Fig. 1 · Structure

Cat. No.: A10081
CAS No.: 520-36-5
Formula: C₁₅H₁₀O₅
Mol. Weight: 270.2

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Apigenin

Name: Apigenin
Brand: Adooq Bioscience
SKU: A10081
Availability: InStock

Cat. No. A10081 CAS 520-36-5

Protein kinase inhibitor

Apigenin, found in many plants, is a natural product belonging to the flavone class that is the aglycone of several naturally-occurring glycosides. Apigenin acts as a monoamine transporter activator, one of the few chemicals demonstrated to possess this property. Apigenin is a ligand for central benzodiazepine receptors that competitively inhibited the binding of flunitrazepam with a Ki of 4μM, exerting anxiolytic and slight sedative effects.

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Biological Activity

Bioactivity / Mechanism

Apigenin competitively inhibited human CYP2C9-mediated diclofenac 4′-hydroxylation in a purified reconstituted enzyme system, with a mean Ki of 2.0 µM. This value describes the tested enzyme–substrate system. [1]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

Target & Activity

Target	Activity	Value
CYP2C9	Ki	2 μM

Cellular Effect

Cell Line	Activity	Value	Description	Reference
A549	EC50	101 μM	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 12027739]
B16-BL6	EC50	31.6 μM	Antiproliferative activity against mouse B16-BL6 cells after 72 hrs by MTT assay	[PMID: 12027739]
BALB/3T3	IC50	141.4 μM	Growth inhibition of BALB/c mouse cloned 3T3/A31 cells after 72 hrs by nigrosin assay	[PMID: 10096863]
C2C12	IC50	26.58 μg/mL	Cytotoxicity against mouse C2C12 cells assessed as reduction in cell viability by MTT assay	[PMID: 33412152]
C8166	CC50	17.2 μg/mL	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	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]
H9	IC50	35 μM	Cytotoxicity against human H9 cells after 3 days	[PMID: 8158164]
H9	EC50	9 μM	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]
HCT-116	EC50	23.8 μM	Cytotoxicity against human HCT116 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 26529431]
HEK293	IC50	> 10 μM	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]
HEK293	IC50	1.13 μM	Inhibition of NOX4 expressed in HEK293 FS cells assessed as H2O2 production by H2O2/Tyr/LPO assay	[PMID: 20731357]
HEK293	EC50	24.9 μM	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]
HeLa	IC50	≥ 10 μM	Cytotoxicity against human HeLa cells by MTT assay	[PMID: 19278239]
HeLa	IC50	21.3 μM	Antiproliferative activity against human HeLa cells after 48 hrs by CCK8 assay	[PMID: 29475587]
HeLa	EC50	92.7 μM	Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay	[PMID: 12027739]
HeLa S3	IC50	> 10 μM	Cytotoxicity against human HeLa S3 cells assessed as cell viability incubated for 48 hrs by microscopic analysis	[PMID: 35704432]
HepG2	IC50	70.18 μM	Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay	[PMID: 26896708]
HL-60	IC50	22.3 μM	Antiproliferative activity against human HL60 cells after 48 hrs by CCK8 assay	[PMID: 29475587]
HT-1080	EC50	36.6 μM	Antiproliferative activity against human HT1080 cells after 72 hrs by MTT assay	[PMID: 12027739]
HT-22	EC50	> 100 μM	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]

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In Vitro Studies

Competitive inhibition of recombinant CYP2C9

Biochemical assay · Purified, reconstituted human CYP2C9 (RECO) with P450 reductase, cytochrome b5 and liposomes; diclofenac 4′-hydroxylation. [1]

Apigenin competitively inhibited diclofenac 4′-hydroxylation, with a reported mean Ki of 2.0 µM. This is an assay-specific biochemical result.

Measured endpoints — not treatment concentrations
Endpoint	Reported result	Reference
Inhibition of diclofenac 4′-hydroxylation	Ki 2.0 µM (mean)	[1]

Literature-Reported Treatment Conditions

Treatment concentration: Table 1: test compound from 0 to approximately 6 times Ki; individual apigenin concentration points not tabulated.
Exposure duration: 20 min
Method: Enzyme incubation at 37°C; diclofenac 2.5–100 µM.
Reported limits: Apigenin vehicle, replicate count and compound-specific uncertainty are not reported in the selected assay description/table. Ki is a measurement, not a recommended treatment concentration.

Methods and source locations

Compound reported in the paper: Apigenin

Literature study of apigenin; not product-lot validation.

