Cat. No.: HY-N1201

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Apigenin

(Synonyms: 4',5,7-Trihydroxyflavone; Apigenol; C.I. Natural Yellow 1)

47 Cited Publications

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Based on 47 publication(s) in Google Scholar

Apigenin (4',5,7-Trihydroxyflavone) is a competitive CYP2C9 inhibitor with a K_i of 2 μM.

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

Purity: 99.22%
CAS No.: 520-36-5
Formula: C₁₅H₁₀O₅
Molecular Weight:270.24

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Apigenin Chemical Structure

CAS No.: 520-36-5

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Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (47)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

Apigenin (4',5,7-Trihydroxyflavone) is a competitive CYP2C9 inhibitor with a K_i of 2 μM.

IC₅₀ & Target

CYP2

All Cytochrome P450 Isoforms :

All Endogenous Metabolite Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	3 x 10^-1 μg/mL Compound: 38	Inhibition of EGFR in human A431 cells Inhibition of EGFR in human A431 cells	[PMID: 1479375]
A549	EC₅₀	101 μM Compound: 6	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 12027739]
B16-BL6	EC₅₀	31.6 μM Compound: 6	Antiproliferative activity against mouse B16-BL6 cells after 72 hrs by MTT assay Antiproliferative activity against mouse B16-BL6 cells after 72 hrs by MTT assay	[PMID: 12027739]
BALB/3T3	IC₅₀	141.4 μM Compound: 4	Growth inhibition of BALB/c mouse cloned 3T3/A31 cells after 72 hrs by nigrosin assay Growth inhibition of BALB/c mouse cloned 3T3/A31 cells after 72 hrs by nigrosin assay	[PMID: 10096863]
C2C12	IC₅₀	26.58 μg/mL Compound: 4	Cytotoxicity against mouse C2C12 cells assessed as reduction in cell viability by MTT assay Cytotoxicity against mouse C2C12 cells assessed as reduction in cell viability by MTT assay	[PMID: 33412152]
C8166	CC₅₀	17.2 μg/mL Compound: 4	Cytotoxicity against human C8166 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay Cytotoxicity against human C8166 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay	[PMID: 24794743]
C8166	EC₅₀	4.46 μg/mL Compound: 4	Antiviral activity against HIV-1 3B infected in human C8166 cells assessed as inhibition of virus-induced cytopathogenicity by measuring syncytial cell number after 3 days by inverted microscopic analysis Antiviral activity against HIV-1 3B infected in human C8166 cells assessed as inhibition of virus-induced cytopathogenicity by measuring syncytial cell number after 3 days by inverted microscopic analysis	[PMID: 24794743]
Col2	ED₅₀	19.3 μg/mL Compound: apigenin	Cytotoxicity against human Col2 cells Cytotoxicity against human Col2 cells	[PMID: 7931367]
DLD-1	IC₅₀	89.5 μM Compound: 34	Antiproliferative activity against human DLD-1 cells assessed as cell growth inhibition Antiproliferative activity against human DLD-1 cells assessed as cell growth inhibition	[PMID: 34355179]
H9	EC₅₀	9 μM Compound: 12	Antiviral activity against HIV1 3B infected in human H9 cells assessed as inhibition of viral replication after 3 days by p24 antigen capture assay Antiviral activity against HIV1 3B infected in human H9 cells assessed as inhibition of viral replication after 3 days by p24 antigen capture assay	[PMID: 8158164]
H9	IC₅₀	35 μM Compound: 12	Cytotoxicity against human H9 cells after 3 days Cytotoxicity against human H9 cells after 3 days	[PMID: 8158164]
H9	EC₅₀	9 μg/mL Compound: 1	Inhibitory activity against HIV-1 IIIB replication in H9 cell line Inhibitory activity against HIV-1 IIIB replication in H9 cell line	10.1016/0960-894X(94)80015-4
H9	IC₅₀	35 μg/mL Compound: 1	Inhibitory activity against H9 cells uninfected with HIV-1 Inhibitory activity against H9 cells uninfected with HIV-1	10.1016/0960-894X(94)80015-4
HCT-116	EC₅₀	23.8 μM Compound: Apigenin	Cytotoxicity against human HCT116 cells assessed as cell viability after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 26529431]
HCT-116	IC₅₀	27.9 μM Compound: 34	Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition	[PMID: 34355179]
HEK293	IC₅₀	>20 μM Compound: 18	Inhibition of human recombinant 17beta-HSD2 expressed in HEK293 cell lysate assessed as conversion of radiolabeled estrone to estradiol Inhibition of human recombinant 17beta-HSD2 expressed in HEK293 cell lysate assessed as conversion of radiolabeled estrone to estradiol	[PMID: 18533708]
HEK293	IC₅₀	0.71 μM Compound: 18	Inhibition of human recombinant 17beta-HSD1 expressed in HEK293 cell lysate assessed as conversion of radiolabeled estrone to estradiol Inhibition of human recombinant 17beta-HSD1 expressed in HEK293 cell lysate assessed as conversion of radiolabeled estrone to estradiol	[PMID: 18533708]
HEK293	IC₅₀	1.13 μM Compound: 7g	Inhibition of NOX4 expressed in HEK293 FS cells assessed as H2O2 production by H2O2/Tyr/LPO assay Inhibition of NOX4 expressed in HEK293 FS cells assessed as H2O2 production by H2O2/Tyr/LPO assay	[PMID: 20731357]
HEK293	EC₅₀	24.9 μM Compound: 15	Agonist activity at mouse PPARgamma expressed in HEK293 cells co-expressing with Gal4 reporter vector after 24 hrs by dual-luciferase reporter assay Agonist activity at mouse PPARgamma expressed in HEK293 cells co-expressing with Gal4 reporter vector after 24 hrs by dual-luciferase reporter assay	[PMID: 24955889]
