Cat. No.: HY-189571

Cou-Coxib

Cou-Coxib is a ROS-responsive fluorescent Celecoxib (HY-14398) prodrug that is activated by ROS triggering and self-immolation to release Celecoxib and the fluorophore Cou-OH. Celecoxib released from Cou-Coxib elevates intracellular ROS levels, induces S-phase arrest in MDA-MB-231 triple-negative breast cancer cells, and downregulates the expression of apoptosis-related proteins Bcl2, Survivin, and procaspase-3. In the H9C2 cardiomyoblast model, Cou-Coxib attenuates the cardiotoxicity caused by Celecoxib, maintains mitochondrial membrane potential, upregulates IL-10, and exhibits biocompatibility in developing zebrafish embryos. Cou-Coxib can be used for research on triple-negative breast cancer.

For research use only. We do not sell to patients.

Formula: C₄₁H₃₇BF₃N₃O₉S
Molecular Weight:815.62

Storage:

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

Cou-Coxib Chemical Structure

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Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

Bcl-2

IL-10

All Interleukin Related Isoforms :

All Bcl-2 Family Isoforms :

All Caspase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
MDA-MB-231	IC50	134.6 μM	Antiproliferative activity against human MDA-MB-231 cells assessed as viability reduction incubated 48 hrs by MTT assay. Antiproliferative activity against human MDA-MB-231 cells assessed as viability reduction incubated 48 hrs by MTT assay.	acs.jmedchem.6c01231
MCF7	IC50	151.6 μM	Antiproliferative activity against human MCF-7 cells assessed as viability reduction incubated 48 hrs by MTT assay. Antiproliferative activity against human MCF-7 cells assessed as viability reduction incubated 48 hrs by MTT assay.	acs.jmedchem.6c01231
HeLa	IC50	185.2 μM	Antiproliferative activity against human HeLa cells assessed as viability reduction incubated 48 hrs by MTT assay. Antiproliferative activity against human HeLa cells assessed as viability reduction incubated 48 hrs by MTT assay.	acs.jmedchem.6c01231
A549	IC50	280.1 μM	Antiproliferative activity against human A549 cells assessed as viability reduction incubated 48 hrs by MTT assay. Antiproliferative activity against human A549 cells assessed as viability reduction incubated 48 hrs by MTT assay.	acs.jmedchem.6c01231
HCT-116	IC50	243.5 μM	Antiproliferative activity against human HCT116 cells assessed as viability reduction incubated 48 hrs by MTT assay. Antiproliferative activity against human HCT116 cells assessed as viability reduction incubated 48 hrs by MTT assay.	acs.jmedchem.6c01231
PC-3	IC50	227.1 μM	Antiproliferative activity against human PC3 cells assessed as viability reduction incubated 48 hrs by MTT assay. Antiproliferative activity against human PC3 cells assessed as viability reduction incubated 48 hrs by MTT assay.	acs.jmedchem.6c01231
HEK293	IC50	248.9 μM	Antiproliferative activity against human HEK-293 cells assessed as viability reduction incubated 48 hrs by MTT assay. Antiproliferative activity against human HEK-293 cells assessed as viability reduction incubated 48 hrs by MTT assay.	acs.jmedchem.6c01231
NHDF	IC50	319.4 μM	Antiproliferative activity against human HDF cells assessed as viability reduction incubated 48 hrs by MTT assay. Antiproliferative activity against human HDF cells assessed as viability reduction incubated 48 hrs by MTT assay.	acs.jmedchem.6c01231
L132	IC50	237.2 μM	Antiproliferative activity against human L132 cells assessed as viability reduction incubated 48 hrs by MTT assay. Antiproliferative activity against human L132 cells assessed as viability reduction incubated 48 hrs by MTT assay.	acs.jmedchem.6c01231
H9c2	IC50	182.1 μM	Cytotoxicity against rat H9C2 cardiomyoblasts assessed as viability reduction incubated 48 hrs by MTT assay. Cytotoxicity against rat H9C2 cardiomyoblasts assessed as viability reduction incubated 48 hrs by MTT assay.	acs.jmedchem.6c01231

In Vitro

Oxidative StressOthersAnti-cancerCell Cycle RegulationApoptosisMitochondrial FunctionInnate ImmunityCytokines & Chemokines

Oxidative Stress

Cou-Coxib is activated by H₂O₂ in PBS, releasing Cou-OH with turn-on fluorescence at 453 nm, reaching saturation at 180 min and approximately 400 μM H₂O₂^[1].

