Home Neuronal Signaling COX inhibitor Celecoxib For research use only.

Celecoxib

Synonyms: SC 58635

Celecoxib is a selective COX-2 inhibitor with IC50 of 40 nM in Sf9 cells.

Celecoxib Chemical Structure

Celecoxib Chemical Structure

CAS No. 169590-42-5

Purity & Quality Control

Celecoxib Related Products

Signaling Pathway

COX Signaling Pathways

COX Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A549 Function Assay 0.1-30 μM 48 h induces ICAM-1 expression on both protein and mRNA level 26513172
H460 Function Assay 0.1-30 μM 48 h induces ICAM-1 expression on both protein and mRNA level 26513172
HKESC-2 Growth Inhibition Assay 20 μM 48 h  significantly increases the IC50 values of oxaliplatin  26474693
CaES-17 Growth Inhibition Assay 20 μM 48 h  significantly increases the IC50 values of oxaliplatin  26474693
HKESC-2 Apoptosis Assay 20 μM 48 h  reduces oxaliplatin-induced apoptosis 26474693
CaES-17 Apoptosis Assay 20 μM 48 h  reduces oxaliplatin-induced apoptosis 26474693
A549 Growth Inhibition Assay 5-160 μM 48 h  DMSO IC50=163.4 μM 26464643
HCC827 Growth Inhibition Assay 5-160 μM 48 h  DMSO IC50=69.2 μM 26464643
A549 Apoptosis Assay 80 µM 48 h  DMSO induces apoptosis 26464643
HCC827 Apoptosis Assay 80 µM 48 h  DMSO induces apoptosis 26464643
SGC-7901/DDP Function Assay 10 µM 24 h inhibits cyclooxygenase-2 and P-glycoprotein expression 26407653
SGC-7901  Growth Inhibition Assay 24 h  IC50=115.08 μM 26407653
SGC-7901/DDP Growth Inhibition Assay 24 h  IC50=35.45 μM 26407653
SGC-7901/DDP Apoptosis Assay 10 µM 24 h induces apoptosis combined with with cisplatin 26407653
SGC-7901/DDP Function Assay 10 µM 24 h inhibits the expression of P-glycoprotein through blocking EP2, and inactivating PKA and CREB  26407653
SGC-7901/DDP Function Assay 10 µM 24 h causes a marked decrease in the level of Bcl-2 protein 26407653
H357 Growth Inhibition Assay 7.5/10 μM 48 h DMSO inhibits cell growth combined with Sabutoclax 26009874
TAF Function Assay 10 µM 7 d affects TAFs adhesive properties 25987127
TAF Function Assay 10 µM 30-120 min poorly affects dAkt phosphorylation consequent to EGF signaling 25987127
TAF Function Assay 10 µM 48 h increases EGFR mRNA and protein expression 25987127
PANC-1 Growth Inhibition Assay 20/60/100 μM 24/48/72 h inhibits cell growth in both time and dose dependent manner 25973062
PANC-1 Function Assay 20/60/100 μM 24 h attenuats cell invasion and migration in a concentration-dependent manner  25973062
HeLa  Growth Inhibition Assay 20 μM  24 h enhances radiation-induced inhibition of cell proliferation 25770423
SACC-83 Growth Inhibition Assay 20 μM  24 h enhances radiation-induced inhibition of cell proliferation 25770423
HeLa  Apoptosis Assay 20 μM  24 h enhances radiation-induced inhibition of cell apoptosis 25770423
SACC-83 Apoptosis Assay 20 μM  24 h enhances radiation-induced inhibition of cell apoptosis 25770423
HeLa  Function Assay 20/40/80 μM 24 h upregulats PTEN partially by inhibiting Sp1, and activates PTEN and inactivates AKT 25770423
SACC-83 Function Assay 20/40/80 μM 24 h upregulats PTEN partially by inhibiting Sp1, and activates PTEN and inactivates AKT 25770423
HLCZ01 Growth Inhibition Assay 0–60 µM 48 h DMSO inhibits cell growth in a dose dependent manner 25724899
HLCZ01 Function Assay 40 μM 24 h DMSO increases accumulation of G0/G1-phase cells combined with IFN-α 25724899
HLCZ01 Apoptosis Assay 40 μM 24 h DMSO enhances apoptosis combined with IFN-α 25724899
HLCZ01 Function Assay 40 μM 24 h DMSO increases TRAIL expression combined with Interferon-α 25724899
MGC803 Growth Inhibition Assay 0-60 μM 72 h IC50=47.25 ± 6.43 μM 25701378
SGC7901 Growth Inhibition Assay 0-60 μM 72 h IC50=43.53 ± 5.12 μM 25701378
MGC803 Function Assay 40 μM 8/16/24 h upregulats Cbl-b expression 25701378
SGC7901 Function Assay 40 μM 8/16/24 h upregulats Cbl-b expression 25701378
MCF-7  Growth Inhibition Assay 1/10 μM 72 h DMSO enhances calcitriol-induced cell growth inhibition 25667510
MDA-MB-231  Growth Inhibition Assay 1/10 μM 72 h DMSO enhances calcitriol-induced cell growth inhibition 25667510
MDA-MB-231 Function Assay 0-40 µM 4-24 h increases COX-2 protein expression in both time and dose dependent manner 25587329
