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Cat. No.: HY-188139

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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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CAS No.: 950388-70-2
Formule: C₂₁H₂₁N₃OS
Masse moléculaire:363.48

Stockage:

Please store the product under the recommended conditions in the Certificate of Analysis.

TQ416 Chemical Structure

CAS No.: 950388-70-2

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

^[1]

PON2

0.775 μM (IC₅₀)

In Vitro

OthersAnti-cancerMitochondrial Oxidative PhosphorylationMitochondrial FunctionApoptosisCell Cycle Regulation

Others

TQ416 (compound 1) binds to recombinant human PON2 with K_d1 and K_d2 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 V_max of recombinant PON2 with increasing concentration while K_M 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].

Anti-cancer

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].

Mitochondrial Oxidative Phosphorylation

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].

Mitochondrial Function

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].

Apoptosis

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].

Cell Cycle Regulation

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.

Western Blot Analysis^[1]

Cell Line:

HeLa and A549 human cell lines
Concentration:

1 μM
Incubation Time:

2 h; 4 h
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.

Real Time qPCR^[2]

Cell Line:

human colonic goblet LS174T cells
Concentration:

1 μM (co-treated with 100 μM C12-HSL)
Incubation Time:

4 h
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.

Cell Cycle Analysis^[2]

Cell Line:

human colonic goblet LS174T cells
Concentration:

1 μM (co-treated with 100 μM C12-HSL)
Incubation Time:

4 h
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%.

Related Protocols :

Chemical Information

CAS No. 950388-70-2
Masse moléculaire 363.48
Formule C₂₁H₂₁N₃OS
SMILES

CC(C=C1)=CC=C1OCCSC2=NN=C3C=C(C)C4=C(N32)C(C)=CC=C4
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Bianconi E, et al. Synthesis and structure-activity relationship study of a library of 1-substituted [1,2,4]triazolo[4,3-a]quinolines as valuable chemical probes for paraxonase-2 (PON2). Journal of Enzyme Inhibition and Medicinal Chemistry. 2026;41(1):2643935.

[2]. Tao S, et al. N-(3-oxododecanoyl)-l-homoserine lactone modulates mitochondrial function and suppresses proliferation in intestinal goblet cells. Life sciences. 2018 May 15;201:81-88.

[3]. Horke S, et al. Novel Paraoxonase 2-Dependent Mechanism Mediating the Biological Effects of the Pseudomonas aeruginosa Quorum-Sensing Molecule N-(3-Oxo-Dodecanoyl)-L-Homoserine Lactone. Infection and immunity. 2015 Sep;83(9):3369-80.

Calculators

Calculateur de molarité

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Calculateur de dilution

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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