Others

Cou-Coxib (100 μM) and H₂O₂ (4 mM) released 72% Celecoxib (HY-14398) and 69% Cou-OH within 4 h in PBS, with 50% release at 14 min and 36 min, respectively^[1].
Cou-Coxib (30 μM) has a log P of 3.68^[1].

Anti-cancer

Cou-Coxib was most effective in MDA-MB-231 and MCF-7 breast cancer cells, with IC₅₀ values of 134.6 and 151.6 μM after 48 h^[1].

Oxidative Stress

Anti-cancer

Cou-Coxib (150-200 μM; 12 h) induces intracellular ROS in MDA-MB-231 cells^[1].
Cou-Coxib (25 μM; 5 h) was taken up by MDA-MB-231 cells and activated by endogenous ROS to produce blue fluorescence, and pre-incubation with NAC (HY-B0215) reduced this fluorescence^[1].

Cell Cycle Regulation

Anti-cancer

Cou-Coxib (150-200 μM; 48 h) arrested MDA-MB-231 cells in the S phase; downregulated procaspase 3, Bcl2, survivin, and p53^[1].

Apoptosis

Cou-Coxib (150-200 μM; 48 h) induced less apoptosis in H9C2 cells than free Celecoxib, indicating reduced cardiotoxicity^[1].

Oxidative Stress

Mitochondrial Function

Cou-Coxib (150 μM; 12 h) induced nominal ROS in H9C2 cells without disrupting the mitochondrial membrane potential^[1].

Innate Immunity

Cytokines & Chemokines

Cou-Coxib (150-200 μM; 48 h) does not induce COX-2 and upregulates IL-10 in H9C2 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis^[1]

Cell Line:

MDA-MB-231 cells
Concentration:

150 μM and 200 μM
Incubation Time:

48 h
Result:

S phase increased from 29.4% in control to 39.5% with Cou-Coxib 150 μM and 65.0% with Cou-Coxib 200 μM.
A reduction in G1-phase population was observed.

Western Blot Analysis^[1]

Cell Line:

MDA-MB-231 cells
Concentration:

150 μM and 200 μM
Incubation Time:

48 h
Result:

Resulted in dose-dependent downregulation of procaspase 3, Bcl2, and survivin.
Also downregulated p53 expression.

Apoptosis Analysis^[1]

Cell Line:

H9C2 cardiomyoblasts
Concentration:

150 μM and 200 μM
Incubation Time:

48 h
Result:

Exhibited an IC50 of 182.1 μM in H9C2 cells.
Exposure to Cou-Coxib produced a concentration-dependent increase in early- and late-stage apoptotic populations, but the apoptotic population was significantly lower than with free celecoxib.

Western Blot Analysis^[1]

Cell Line:

H9C2 cardiomyoblasts
Concentration:

150 μM and 200 μM
Incubation Time:

48 h
Result:

Produced negligible induction of COX-2 expression.
Significantly upregulated IL-10 expression.

Cell Viability Assay^[1]

Cell Line:

H9C2 cardiomyoblasts
Concentration:

0, 5, 10, 25, 50, 100, 200 μM
Incubation Time:

48 h
Result:

showed a significantly higher IC₅₀ value (182.1 μM).

In Vivo

Cou-Coxib (10-100 μM; administered to zebrafish embryos at 72 hpf) produced a dose-dependent fluorescence turn-on signal, with no obvious developmental toxicity to zebrafish embryos^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Related Protocols :

Chemical Information

Molecular Weight 815.62
Formula C₄₁H₃₇BF₃N₃O₉S
SMILES

O=C1C=CC2=CC=C(OCC3=C(B4OC(C)(C)C(C)(C)O4)C=CC(COC(NS(C5=CC=C(N6N=C(C(F)(F)F)C=C6C7=CC=C(C)C=C7)C=C5)(=O)=O)=O)=C3)C=C2O1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Mistra R, et al. Strategic Development of Activatable Turn-On Fluorogenic Prodrugs of Celecoxib with Selective Anticancer Activity and Attenuated Cardiotoxicity. Journal of Medicinal Chemistry. 2026;69(18):21311-21334.

Calculators

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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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Cou-Coxib

All Interleukin Related Isoforms

All Bcl-2 Family Isoforms

All Caspase Isoforms