MCF-7 Function Assay 0-40 µM 4-24 h enhances the effects of TPA on ABCG2 expression  25587329
MCF7-MX  Function Assay 0-40 µM 4-24 h enhances the effects of TPA on ABCG2 expression  25587329
MDA-MB-231 Function Assay 0-40 µM 4-24 h stimulates the expression of ABCG2 up to 4.27 times to control level by 12 h  25587329
A2780 Function Assay 5/10/15 μM 48 h decreases Cox-2 expression in a dose-dependent manner 25424898
SKOV3  Function Assay 5/10/15 μM 48 h decreases Cox-2 expression in a dose-dependent manner 25424898
A2780 Function Assay 5/10/15 μM 48 h elevates the expression of E-cadherin and keratin 25424898
SKOV3  Function Assay 5/10/15 μM 48 h elevates the expression of E-cadherin and keratin 25424898
A2780 Function Assay 5/10/15 μM 48 h decreases the expression of N-cadherin and Vimentin 25424898
SKOV3  Function Assay 5/10/15 μM 48 h decreases the expression of N-cadherin and Vimentin 25424898
A2780 Function Assay 5/10/15 μM 1 h increases the expression of p-AKT and p-ERK in a dose-dependent manner 25424898
SKOV3  Function Assay 5/10/15 μM 1 h increases the expression of p-AKT and p-ERK in a dose-dependent manner 25424898
HCT-15 Function Assay 10-50 μM 6-36 h induces the expression of COX-2 in both dose and time dependent manner 25218028
HT-29  Function Assay 10-50 μM 6-36 h induces the expression of COX-2 in both dose and time dependent manner 25218028
HSC3  Cell Viability Assay 0–40 μM 48 h IC50=25.5±1.780 μM 25198789
HSC3  Apoptosis Assay 25 μM 48 h induces apoptosis 25198789
HSC3  Function Assay 25 μM 48 h exhibits significantly reduced migration combined with CET 25198789
HSC3  Function Assay 25 μM 48 h inhibits HSC3 cell invasion combined with CET 25198789
HSC3  Function Assay 25 μM 72 h decreases MMP-2 and MMP-9 proteins  25198789
201T  Growth Inhibition Assay 72 h DMSO IC50=48.6 µM 25057941
273T Growth Inhibition Assay 72 h DMSO IC50=80.5 µM 25057941
Hep-2 Growth Inhibition Assay 30/50/100 μM 12/24/36/48 h DMSO inhibits cell growth in both time and dose dependent manner 24998564
Hep-2 Apoptosis Assay 50 μM 0-48 h DMSO induces apoptosis in a time dependent manner 24998564
Hep-2 Function Assay 50 μM 0-48 h DMSO reduces the telomerase activity gradually 24998564
Hep-2 Function Assay 50 μM 0-48 h DMSO decreases the mRNA expression of hTERT 24998564
SGC-7901 Growth Inhibition Assay 10/50/100 μM 24/48/72 h DMSO inhibits cell growth in both time and dose dependent manner 24992958
MKN-45 Growth Inhibition Assay 10/50/100 μM 24/48/72 h DMSO inhibits cell growth in both time and dose dependent manner 24992958
SGC-7901 Function Assay 10/50/100 μM 48 h DMSO downregulates the mRNA expression levels of COX-2 and PCNA in a dose dependent manner 24992958
MKN-45 Function Assay 10/50/100 μM 48 h DMSO downregulates the mRNA expression levels of COX-2 and PCNA in a dose dependent manner 24992958
C666-1 Cytotoxicity Assay 20-80 μM 24 h decreases colony formation in a dose-dependent manner  24854838
CNE-1 Cytotoxicity Assay 20-80 μM 24 h decreases colony formation in a dose-dependent manner  24854838
CNE-2 Cytotoxicity Assay 20-80 μM 24 h decreases colony formation in a dose-dependent manner  24854838
C666-1 Cytotoxicity Assay 60 μM 7 d enhances radiation cytotoxicity through COX-2-dependent manner 24854838
CNE-1 Cytotoxicity Assay 60 μM 7 d enhances radiation cytotoxicity through COX-2-dependent manner 24854838
SNU-1041 Growth Inhibition Assay 0-40 μM 48 h inhibits cell viability in a dose dependent manner 24692703
SNU-1041 Function Assay 20/30 μM 4 h induces expression of CHOP, GRP78 and XBP1 at the RNA level  24692703
SNU-1041 Function Assay 0-40 μM 4 h up-regulates CHOP after treatment with high concentrations 24692703
SGC-7901 Growth Inhibition Assay 50-125 μM 24/48/72 h inhibits cell growth in both time and dose dependent manner 24676394
SGC-7901 Apoptosis Assay 100 μM 72 h induces apoptosis 24676394
SGC-7901 Function Assay 75/100/125 μM 24/48/72 h increases caspase-8 and -9 mRNA expression in both time and dose manner 24676394
LMeC  Function Assay 20/50 μM 48 h decreases the expression of COX-2 protein 24656746
CMeC-1 Cell Viability Assay 20/50 μM 48 h inhibits cell viability in a dose dependent manner 24656746