HEK293	IC₅₀	>10 μM Compound: 24	Inhibition of human TRPC5 expressed in HEK293 cells assessed as reduction in gadolinium-induced calcium entry after 30 mins by fluo-4 dye based fluorescence assay Inhibition of human TRPC5 expressed in HEK293 cells assessed as reduction in gadolinium-induced calcium entry after 30 mins by fluo-4 dye based fluorescence assay	[PMID: 30943030]
HeLa	EC₅₀	92.7 μM Compound: 6	Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay	[PMID: 12027739]
HeLa	IC₅₀	≥10 μM Compound: apigenin	Cytotoxicity against human HeLa cells by MTT assay Cytotoxicity against human HeLa cells by MTT assay	[PMID: 19278239]
HeLa	IC₅₀	21.3 μM Compound: 8	Antiproliferative activity against human HeLa cells after 48 hrs by CCK8 assay Antiproliferative activity against human HeLa cells after 48 hrs by CCK8 assay	[PMID: 29475587]
HeLa	IC₅₀	6.092 μM Compound: Apigenin	Cytotoxicity against human HeLa cells Cytotoxicity against human HeLa cells	[PMID: 31784199]
HeLa S3	IC₅₀	>10 μM Compound: 9	Cytotoxicity against human HeLa S3 cells assessed as cell viability incubated for 48 hrs by microscopic analysis Cytotoxicity against human HeLa S3 cells assessed as cell viability incubated for 48 hrs by microscopic analysis	[PMID: 35704432]
HepG2	IC₅₀	70.18 μM Compound: Apigenin	Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay	[PMID: 26896708]
HL-60	IC₅₀	22.3 μM Compound: 8	Antiproliferative activity against human HL60 cells after 48 hrs by CCK8 assay Antiproliferative activity against human HL60 cells after 48 hrs by CCK8 assay	[PMID: 29475587]
HT-1080	EC₅₀	36.6 μM Compound: 6	Antiproliferative activity against human HT1080 cells after 72 hrs by MTT assay Antiproliferative activity against human HT1080 cells after 72 hrs by MTT assay	[PMID: 12027739]
HT-1080	ED₅₀	12.2 μg/mL Compound: apigenin	Cytotoxicity against human HT1080 cells Cytotoxicity against human HT1080 cells	[PMID: 7931367]
HT-22	EC₅₀	>100 μM Compound: 10	Neuroprotective activity against glutamate-induced cell death in mouse HT-22 cells assessed as increase in cell viability after 24 hrs by EZ-Cytox assay Neuroprotective activity against glutamate-induced cell death in mouse HT-22 cells assessed as increase in cell viability after 24 hrs by EZ-Cytox assay	[PMID: 32991171]
HT-29	IC₅₀	2 μM Compound: 34	Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition	[PMID: 34355179]
Huh-7	CC₅₀	>50 μM Compound: 21	Cytotoxicity against human Huh7.5.1 cells by MTT assay Cytotoxicity against human Huh7.5.1 cells by MTT assay	[PMID: 22445328]
Huh-7	EC₅₀	12 μM Compound: 21	Antiviral activity against HCV genotype 2a J399LM in Human Huh7.5.1 replicon cells assessed as suppression of viral replication after 72 hrs by luciferase reporter gene assay Antiviral activity against HCV genotype 2a J399LM in Human Huh7.5.1 replicon cells assessed as suppression of viral replication after 72 hrs by luciferase reporter gene assay	[PMID: 22445328]
Huh-7	EC₅₀	7.9 μM Compound: 21	Antiviral activity against HCV JFH-1 J399EM infected in Human Huh7.5.1 cells assessed as suppression of viral replication after 72 hrs by EGFP assay Antiviral activity against HCV JFH-1 J399EM infected in Human Huh7.5.1 cells assessed as suppression of viral replication after 72 hrs by EGFP assay	[PMID: 22445328]
Jurkat	IC₅₀	30 μg/mL Compound: Apigenin	Growth inhibition of human Jurkat cells Growth inhibition of human Jurkat cells	[PMID: 19026536]
Jurkat	IC₅₀	6.7 μg/mL Compound: Apigenin	Cytotoxicity against human Jurkat cells in presence and relative to TRAIL Cytotoxicity against human Jurkat cells in presence and relative to TRAIL	[PMID: 19026536]
Jurkat	IC₅₀	1 μM Compound: Apigenin	Inhibition of chymotrypsin-like activity of human 26S proteasome in human Jurkat cells assessed as decrease in AMC hydrolysis using Z-Gly-Gly-Leu-AMC as substrate after 24 hrs by fluorescence based method Inhibition of chymotrypsin-like activity of human 26S proteasome in human Jurkat cells assessed as decrease in AMC hydrolysis using Z-Gly-Gly-Leu-AMC as substrate after 24 hrs by fluorescence based method	[PMID: 30776692]
Jurkat	IC₅₀	1.8 μM Compound: Apigenin	Inhibition of chymotrypsin-like activity of purified human 20S proteasome expressed in human Jurkat cells assessed as decrease in AMC hydrolysis using Suc-Leu-Leu-Val-Tyr-AMC as substrate incubated for 2 hrs by fluorescence based method Inhibition of chymotrypsin-like activity of purified human 20S proteasome expressed in human Jurkat cells assessed as decrease in AMC hydrolysis using Suc-Leu-Leu-Val-Tyr-AMC as substrate incubated for 2 hrs by fluorescence based method	[PMID: 30776692]
KB	ED₅₀	7.4 μg/mL Compound: NSC-83244	Cytotoxicity against human KB cells Cytotoxicity against human KB cells	[PMID: 469554]
KB	ED₅₀	>20 μg/mL Compound: apigenin	Cytotoxicity against human KB cells Cytotoxicity against human KB cells	[PMID: 7931367]
KB-V1	ED₅₀	16.8 μg/mL Compound: apigenin	Cytotoxicity against human KBV1 cells Cytotoxicity against human KBV1 cells	[PMID: 7931367]