Table 1 (apigenin row, caption and competitive-inhibition footnote); Materials; Enzyme Assays; Kinetic Analysis (pp. 629–631)

Inhibition of diclofenac 4′-hydroxylation: HPLC product measurement and nonlinear regression of enzyme kinetic data. — Table 1 (apigenin row, caption and competitive-inhibition footnote); Materials; Enzyme Assays; Kinetic Analysis (pp. 629–631)

In Vivo Studies

In Adriamycin-treated mice, oral apigenin for 17 days reduced serum LDH at 125 and 250 mg/kg/day and AST at 250 mg/kg/day. These results concern serum injury markers; they do not establish exposure, survival benefit or a causal signaling mechanism. [2]

Serum injury markers in Adriamycin-treated mice

Animal study · Male Kunming mice, 26 ± 2 g; Adriamycin-associated myocardial injury; 15 mice initially assigned per group. [2]

Apigenin reduced serum LDH at both tested doses and AST at the higher dose versus the Adriamycin group. The lower dose did not have a significant AST reduction marked in Figure 1a. These are injury-marker outcomes, not pharmacokinetic or clinical efficacy measurements.

Measured endpoints — not treatment concentrations
Endpoint	Reported result	Reference
Serum AST versus Adriamycin control	Reported statistical comparison 250 mg/kg/day: P = 0.003; 125 mg/kg/day: no significance marker in Figure 1a	[2]
Serum LDH versus Adriamycin control	Reported statistical comparison 125 mg/kg/day: P = 0.001; 250 mg/kg/day: P = 0.002	[2]

Conditions shared by the study groups

Route: Gastric gavage
Frequency: Daily
Treatment course: 17 days
Vehicle: 0.5% CMC-Na

Study groups and reported outcomes
Group / dose	Comparator	Observed result	Reference
Low-dose apigenin 125 mg/kg/day	Adriamycin plus CMC-Na; additional normal control received saline plus CMC-Na.	LDH reduced (P = 0.001); AST reduction not marked significant.	[2]
High-dose apigenin 250 mg/kg/day	Adriamycin plus CMC-Na; additional normal control received saline plus CMC-Na.	LDH reduced (P = 0.002) and AST reduced (P = 0.003).	[2]

Low-dose apigenin: Model: Adriamycin-treated Kunming mice; Reported limits: 15 initially assigned per group; Figure 1 reports n = 10. The paper reports 3 deaths in ADR control, 3 at low dose and 1 at high dose; no survival efficacy claim.

High-dose apigenin: Model: Adriamycin-treated Kunming mice; Reported limits: 15 initially assigned per group; Figure 1 reports n = 10. The paper reports 3 deaths in ADR control, 3 at low dose and 1 at high dose; no survival efficacy claim.

Methods and source locations

Compound reported in the paper: Apigenin; Compound label in the paper: API

Literature study of apigenin; not product-lot validation.

Sections 2.1, 2.2, 2.4, 2.7 and 3.1; Figure 1a–b and legend

Serum AST versus Adriamycin control: Serum assay kit; Figure 1 n = 10 per group, mean ± SEM; one-way ANOVA with LSD post hoc test. — Sections 2.1, 2.2, 2.4, 2.7 and 3.1; Figure 1a–b and legend

Serum LDH versus Adriamycin control: Serum assay kit; Figure 1 n = 10 per group, mean ± SEM; one-way ANOVA with LSD post hoc test. — Sections 2.1, 2.2, 2.4, 2.7 and 3.1; Figure 1a–b and legend

Low-dose apigenin · Sections 2.1, 2.2, 2.4, 2.7 and 3.1; Figure 1a–b and legend

High-dose apigenin · Sections 2.1, 2.2, 2.4, 2.7 and 3.1; Figure 1a–b and legend

Specifications

Manufacturer	Adooq Bioscience
Actions	Activator
CAS Number	520-36-5
Applications	Protein kinase inhibitor
Formula	C₁₅H₁₀O₅
Molecular Weight	270.2
Synonyms	4',5,7-Trihydroxyflavone; Apigenol; C.I. Natural Yellow 1
SMILES	C1=CC(=CC=C1C2=CC(=O)C3=C(C=C(C=C3O2)O)O)O

Storage & Solubility

In Vitro Solubility

Reported Solubility

Solvent	Reported Solubility
DMSO	46 mg/mL (170.22 mM)
Water	Insoluble
Ethanol	Insoluble

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

[1] Si D, Wang Y, Zhou YH, et al. Mechanism of CYP2C9 inhibition by flavones and flavonols. Drug metabolism and disposition: the biological fate of chemicals (2009). PMID: 19074529 DOI: 10.1124/dmd.108.023416 Source material
[2] Yu W, Sun H, Zha W, et al. Apigenin Attenuates Adriamycin-Induced Cardiomyocyte Apoptosis via the PI3K/AKT/mTOR Pathway. Evidence-based complementary and alternative medicine : eCAM (2017). PMID: 28684964 DOI: 10.1155/2017/2590676 Source material