LMeC Cell Viability Assay 20/50 μM 48 h inhibits cell viability in a dose dependent manner 24656746
CMeC-1 Function Assay 20/50 μM 48 h induces G1-S arrest 24656746
LMeC Function Assay 20/50 μM 48 h induces G1-S arrest 24656746
CMeC-1 Function Assay 20/50 μM 48 h decreases the levels of cyclin D1 in a dose-dependent manner 24656746
LMeC Function Assay 20/50 μM 48 h decreases the levels of cyclin D1 in a dose-dependent manner 24656746
CMeC-1 Function Assay 20/50 μM 48 h induces caspase-3 activation 24656746
LMeC Function Assay 20/50 μM 48 h induces caspase-3 activation 24656746
OVCAR-3 Cell Viability Assay 10 µM 1 h enhances paclitaxel-induced ovarian cancer cell death  24520227
OVCAR-3 Apoptosis Assay 10 µM 1 h promotes paclitaxel-induced apoptosis  24520227
OVCAR-3 Function Assay 10 µM 1 h enhances paclitaxel-induced activation of caspase-9  24520227
OVCAR-3 Function Assay 10 µM 1 h down-regulates NF-κB activation induced by paclitaxel 24520227
OVCAR-3 Function Assay 10 µM 1 h inhibits paclitaxel-induced Akt phosphorylation 24520227
CF33 Function Assay 100 μM 24 h induces downregulation of COX-2 protein expression 24503782
CF33 Growth Inhibition Assay 10-100 μM 0-4 d inhibits cell proliferation in a dose-dependent manner 24503782
CF33 Function Assay 10-100 μM 4-24 h decreases cells in the S phase and increases cells in G0/G1 arrest 24503782
LNCaP Growth Inhibition Assay 2/5/10 μM 96 h inhibits cell growth significantly combined with atorvastatin 24296978
LNCaP Apoptosis Assay 2/5/10 μM 96 h induces apoptosis combined with atorvastatin 24296978
PC-3  Growth Inhibition Assay 0-50 μM 48 h inhibits cell growth in a dose dependent manner 24127882
PC-3  Cell Viability Assay 0-100 μM 72 h decreases cell viability in a dose dependent manner 24127882
HCA-7 Function assay 72 hrs Inhibition of IL-1beta-induced PGE2 production in human HCA-7 cells after 72 hrs by EIA, EC50 = 0.00115 μM. 22516282
CHO Function assay In vitro inhibitory potency against human COX-2 in stably transfected chinese hamster ovary (CHO) cells, IC50 = 0.002 μM. 10576684
CHO Function assay Inhibition of PGE-2 production in CHO cells expressing human COX-2, IC50 = 0.002 μM. 10576685
CHO Function assay In vitro potency against human Prostaglandin G/H synthase 2 in transfected CHO cells, IC50 = 0.002 μM. 10197970
CHO Function assay Inhibitory of human Prostaglandin G/H synthase 2 expressed in CHO cells, IC50 = 0.002 μM. 12643942
synovial cells Function assay Inhibitory effect on production of cyclooxygenase-2 (COX-2) prostaglandin E2 (PGE2) in human IL1-beta stimulated synovial cells, IC50 = 0.0079 μM. 10821716
RAW264.7 Function assay Inhibition of COX-2 in mouse RAW264.7 cells assessed as decrease in LPS-induced PGE2 production treated prior to LPS challenge by enzyme immunoassay, IC50 = 0.0087 μM. 24656662
HEK293 Function assay Inhibition of cloned Stylophora pistillata alpha-CA expressed in human HEK293 cells by stopped-flow CO2 assay, Ki = 0.0342 μM. 19520577
SF9 Function assay Inhibitory activity against human Prostaglandin G/H synthase 2 expressed in sf-9 cells infected with baculovirus, IC50 = 0.036 μM. 14698190
SF9 Function assay In vitro inhibitory activity against human recombinant prostaglandin G/H synthase 2 expressed in sf-9 cells infected with baculovirus, IC50 = 0.036 μM. 15026050
CHO Function assay Inhibition of COX2 expressed in CHO cells assessed as inhibition of arachidonic acid-stimulated PGE2 production by enzyme immunoassay, IC50 = 0.036 μM. 15566290
insect cells Function assay 1 min Inhibition of human recombinant COX2 expressed in insect cells using arachidonic acid as substrate incubated for 1 min prior to substrate addition measured for 25 secs by TMPD-based chromogenic assay, IC50 = 0.042 μM. 23010270
HNSCC 1483 Function assay 30 mins Inhibition of COX-2 in human HNSCC 1483 cells using [14C] arachidonic acid as substrate preincubated for 30 mins before substrate addition measured after 30 mins, IC50 = 0.054 μM. 22263894
J774 Function assay Inhibition of COX2 in LPS-stimulated J774 cells assessed as inhibition of PGE2 levels by radioimmunoassay, IC50 = 0.06 μM. 17915854