L02	IC₅₀	>100 μM Compound: Apigenin	Cytotoxicity against human LO2 cells after 48 hrs by MTT assay Cytotoxicity against human LO2 cells after 48 hrs by MTT assay	[PMID: 26896708]
L6	IC₅₀	18.1 μg/mL Compound: 16	Cytotoxicity against rat L6 cells after 72 hrs by alamar blue staining based fluorescence analysis Cytotoxicity against rat L6 cells after 72 hrs by alamar blue staining based fluorescence analysis	10.1039/C5MD00481K
L6	IC₅₀	21.8 μg/mL Compound: 16	Antitrypanosomal activity against trypomastigote forms of Trypanosoma cruzi Tulahuen C2C4 infected in rat L6 cells after 96 hrs by photometric method Antitrypanosomal activity against trypomastigote forms of Trypanosoma cruzi Tulahuen C2C4 infected in rat L6 cells after 96 hrs by photometric method	10.1039/C5MD00481K
Lu1	ED₅₀	14 μg/mL Compound: apigenin	Cytotoxicity against human Lu1 cells Cytotoxicity against human Lu1 cells	[PMID: 7931367]
MCF7	IC₅₀	5.9 μM Compound: 9	Inhibition of BCRP expressed in MCF-7 MX cells using Hoechst 33342 staining Inhibition of BCRP expressed in MCF-7 MX cells using Hoechst 33342 staining	[PMID: 21354800]
MCF7	IC₅₀	1 μM Compound: Apigenin	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 6 days by SRB assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 6 days by SRB assay	[PMID: 33257172]
MCF7	IC₅₀	>100 μM Compound: apigenin	Anti-proliferative activity against estrogen-responsive human breast cancer cell line MCF-7 in the presence of ER at a 10e-4 uM concentration of estradiol Anti-proliferative activity against estrogen-responsive human breast cancer cell line MCF-7 in the presence of ER at a 10e-4 uM concentration of estradiol	[PMID: 8784443]
MCF7	IC₅₀	95 μM Compound: apigenin	Inhibition of 10e-4 uM estradiol induced estrogen receptor positive MCF-7 human breast cancer cell proliferation Inhibition of 10e-4 uM estradiol induced estrogen receptor positive MCF-7 human breast cancer cell proliferation	[PMID: 8784443]
MDCK	CC₅₀	39.59 μM Compound: 1	Cytotoxicity against MDCK cells by MTT assay Cytotoxicity against MDCK cells by MTT assay	[PMID: 18640042]
MDCK	CC₅₀	>300 μM Compound: 1	Cytotoxicity against MDCK cells after 48 hrs by MTT assay Cytotoxicity against MDCK cells after 48 hrs by MTT assay	[PMID: 19729316]
MDCK	EC₅₀	42.7 μM Compound: 1	Antiviral activity against influenza A virus H9N2 A/Chicken/Korea/MS96/96 infected in MDCK cells assessed as reduction in virus-induced cytopathic effect Antiviral activity against influenza A virus H9N2 A/Chicken/Korea/MS96/96 infected in MDCK cells assessed as reduction in virus-induced cytopathic effect	[PMID: 19729316]
MDCK	EC₅₀	60.4 μM Compound: 1	Antiviral activity against influenza A virus H1N1 A/PR/8/34 infected in MDCK cells assessed as reduction in virus-induced cytopathic effect Antiviral activity against influenza A virus H1N1 A/PR/8/34 infected in MDCK cells assessed as reduction in virus-induced cytopathic effect	[PMID: 19729316]
MDCK	IC₅₀	3.1 μM Compound: 9	Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining	[PMID: 21354800]
Monocyte	IC₅₀	20 μM Compound: Apigenin	Inhibition of TNFalpha expression in LPS-stimulated human monocytes treated 30 mins before LPS challenge measured after 14 hrs by ELISA Inhibition of TNFalpha expression in LPS-stimulated human monocytes treated 30 mins before LPS challenge measured after 14 hrs by ELISA	[PMID: 10096854]
Monocyte	IC₅₀	1.2 μM Compound: apigenin	Inhibition of procoagulant activity in monocyte from human blood assessed as counteraction of IL1-induced tissue factor expression after 18 hrs Inhibition of procoagulant activity in monocyte from human blood assessed as counteraction of IL1-induced tissue factor expression after 18 hrs	[PMID: 8882428]
Monocyte	IC₅₀	1.2 x 10^-6 M Compound: apigenin	Inhibition of procoagulant activity in monocyte from human blood assessed as counteraction of IL1-induced tissue factor expression after 18 hrs Inhibition of procoagulant activity in monocyte from human blood assessed as counteraction of IL1-induced tissue factor expression after 18 hrs	[PMID: 8882428]
MV4-11	GI₅₀	2.81 μM Compound: 2	Cytotoxicity against human MV4-11 cells harboring FLT3 mutation after 72 hrs by tetrazolium based Ez CyTox cell viability assay Cytotoxicity against human MV4-11 cells harboring FLT3 mutation after 72 hrs by tetrazolium based Ez CyTox cell viability assay	[PMID: 23411073]
N9	IC₅₀	>30 μM Compound: 1	Inhibitory effect of compound on the accumulation of NO2 in the culture media of N9 cells in response to LPS/IFN-gamma Inhibitory effect of compound on the accumulation of NO2 in the culture media of N9 cells in response to LPS/IFN-gamma	[PMID: 15013012]
NCI/ADR-RES	IC₅₀	200 nM Compound: 63	Cytotoxicity against human MCF7ADR cells Cytotoxicity against human MCF7ADR cells	[PMID: 37847948]
Neutrophil	IC₅₀	12.3 μM Compound: 4c	Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of HOCl-induced oxidation of APF after 6 mins by fluorescence assay Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of HOCl-induced oxidation of APF after 6 mins by fluorescence assay	[PMID: 23871908]
