endogenous PON2 protein expression in both cell lines.
In HeLa cells, increased PON2 levels by approximately 20% at 2 h and 40-50% at 4 h relative to untreated controls.
In A549 cells, increased PON2 levels by approximately 15% at 2 h and 45-60% at 4 h relative to untreated controls.
Substantially inhibited lactonase activity despite the increase in protein abundance.
Reduced residual lactonase activity in HeLa cells to ~40% at 2 h and ~35% at 4 h compared with controls.
Reduced residual lactonase activity in A549 cells to 45-50% compared with controls.
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Cell Line:human colonic goblet LS174T cells
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Concentration:1 μM (co-treated with 100 μM C12-HSL)
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Incubation Time:4 h
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Result:Reduced caspase-6 mRNA relative abundance from 1.6745 to 0.9539.
Reduced caspase-8 from 2.0977 to 1.0949.
Reduced caspase-9 from 3.3133 to 1.3402.
Reduced caspase-10 from 2.9879 to 1.3909.
Increased CCND1 mRNA relative abundance from 0.4262 to 0.7975.
Increased CCND2 mRNA relative abundance from 0.4706 to 1.0444.
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Cell Line:human colonic goblet LS174T cells
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Concentration:1 μM (co-treated with 100 μM C12-HSL)
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Incubation Time:4 h
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Result:Reduced the G0/G1-phase proportion from 78.1133% to 67.5267%.
Increased the S+G2/M-phase proportion from 21.8867% to 32.4733%.
Chemical Information
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No. CAS 950388-70-2
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Peso molecular 363.48
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Fòrmula C21H21N3OS
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SMILES
CC(C=C1)=CC=C1OCCSC2=NN=C3C=C(C)C4=C(N32)C(C)=CC=C4
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TQ416 Related Classifications
HY-188139 Related Classifications
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