J774 Function assay 15 mins Inhibition of COX2 in LPS-stimulated mouse J774 cells assessed as inhibition of PGE2 production after 15 mins by radioimmunoassay, IC50 = 0.06 μM. 18752957
J774 Function assay 24 hrs Inhibition of COX-2-mediated PGE2 production in LPS-stimulated mouse J774 cells after 24 hrs by radioimmunoassay, IC50 = 0.061 μM. 21992176
J774 Function assay Inhibition of COX2 in mouse J774 cells assessed as inhibition of LPS-induced PGE2 production by radioimmunoassay, IC50 = 0.061 μM. 23680444
SF9 Function assay Inhibition of human COX2 expressed in baculovirus-infected SF9 cells assessed as inhibition of arachidonic acid-stimulated PGE2 production treated 1 hr before arachidonic acid challenge by enzyme immunoassay, IC50 = 0.063 μM. 19520573
COS Function assay Inhibition of human cyclooxygenase-2 expressed in COS cells, IC50 = 0.068 μM. 15454242
COS Function assay Inhibition of human COX2 expressed in african green monkey COS cells assessed as inhibition of arachidonic acid-stimulated PGE2 production treated 1 hr before arachidonic acid challenge by enzyme immunoassay, IC50 = 0.068 μM. 19520573
143982 Function assay In vitro inhibitory activity against human Prostaglandin G/H synthase 2 (COX-2) in 143982 cells, IC50 = 0.079 μM. 12877584
J774 Function assay In vitro inhibitory activity against Prostaglandin G/H synthase 2 in murine J774 cells, IC50 = 0.079 μM. 15857149
J774 Function assay Inhibition of COX2-dependent PGE2 production in LPS-stimulated mouse J774 cells by RIA, IC50 = 0.079 μM. 19957931
osteosarcoma cells Function assay Inhibition of Prostaglandin G/H synthase 2 in 143.98.2 from human osteosarcoma cells, IC50 = 0.08 μM. 11462976
SF9 Function assay Inhibition of human COX2 expressed in sf9 cells, IC50 = 0.08 μM. 16252917
RAW264.7 Antiinflammatory assay Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced PGE2 production, IC50 = 0.1 μM. 22000948
RAW264.7 Function assay Inhibition of COX-2 in mouse RAW264.7 cells assessed as decrease in LPS-induced PGE2 production, IC50 = 0.12 μM. 23353741
Sf21 Function assay Inhibition of recombinant human N-terminal His-tagged COX2 expressed in baculovirus infected Sf21 cells assessed as reduction in prostaglandin production by enzyme immunoassay, IC50 = 0.15 μM. 29373271
Sf21 Function assay 5 mins Inhibition of recombinant N-terminal His6-tagged human COX-2 expressed in Baculovirus infected Sf21 cells using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 1 hr, IC50 = 0.26 μM. 30293795
MC9 Function assay Inhibition of PGF2apha production in arachidonic acid-stimulated mouse MC9 cells, IC50 = 0.3 μM. 18498150
MC9 Function assay Inhibition of PGF2alpha production in mouse MC9 cells, IC50 = 0.4 μM. 18498150
293E Function assay Inhibition of human microsomal PGES1 expressed in 293E cells by LC/MS/MS analysis, IC50 = 0.425 μM. 26653180
SF9 Function assay 15 mins Inhibition of full length recombinant human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay, IC50 = 0.643 μM. 29500130
HT-29 Cytotoxicity assay 48 hrs Cytotoxicity against COX-2 positive human HT-29 cells transfected with CD44v6shRNA assessed as growth inhibition after 48 hrs by MTT assay, IC50 = 0.7 μM. 24295787
SF9 Function assay 15 mins Inhibition of recombinant Leishmania donovani chagasi beta-carbonic anhydrase expressed in baculovirus infected insect Sf9 cells incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay, Ki = 0.705 μM. 23977960
HCA-7 Cytotoxicity assay 48 hrs Cytotoxicity against COX-2 positive human HCA-7 cells transfected with CD44v6shRNA assessed as growth inhibition after 48 hrs by MTT assay, IC50 = 0.75 μM. 24295787
HepG2 Antiproliferative assay 48 hrs Antiproliferative activity against human HepG2 cells incubated for 48 hrs by MTT assay, IC50 = 0.76 μM. 26346367
SF9 Function assay 15 mins Inhibition of full length recombinant human C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence ass, IC50 = 1.185 μM. 29500130
RAW264.7 Antiinflammatory assay 18 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha secretion after 18 hrs by sandwich ELISA, IC50 = 1.28 μM. 24679441