Neutrophil	IC₅₀	16.2 μM Compound: 4c	Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of H2O2-induced oxidation of amplex red incubated for 5 mins prior to PMA challenge by fluorescence assay Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of H2O2-induced oxidation of amplex red incubated for 5 mins prior to PMA challenge by fluorescence assay	[PMID: 23871908]
Neutrophil	IC₅₀	24 μM Compound: 4c	Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of ROS-induced luminol oxidation incubated for 5 mins prior to PMA challenge by chemiluminescence assay Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of ROS-induced luminol oxidation incubated for 5 mins prior to PMA challenge by chemiluminescence assay	[PMID: 23871908]
Neutrophil	IC₅₀	7.7 μM Compound: 4c	Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of superoxide anion radical-induced lucigenin oxidation incubated for 5 mins prior to PMA challenge by chemiluminescence assay Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of superoxide anion radical-induced lucigenin oxidation incubated for 5 mins prior to PMA challenge by chemiluminescence assay	[PMID: 23871908]
P388	ED₅₀	12.2 μg/mL Compound: apigenin	Cytotoxicity against mouse P388 cells Cytotoxicity against mouse P388 cells	[PMID: 7931367]
Peritoneal macrophage	IC₅₀	7.7 μM Compound: 2;kp16	Inhibition of LPS-stimulated nitric oxide production in ddy mouse peritoneal macrophages measured after 20 hrs by Greiss method Inhibition of LPS-stimulated nitric oxide production in ddy mouse peritoneal macrophages measured after 20 hrs by Greiss method	[PMID: 27955927]
RAW	IC₅₀	10.7 μM Compound: 1	Inhibitory effect of compound on the accumulation of NO2 in the culture media of RAW 264.7 cells in response to LPS Inhibitory effect of compound on the accumulation of NO2 in the culture media of RAW 264.7 cells in response to LPS	[PMID: 15013012]
RAW264.7	IC₅₀	0.5 μM Compound: apigenin	Inhibition of COX2 protein expression in mouse RAW264.7 cells Inhibition of COX2 protein expression in mouse RAW264.7 cells	[PMID: 16038536]
RAW264.7	IC₅₀	6.7 μM Compound: 8	Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced nitrite accumulation after 24 hrs by Griess reagent method Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced nitrite accumulation after 24 hrs by Griess reagent method	[PMID: 19778086]
RAW264.7	IC₅₀	7.7 μM Compound: Apigenin	Antiinflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of nitric oxide production after 24 hrs by Griess reagent Antiinflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of nitric oxide production after 24 hrs by Griess reagent	[PMID: 20363145]
RAW264.7	IC₅₀	14 μM Compound: 2;kp16	Inhibition of LPS/INF-gamma-stimulated nitric oxide production in mouse RAW264.7 cells measured after 16 hrs Inhibition of LPS/INF-gamma-stimulated nitric oxide production in mouse RAW264.7 cells measured after 16 hrs	[PMID: 27955927]
RAW264.7	IC₅₀	13.4 μM Compound: 12	Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as decrease in PGE2 production preincubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as decrease in PGE2 production preincubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA	[PMID: 31747281]
RAW264.7	CC₅₀	65.1 μM Compound: 18	Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay	[PMID: 33667099]
RAW264.7	IC₅₀	18.4 μM Compound: 18	Inhibition of LPS induced NO production in mouse RAW264.7 cells measured after 24 hrs by Griess reagent based assay Inhibition of LPS induced NO production in mouse RAW264.7 cells measured after 24 hrs by Griess reagent based assay	[PMID: 33667099]
RAW264.7	IC₅₀	12.16 μM Compound: 25; 37	Anti-inflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production Anti-inflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production	[PMID: 37683361]
RBL-2H3	IC₅₀	124 μM Compound: 5	Antihistaminic activity in rat RBL2H3 cells assessed as inhibition of DNP-BSA-induced beta-hexosaminidase release preincubated for 10 mins before DNP-BSA challenge Antihistaminic activity in rat RBL2H3 cells assessed as inhibition of DNP-BSA-induced beta-hexosaminidase release preincubated for 10 mins before DNP-BSA challenge	[PMID: 14510616]
RS4-11	GI₅₀	27.9 μM Compound: 2	Cytotoxicity against human RS4:11 cells harboring wild type FLT3 after 72 hrs by tetrazolium based Ez CyTox cell viability assay Cytotoxicity against human RS4:11 cells harboring wild type FLT3 after 72 hrs by tetrazolium based Ez CyTox cell viability assay	[PMID: 23411073]
SK-MEL-2	ED₅₀	13.6 μg/mL Compound: apigenin	Cytotoxicity against human SK-MEL-2 cells Cytotoxicity against human SK-MEL-2 cells	[PMID: 7931367]
THP-1	IC₅₀	60 μM Compound: Apigenin	Cytotoxicity against human THP1 cells after 24 hrs by MTS assay Cytotoxicity against human THP1 cells after 24 hrs by MTS assay	[PMID: 19879672]
THP-1	IC₅₀	60 μM/L Compound: Apigenin	Cytotoxicity against human THP1 cells after 24 hrs by MTS assay Cytotoxicity against human THP1 cells after 24 hrs by MTS assay	[PMID: 19879672]
Vero	CC₅₀	54 μg/mL Compound: apigenin	Cytotoxicity against african green monkey Vero cells Cytotoxicity against african green monkey Vero cells	[PMID: 1338212]