APC10.1 Cytotoxicity assay 48 hrs Cytotoxicity against COX-2 positive mouse APC10.1 cells transfected with CD44v6shRNA overexpressing HAS-2 assessed as growth inhibition after 48 hrs by MTT assay, IC50 = 1.3 μM. 24295787
RAW264.7 Antiinflammatory assay 30 mins Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production preincubated for 30 mins followed by LPS stimulation measured after 24 hrs by Griess assay, IC50 = 1.6 μM. 26444098
COS Function assay Inhibition of human cyclooxygenase-1 expressed in COS cells, IC50 = 1.689 μM. 15454242
COS Function assay Inhibition of human COX1 expressed in african green monkey COS cells assessed as inhibition of arachidonic acid-stimulated PGE2 treated 1 hr before arachidonic acid challenge by enzyme immunoassay, IC50 = 1.689 μM. 19520573
RAW264.7 Antiinflammatory assay 18 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 18 hrs by griess reaction analysis, IC50 = 1.84 μM. 24679441
HCA-7 Cytotoxicity assay 18 hrs Cytotoxicity against human HCA-7 cells assessed as decrease in cell survival after 18 hrs by MTS assay, IC50 = 2 μM. 23517721
A549 Antiproliferative assay 48 hrs Antiproliferative activity against human A549 cells incubated for 48 hrs by MTT assay, IC50 = 2.15 μM. 26346367
Escherichia coli Arctic cells Function assay 15 mins Inhibition of recombinant Streptococcus mutans UA159 beta-carbonic anhydrase expressed in Escherichia coli Arctic cells preincubated for 15 mins by stopped flow CO2 hydrase assay, Ki = 2.425 μM. 25913199
HT-29 Cytotoxicity assay 18 hrs Cytotoxicity against human HT-29 cells assessed as decrease in cell survival after 18 hrs by MTS assay, IC50 = 3 μM. 23517721
J774 Function assay Inhibition of COX1 in mouse J774 cells assessed as arachidonic acid-induced PGE2 levels by radio immunoassay, IC50 = 3.7 μM. 17915854
J774 Function assay 15 mins Inhibition of COX1 in arachidonic acid-stimulated mouse J774 cells assessed as inhibition of PGE2 production after 15 mins by radioimmunoassay, IC50 = 3.7 μM. 18752957
J774 Function assay 15 mins Inhibition of COX-1-mediated PGE2 production in arachidonic acid-stimulated mouse J774 cells incubated for 15 mins prior to arachidonic acid-challenge by radioimmunoassay, IC50 = 3.84 μM. 21992176
J774 Function assay 15 mins Inhibition of COX1 in mouse J774 cells using arachidonic acid as substrate assessed as inhibition of PGE2 production incubated for 15 mins prior to substrate addition measured after 30 mins by radioimmunoassay, IC50 = 3.84 μM. 23680444
APC10.1 Cytotoxicity assay 18 hrs Cytotoxicity against mouse APC10.1 cells assessed as decrease in cell survival after 18 hrs by MTS assay, IC50 = 4.2 μM. 23517721
B16F10 Antiproliferative assay 24 hrs Antiproliferative activity against mouse B16F10 cells after 24 hrs by MTT assay, IC50 = 4.56 μM. 25866240
HCA-7 Cytotoxicity assay Cytotoxicity against COX-2 positive human HCA-7 cells assessed as growth inhibition by CellTiter-96 AQueous assay, IC50 = 4.9 μM. 24295787
SH-SY5Y Antineurotoxicity assay 72 hrs Antineurotoxicity in human SH-SY5Y cells assessed as inhibition human THP1 cell supernatant-induced cytotoxicity compound pretreated 24 to 48 hrs to THP1 cells measured after 72 hrs of supernatant addition, IC50 = 5 μM. 20138770
THP1 Neuroprotective assay 72 hrs Neuroprotective activity against LPS and IFN-gamma-stimulated neurotoxin production in human THP1 cell assessed as inhibition of THP1 cell secretion-induced toxicity to human SH-SY5Y cells after 72 hrs by MTT assay, IC50 = 5 μM. 20609589
U-937 Function assay Inhibition of Prostaglandin G/H synthase 1 in U-937 cells from human histiocytic lymphoma, IC50 = 5.1 μM. 11462976
U-937 Function assay In vitro inhibitory activity against human Prostaglandin G/H synthase 1 (COX-1) in U-937 cells, IC50 = 5.1 μM. 12877584
J774 Function assay In vitro inhibitory activity against Prostaglandin G/H synthase 1 in murine J774 cells, IC50 = 5.1 μM. 15857149
J774 Function assay Inhibition of COX1-dependent PGE2 production in LPS-stimulated mouse J774 cells by RIA, IC50 = 5.1 μM. 19957931
HT-29 Cytotoxicity assay Cytotoxicity against COX-2 positive human HT-29 cells assessed as growth inhibition by CellTiter-96 AQueous assay, IC50 = 5.7 μM. 24295787
MCF7 Antiproliferative assay 24 hrs Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay, IC50 = 5.94 μM. 25866240
APC10.1 Function assay 18 hrs Inhibition of hyaluronan-induced CD44 antigen variant exon 6 activity in mouse APC10.1 cells expressing Has2 assessed as decrease in cell survival after 18 hrs by MTS assay, IC50 = 6 μM. 23517721
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells incubated for 48 hrs by MTT assay, IC50 = 6.88 μM. 26346367
SW480 Cytotoxicity assay Cytotoxicity against COX-2 negative human SW480 cells assessed as growth inhibition by CellTiter-96 AQueous assay, IC50 = 6.9 μM. 24295787
HeLa Antiproliferative assay 24 hrs Antiproliferative activity against human HeLa cells after 24 hrs by MTT assay, IC50 = 7.35 μM. 25866240
HeLa Antiproliferative assay 48 hrs Antiproliferative activity against human HeLa cells incubated for 48 hrs by MTT assay, IC50 = 7.55 μM. 26346367
HeLa Antiproliferative assay 24 hrs Antiproliferative activity against human HeLa cells after 24 hrs by MTT assay, IC50 = 7.79 μM. 27349331
HepG2 Antiproliferative assay 24 hrs Antiproliferative activity against human HepG2 cells after 24 hrs by MTT assay, IC50 = 10.03 μM. 27349331
APC10.1 Cytotoxicity assay Cytotoxicity against COX-2 positive mouse APC10.1 cells overexpressing HAS-2 assessed as growth inhibition by CellTiter-96 AQueous assay, IC50 = 13.4 μM. 24295787
CHO Function assay Inhibition of COX1 expressed in CHO cells assessed as inhibition of arachidonic acid-stimulated PGE2 production by enzyme immunoassay, IC50 = 13.5 μM. 15566290
B16F10 Antiproliferative assay 24 hrs Antiproliferative activity against mouse B16F10 cells after 24 hrs by MTT assay, IC50 = 14.36 μM. 27349331
A549 Antitumor assay 48 hrs Antitumor activity against human A549 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay, IC50 = 15.6 μM. 23353741
A549 Antiproliferative assay 24 hrs Antiproliferative activity against human A549 cells after 24 hrs by MTT assay, IC50 = 15.64 μM. 27349331
HeLa Antiproliferative assay 48 hrs Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay, IC50 = 15.69 μM. 30031652
A549 Antiproliferative assay 48 hrs Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50 = 16.08 μM. 30031652
NCI60 Growth inhibition assay 48 hrs Growth inhibition of human NCI60 cells after 48 hrs by sulforhodamine B assay, GI50 = 17.5 μM. 20387815
HCA-7 Function assay 18 hrs Inhibition of hyaluronan-induced CD44 antigen variant exon 6 activity in human HCA-7 cells expressing Has2 assessed as decrease in cell survival after 18 hrs by MTS assay, IC50 = 17.5 μM. 23517721
HT-29 Function assay 18 hrs Inhibition of hyaluronan-induced CD44 antigen variant exon 6 activity in human HT-29 cells expressing Has2 assessed as decrease in cell survival after 18 hrs by MTS assay, IC50 = 18.3 μM. 23517721
platelet Function assay Inhibitory effect on production of cyclooxygenase-1 (COX-1) thromboxane B2 (TXB2) in human platelet cells, IC50 = 19 μM. 10821716
B16F10 Antiproliferative assay 48 hrs Antiproliferative activity against mouse B16F10 cells after 48 hrs by MTT assay, IC50 = 19.15 μM. 30031652
MDA231 Antiproliferative assay Antiproliferative activity against human MDA231 cells by MTT assay, IC50 = 22.79 μM. 30216848
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 26.78 μM. 30031652
HCT116 Antiproliferative assay Antiproliferative activity against human HCT116 cells by MTT assay, IC50 = 29.54 μM. 30216848
MCF7 Antiproliferative assay Antiproliferative activity against human MCF7 cells by MTT assay, IC50 = 31.28 μM. 30216848
LNCAP Cytotoxicity assay 72 hrs Cytotoxicity against human LNCAP cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 32.6 μM. 28057407
BL21(DE3) Function assay 15 mins Inhibition of GST-tagged Malassezia globosa ATCC 96807/CBS 7966 MG-CA expressed in Escherichia coli BL21(DE3) cells preincubated for 15 mins measured for 10 to 100 sec by stopped-flow method, Ki = 34.8 μM. 22424239
HeLa Antiproliferative assay Antiproliferative activity against human HeLa cells by MTT assay, IC50 = 36.08 μM. 30216848
MDA-MB-231 Cytotoxicity assay 48 hrs Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTS assay, IC50 = 40 μM. 22780961