In Vitro

Apigenin (4',5,7-Trihydroxyflavone) inhibits cytochrome P450 2C9 (CYP2C9) with a K_i of 2 μM in the CYP2C9 RECO system (a purified, reconstituted enzyme system containing recombinant human CYP2C9, P450 reductase, cytochrome b₅, and liposomes)^[1]. Apigenin inhibits cell proliferation. The growth inhibition rate (IR) of 20, 40, and 80 μM of Apigenin is 38%, 71%, and 99% respectively on the 7^thd. after exposure to Apigenin for 24 or 48 h, the clone formation of SGC-7901 cells is suppressed in a dose- and time-dependent manner. The cloning efficiency in 80 μM is 9.8% and 5% after treatment with Apigenin for 24 and 48 h, while in the control group, it is 40.4% and 43.4%^[2].

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

In Vivo

Apigenin (4',5,7-Trihydroxyflavone), a natural flavonoid, possesses a broad spectrum of biological properties, including antioxidative, anti-inflammatory, anticancer, and neuroprotective effects. Apigenin (125 mg/kg and 250 mg/kg) alleviates Adriamycin (ADR) (24 mg/kg)-induced myocardial injury. Apigenin inhibits serum aspartate amino transferase (AST) release. Apigenin reduces serum lactate dehydrogenase (LDH) release. Apigenin reduces serum creatine kinase (CK) contents^[3].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 520-36-5
Appearance Solid
Molecular Weight 270.24
Formula C₁₅H₁₀O₅
Color Light yellow to green yellow
SMILES