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT colorimetric assay, IC50 = 40.8 μM. 22000948
MCF7 Antitumor assay 48 hrs Antitumor activity against human MCF7 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay, IC50 = 40.8 μM. 23353741
Caco2 Antiproliferative assay Antiproliferative activity against human Caco2 cells by MTT assay, IC50 = 42.74 μM. 30216848
HCT116 Anticancer assay 72 hrs Anticancer activity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 43.3 μM. 21678971
L1210 Cytotoxicity assay 72 hrs Cytotoxicity against mouse L1210 cells after 72 hrs by MTT assay, IC50 = 44 μM. 20451397
HT-29 Cytotoxicity assay Cytotoxicity against human HT-29 cells by MTT assay, IC50 = 45.5 μM. 20804197
PC3 Anticancer assay Anticancer activity against human PC3 cells, GI50 = 47 μM. 18262309
PC3 Antiproliferative assay 72 hrs Antiproliferative activity against androgen-independent human PC3 cells after 72 hrs by MTT test, IC50 = 47 μM. 15566290
PC3 Antiproliferative assay 72 hrs Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay, IC50 = 48 μM. 17937972
PC3 Function assay 2 hrs Inhibition of PDK1-mediated Akt activation in human PC3 cells after 2 hrs by Western blotting analysis, IC50 = 48 μM. 23735281
PC3 Cytotoxicity assay 72 hrs Cytotoxicity against human PC3 cells after 72 hrs by MTT assay, IC50 = 48.5 μM. 20451397
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 49.66 μM. 29191502
A549 Function assay Inhibition of COX2-dependent PGE2 production in IL1B stimulated human A549 cells in presence of arachidonic acid 18498150
A549 Function assay Inhibition of COX2-dependent PGE2 production in IL1B stimulated human A549 cells 18498150
A549 Function assay 5 uM Inhibition of mPGES1 in human A549 cells assessed as inhibition of IL-1-beta-induced PGE2 formation at 5 uM by cell-intact assay 19053751
A549 Function assay 5 uM 10 mins Inhibition of mPGES1 in IL1-beta induced human A549 cells assessed as PGE2 production at 5 uM preincubated for 10 mins 19884011
PANC1 Function assay 25 to 50 M 30 mins Inhibition of IL-6-induced STAT3 phosphorylation in human PANC1 cells at 25 to 50 M pretreated 2 hrs prior to IL-6 challenge measured after 30 mins 21678971
HT29 Function assay 10 uM Inhibition of hyaluronan-induced CD44 antigen variant exon 6 activity in human HT29 cells assessed as decrease in 5-LOX expression at 10 uM 23517721
HT29 Function assay 10 uM Inhibition of hyaluronan-induced CD44 antigen variant exon 6 activity in human HT29 cells assessed as decrease in COX-2 expression at 10 uM 23517721
HCA-7 Function assay 5 uM 24 hrs Inhibition of hyaluronan-induced CD44v6 in human HCA-7 cells transfected with Has2cDNA assessed as downregulation of 5-LOX protein expression at 5 uM after 24 hrs by Western blotting analysis 24295787
HCA-7 Function assay 5 uM 24 hrs Inhibition of hyaluronan-induced CD44v6 in human HCA-7 cells transfected with Has2cDNA assessed as downregulation of COX-2 protein expression at 5 uM after 24 hrs by Western blotting analysis 24295787
HCA-7 Function assay 5 uM 24 hrs Inhibition of hyaluronan-induced CD44v6 in human HCA-7 cells transfected with Has2cDNA assessed as downregulation of COX-1 protein expression at 5 uM after 24 hrs by Western blotting analysis 24295787
HeLa Function assay 100 uM 24 hrs Inhibition of mPGES-1 in human HeLa cells using PGH2 as substrate assessed as inhibition of IL-1beta/TNFalpha-stimulated PGE2 production at 100 uM after 24 hrs by LC-MS/MS analysis 24183739
HeLa Function assay 0.1 uM 24 hrs Inhibition of PGE2 secretion in human HeLa cells at 0.1 uM after 24 hrs by EIA monoclonal assay 27349331
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
RAW264.7 Antiinflammatory assay 20 uM 2 hrs Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS induced cox-2 expression at 20 uM preincubated for 2 hrs followed by LPS challenge measured after 24 hrs by Western blot method 29100799
RAW264.7 Antiinflammatory assay 20 uM 2 hrs Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS induced iNOS expression at 20 uM preincubated for 2 hrs followed by LPS challenge measured after 24 hrs by Western blot method 29100799
Click to View More Cell Line Experimental Data