OC1=C2C(OC(C3=CC=C(O)C=C3)=CC2=O)=CC(O)=C1
Synonyms

4',5,7-Trihydroxyflavone; Apigenol; C.I. Natural Yellow 1
Structure Classification
- Flavonoids
- Flavones
- Phenols
- Polyphenols
Initial Source
- Plants
- Umbelliferae
- Endogenous metabolite
- Human Gut Microbiota Metabolites
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (47)

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J Exp Clin Cancer Res

Apigenin suppresses PD-L1 expression in melanoma and host dendritic cells to elicit synergistic therapeutic effects. [Abstract]

2018 Oct 29;37(1):261. PMID: 30373602

Apigenin purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Oct 29;37(1):261. [Abstract]

A375, A2058, and RPMI-7951 cells were treated with DMSO (control), Curcumin (25 μM), or Apigenin (30 μM) for 24 h. Apigenin and Curcumin induce apoptosis in melanoma cells.

Apigenin purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Oct 29;37(1):261. [Abstract]

The protein expression levels of cleaved PARP are detected from Curcumin and Apigenin-treated A375, A2058, and RPMI-7951 cell lysates compared to control samples using Western blotting analyses.

Apigenin purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Oct 29;37(1):261. [Abstract]

A375 cells are incubated with DMSO, curcumin (25 μM), or apigenin (30 μM) for 4 h and then treated with IFN-γ (10 ng/mL) for indicated times. The levels of STAT1 phosphorylation at Tyr701 and total STAT1 are detected by Western blot analysis.

Apigenin purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Oct 29;37(1):261. [Abstract]

A375 cells are incubated with DMSO, curcumin (25 μM), or apigenin (30 μM) for 4 h and then treated with IFN-γ (10 ng/mL) for indicated times. The levels of STAT1 phosphorylation at Tyr701 and total STAT1 are detected by Western blot analysis.

Apigenin purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Oct 29;37(1):261. [Abstract]

A375 cells are incubated with DMSO, curcumin (25 μM), or apigenin (30 μM) for 4 h and then treated with IFN-γ (10 ng/mL) for indicated times. The levels of STAT1 phosphorylation at Tyr701 and total STAT1 are detected by Western blot analysis.

Apigenin purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Oct 29;37(1):261. [Abstract]

Western analysis of PD-L1 expression in A375, A2058, and RPMI-7951 cells treated with IFN-γ, curcumin, or apigenin.
Int J Surg

2026 Mar 11.
Cancer Lett

Apigenin inhibits recurrent bladder cancer progression by targeting VEGF-β. [Abstract]

2025 Apr 2:217676. PMID: 40185304
Food Chem

Effects of sun drying combined with baking processes on the flavor quality of Chongqing Tuocha raw tea. [Abstract]

2025 Dec 30:497:146992. PMID: 41285060
Food Chem

Flavonoid-mediated metabolic underpinning quality variation in red bud-sport pear mutants. [Abstract]

2025 May 31:489:144992. PMID: 40466530
Phytomedicine

Bruceantin inhibits the c-Myc/RL27A axis to suppress tumor progression in hepatocellular carcinoma. [Abstract]

2025 Dec 24:150:157740. PMID: 41477978
Phytomedicine

Fangchinoline suppresses nasopharyngeal carcinoma progression by inhibiting SQLE to regulate the PI3K/AKT pathway dysregulation. [Abstract]

2025 May:140:156484. PMID: 40090046
Clin Sci

A novel epigenetic drug conjugating flavonoid and HDAC inhibitor confer suppression of acute myeloid leukemogenesis. [Abstract]

2021 Jul 30;135(14):1751-1765. PMID: 34282832
Biomed Pharmacother

Apigenin attenuates visceral hypersensitivity in water avoidance stress rats by modulating the microbiota-gut-brain axis and inhibiting mast cell activation. [Abstract]

2023 Nov:167:115562. PMID: 37801900
Biomed Pharmacother

Apigenin ameliorates doxorubicin-induced renal injury via inhibition of oxidative stress and inflammation. [Abstract]

2021 May:137:111308. PMID: 33556877
Food Science and Human Wellness

2024 Jan, 13(1), Pages 211-224.
PLoS Biol

A high-throughput behavioral screening platform for measuring chemotaxis by C. elegans. [Abstract]

2024 Jun 27;22(6):e3002672. PMID: 38935621
Antioxidants (Basel)

Bioactive Extracts and Constituents from Taraxacum mongolicum: Antioxidant, Anti-Inflammatory, Enzyme-Inhibitory, and Molecular Docking Studies. [Abstract]

2026 May 29;15(6):688. PMID: 42351994
Antioxidants (Basel)

2025 Dec 29.
Lwt-Food Sci Technol

2022 May.
J Agric Food Chem

Natural Dietary Flavonoid Apigenin Mitigates Ulcerative Colitis via Modulating the AMPK/NF-κB/NLRP3 Signaling Axis. [Abstract]