Biological Activity

Description Celecoxib is a selective COX-2 inhibitor with IC50 of 40 nM in Sf9 cells.
Targets
COX-2 [1]
(Sf9 cells)
40 nM
In vitro
In vitro

Celecoxib shows low sensitivity against COX-1 with IC50 of 15 μM. [1] Celecoxib shows an anti-proliferative effect on nasopharyngeal carcinoma (NPC) cell lines including HNE1 and CNE1-LMP1 with IC50 of 32.86 μM and 61.31 μM, respectively. [2]
Kinase Assay COX enzyme assay in vitro
Expression of COX protein in insect cells is determined by assessing PG-synthetic capability in homogenates from cells incubated for 3 days with COX-1 or COX-2 baculovirus. Cells expressing COX-1 or COX-2 are homogenized and incubated with arachidonic acid (10 μM). COX activity is determined by monitoring PG production. No COX activity is detected in mock-infected Sf9 cells. Celecoxib are preincubated with crude 1% CHAPS homogenates (2-10 μg of protein) for 10 minutes before addition of arachidonic acid. PGE2 formed is detected by ELISA after 10 minute incubation.
Cell Research Cell lines HNE1 and CNE1-LMP1
Concentrations 0-75 μM
Incubation Time 48 hours
Method

The antiproliferative effect of Celecoxib on NPC cells is assessed using an MTT assay. Cells are seeded into 96-well plates and allowed to attach for 24 hours. The cells are then treated with increasing concentrations of Celecoxib (0 to 75 μM) dissolved in DMSO (final concentration ≤0.1%) and incubated for up to 48 hours. After the incubation, 20 μL of MTT dye (5 mg/mL) are added to each well and cells are incubated at 37 °C for 4 hours. After removing the supernatants, the crystals are dissolved in DMSO and the absorbance is measured at 490 nm. The half-maximal inhibitory concentration (IC50) values and the 95% confidence intervals are calculated using probit regression using SPSS 15.0 software. The experiment is performed in triplicate and repeated at least three times.
Experimental Result Images Methods Biomarkers Images PMID
Western blot Fibronectin / Vimentin / N-cadherin / E-cadherin COX-2 pAKT / AKT / PPARγ / PTEN 28978083
Immunofluorescence PPARγ / PTEN 24721996
Growth inhibition assay Cell viability 28521485
In Vivo
In vivo

Celecoxib exhibits a potent, oral anti-inflammatory activity. Celecoxib reduces acute inflammation in the carrageenan edema assay and chronic inflammation in the adjuvant arthritis model with ED50 of 7.1 mg/kg and 0.37 mg/kg/day, respectively. In addition, Celecoxib also exhibits analgesic activity in the Hargreaves hyperalgesia model with ED50 of 34.5 mg/kg. Besides, Celecoxib produces no acute GI toxicity in rats at doses up to 200 mg/kg and no chronic GI toxicity in rats at doses up to 600 mg/kg/day over 10 days. [1] In a C3Hf/KamLaw female mouse model, Celecoxib increases median survival time of 105 days (range, 79-145 days) after 13.5 Gy local thoracic irradiation (LTI) alone to 142 days (range, 94-155 days). [3]
Animal Research Animal Models A 0.1 mL aliquot of a 1% solution of carrageenan in 0.9% sterile saline or 1 mg of Mycobacterium butyricum in 50 μL of mineral oil is administered to the right hind foot pad of male Sprague−Dawley rats.
Dosages ≤200 mg/kg
Administration Administered via p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01344200 Recruiting
Pharmacokinetics of Celecoxib in Children
Children''s Hospital of Eastern Ontario
 January 29 2024 Phase 2
NCT05648916 Enrolling by invitation
Heterotopic Ossification
McGill University Health Centre/Research Institute of the McGill University Health Centre
 August 2 2022 --
NCT05256823 Active not recruiting
To Evaluate the Safety and Efficacy of Celecoxib Plus Nucleos(t)Ide Analogues in Nucleos(t)Ide-treated Patients With Chronic Hepatitis B
Lai Wei|Beijing Tsinghua Chang Gung Hospital
 February 24 2022 Phase 2
NCT05324163 Completed
KNEE OSTEOARTHRITIS
Jiangsu XinChen-Techfields Pharma Co. LTD.
 September 29 2021 Phase 3
NCT04526197 Completed
Wilson Disease
Alexion Pharmaceuticals Inc.
 July 7 2020 Phase 1

Chemical Information & Solubility

Molecular Weight 381.37 Formula

C17H14F3N3O2S
CAS No. 169590-42-5 SDF Download Celecoxib SDF
Smiles CC1=CC=C(C=C1)C2=CC(=NN2C3=CC=C(C=C3)S(=O)(=O)N)C(F)(F)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 76 mg/mL ( (199.28 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 33 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
I am doing an animal experiment with mice and planning to administrate S1261 via oral gavage. what are your recommendations for diluting the compound?

Answer:
For oral administration, Celecoxib can be dissolved in vehicle one: "0.5% methyl cellulose and 0.025% Tween-20", or the vehicle 2 "2% DMSO/30% PEG 300/5% Tween 80/ ddH2O".

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