2025 Dec 22. PMID: 41428381
Ind Crops Prod

2025 Dec 11;239:122458.
J Agric Food Chem

Apigenin-Mediated ESCRT-III Activation and Mitophagy Alleviate LPS-Induced Necroptosis in Renal Cells. [Abstract]

2025 Apr 10. PMID: 40211127
Biochem Pharmacol

A novel Apigenin derivative suppresses renal cell carcinoma via directly inhibiting wild-type and mutant MET. [Abstract]

2021 Aug:190:114620. PMID: 34043966
Food Funct

Apigenin protects mice against 3,5-diethoxycarbonyl-1,4-dihydrocollidine-induced cholestasis. [Abstract]

2021 Mar 15;12(5):2323-2334. PMID: 33620063
Drug Des Devel Ther

Luteolin Alleviates Liver Fibrosis in Rat Hepatic Stellate Cell HSC-T6: A Proteomic Analysis. [Abstract]

2023 Jun 17:17:1819-1829. PMID: 37360572
CNS Neurosci Ther

Apigenin inhibits fibrous scar formation after acute spinal cord injury through TGFβ/SMADs signaling pathway. [Abstract]

2022 Nov;28(11):1883-1894. PMID: 35906830
Front Pharmacol

Exploring the Therapeutic Mechanism of Desmodium styracifolium on Oxalate Crystal-Induced Kidney Injuries Using Comprehensive Approaches Based on Proteomics and Network Pharmacology. [Abstract]

2018 Jun 13:9:620. PMID: 29950996
J Mol Struct

2024 Sep 21.
Cancers (Basel)

Anticancer Effects and Molecular Mechanisms of Apigenin in Cervical Cancer Cells. [Abstract]

2022 Apr 4;14(7):1824. PMID: 35406599
ACS Omega

Delineating the Antiapoptotic Property of Apigenin as an Antitumor Agent: A Computational and In Vitro Study on HeLa Cells. [Abstract]

2024 May 30;9(23):24751-24760. PMID: 38882173
Front Cell Dev Biol

Curdione and Schisandrin C Synergistically Reverse Hepatic Fibrosis via Modulating the TGF-β Pathway and Inhibiting Oxidative Stress. [Abstract]

2021 Nov 10;9:763864. PMID: 34858986
Biochim Biophys Acta Mol Basis Dis

Apigenin enhancing oxidative resistance and proteostasis to extend lifespan via PTEN-mediated AKT signalling pathway. [Abstract]

2025 Jan 16:167670. PMID: 39826849
Biochim Biophys Acta Mol Basis Dis

Dietary apigenin ameliorates obesity-related hypertension through TRPV4-dependent vasorelaxation and TRPV4-independent adiponectin secretion. [Abstract]

2024 Aug 30:167488. PMID: 39218272
J Inflamm Res

Apigenin Suppresses NLRP3 Inflammasome Activation and Pyroptosis and Promotes Functional Recovery by Promoting Mitophagy in Experimental Spinal Cord Injured Rats. [Abstract]

2025 Oct 8:18:13965-13984. PMID: 41084615
Biomedicines

Rescue of Mutant CFTR Channel Activity by Investigational Co-Potentiator Therapy. [Abstract]

2025 Jan 1;13(1):82. PMID: 39857666
J Periodontal Res

Semaphorin 3A attenuates the hypoxia suppression of osteogenesis in periodontal ligament stem cells. [Abstract]

2022 Apr;57(2):425-433. PMID: 35037251
J Bioenerg Biomembr

PTGS2 as a potential target for apigenin to promote spinal cord injury repair. [Abstract]

2026 Mar 18. PMID: 41849073
Vet Microbiol

The Chinese medicine monomer Schisandrin C inhibits PRRSV infection by regulating the OGT-PI3K/AKT/mTOR signaling pathway. [Abstract]

2026 May:316:110992. PMID: 41865607
Toxicol In Vitro

Inhibitory potential of phytochemicals on species-specific breast cancer resistance protein transport activity. [Abstract]

2025 Dec:109:106128. PMID: 40796067
Exp Ther Med

Critical roles of Rad54 in tolerance to apigenin-induced Top1-mediated DNA damage. [Abstract]

2021 May;21(5):505. PMID: 33791014
Cytotechnology

Apigenin inhibits liver cancer via mitochondrial apoptosis and Th1/Th2 balance regulation. [Abstract]

2025 Dec;77(6):195. PMID: 41234482
Biol Pharm Bull

Regioselective Glucuronidation of Flavones at C5, C7, and C4' Positions in Human Liver and Intestinal Microsomes: Comparison among Apigenin, Acacetin, and Genkwanin. [Abstract]

2022;45(8):1116-1123. PMID: 35908893
Turk J Biol

Apigenin attenuates ischemia-reperfusion-induced pulmonary ferroptosis and fibrosis by activating the Nrf2/HO-1/GPX4 axis in mice. [Abstract]

2024 Oct 18;49(2):138-147. PMID: 40365099
Res Sq

2026 Apr 39.
SSRN

2025 May 7.
Res Sq

2025 Jan 09.
Research Square Preprint

2024 Mar 19.
Research Square Preprint

2023 Oct 23.
Phytomed Plus

2023 Sep 1, 100483.
bioRxiv

An efficient behavioral screening platform classifies natural products and other chemical cues according to their chemosensory valence in C. elegans. [Abstract]

2024 Apr 3:2023.06.02.542933. PMID: 37333363
Food Research

2021 5(1):357-365.

Solvent & Solubility

In Vitro:

DMSO : 80 mg/mL (296.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.7004 mL

18.5021 mL

37.0041 mL

5 mM

0.7401 mL

3.7004 mL

7.4008 mL

10 mM

0.3700 mL

1.8502 mL

3.7004 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (7.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (7.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% CMC-Na/saline water

Solubility: 10 mg/mL (37.00 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocol

Cell Assay^[2]

The effect of Apigenin on the viability of cells is determined by MTT assay. Near-confluent stock cultures of human gastric cancer SGC-7901 cells are harvested with 0.2% EDTA and plated at a density of 2.5×10³/well in 96-well microtiter plates. After an overnight incubation to allow cell attachment, the medium is replaced by fresh medium containing different concentrations (0, 20, 40, and 80 μM) of Apigenin. Control wells receive DMSO (0.2%). Each concentration of Apigenin is repeated in four wells. After incubation for 24 h, one plate is assayed with a microplate reader at the wavelength of 570 nm. Before the assay, MTT (5 mg/mL in PBS) is added to each well and incubated for 4 h, then MTT solution is removed from the wells by aspiration. After careful removal of the medium, 0.1 mL of DMSO is added to each well, and the plate is shaken for 15 min. The data of 7 d are fed into the computer and the growth curve is drawn. The growth inhibition rate (IR) is calculated^[2].

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

Animal Administration^[3]

Mice^[3]
Sixty healthy Kunming mice (26±2 g) are randomly assigned into two groups: a control group (n=15) and an ADR group (n=45). The ADR group is divided into three subgroups: ADR only without Apigenin (ADR, n=15), low-dose Apigenin (125 mg/kg/day, n=15), and high-dose Apigenin (250 mg/kg/day, n=15). All Apigenin-treated groups are treated daily via gastric gavage for seventeen days with a 125 or 250 mg/kg/day dose. ADR (3 mg/kg/day) is injected intraperitoneally into animals at an interval of 48 h (in total, eight times at a cumulative dose of 24 mg/kg). The mice in the control group receive injections of 0.9% sterile saline. On the 17th day after the first treatment, the mice are sacrificed, and blood samples are collected. A number of hearts are fixed with 2.5% glutaraldehyde fixative for electron microscopy analysis, and the others are stored at -80°C for western blot analysis.

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (289 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Si D, et al. Mechanism of CYP2C9 inhibition by flavones and flavonols. Drug Metab Dispos. 2009 Mar;37(3):629-34. [Content Brief]

[2]. Wu K, et al. Inhibitory effects of apigenin on the growth of gastric carcinoma SGC-7901 cells. World J Gastroenterol. 2005 Aug 7;11(29):4461-4. [Content Brief]

[3]. Yu W, et al. Apigenin Attenuates Adriamycin-Induced Cardiomyocyte Apoptosis via the PI3K/AKT/mTOR Pathway. Evid Based Complement Alternat Med. 2017;2017:2590676. [Content Brief]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.7004 mL	18.5021 mL	37.0041 mL	92.5104 mL
	5 mM	0.7401 mL	3.7004 mL	7.4008 mL	18.5021 mL
	10 mM	0.3700 mL	1.8502 mL	3.7004 mL	9.2510 mL
	15 mM	0.2467 mL	1.2335 mL	2.4669 mL	6.1674 mL
	20 mM	0.1850 mL	0.9251 mL	1.8502 mL	4.6255 mL
	25 mM	0.1480 mL	0.7401 mL	1.4802 mL	3.7004 mL
	30 mM	0.1233 mL	0.6167 mL	1.2335 mL	3.0837 mL
	40 mM	0.0925 mL	0.4626 mL	0.9251 mL	2.3128 mL
	50 mM	0.0740 mL	0.3700 mL	0.7401 mL	1.8502 mL
	60 mM	0.0617 mL	0.3084 mL	0.6167 mL	1.5418 mL
	80 mM	0.0463 mL	0.2313 mL	0.4626 mL	1.1564 mL
	100 mM	0.0370 mL	0.1850 mL	0.3700 mL	0.9251 mL

Keywords

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CAS No.:
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Apigenin

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Natural Product Library

Anti-Cancer Compound Library

Clinical Compound Library

Autophagy Compound Library

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Publications Citing Use of MedChemExpress (MCE) Apigenin

All Cytochrome P450 Isoforms

All Endogenous Metabolite Isoforms

Biological Activity

Chemical Information

Publications (47)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Apigenin Related Classifications

Cat. No.: HY-N1201