Cat. No.: HY-N1950

Hispidulin

(Synonyms: Dinatin)

7 Cited Publications

Customer Review

Based on 7 publication(s) in Google Scholar

Hispidulin is a natural flavone with a broad spectrum of biological activities. Hispidulin is a Pim-1 inhibitor with an IC₅₀ of 2.71 μM.

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

Purity: 99.74%
CAS No.: 1447-88-7
Formula: C₁₆H₁₂O₆
Molecular Weight:300.26

Storage:

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

Hispidulin Chemical Structure

CAS No.: 1447-88-7

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Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (7)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Hispidulin is a natural flavone with a broad spectrum of biological activities. Hispidulin is a Pim-1 inhibitor with an IC₅₀ of 2.71 μM.

IC₅₀ & Target

IC50: 2.71 μM (Pim-1)^[1]

All Pim Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	ED₅₀	1.2 μg/mL Compound: hispidulin	Cytotoxicity against human A431 cells Cytotoxicity against human A431 cells	[PMID: 10579870]
BC1 cell line	ED₅₀	>20 μg/mL Compound: hispidulin	Cytotoxicity against human BC1 cells Cytotoxicity against human BC1 cells	[PMID: 10579870]
BC1 cell line	ED₅₀	19 μg/mL Compound: hispidulin	Cytotoxicity against human BC1 cells Cytotoxicity against human BC1 cells	[PMID: 7931367]
Col2	ED₅₀	>20 μg/mL Compound: hispidulin	Cytotoxicity against human Col2 cells Cytotoxicity against human Col2 cells	[PMID: 10579870]
Col2	ED₅₀	>20 μg/mL Compound: hispidulin	Cytotoxicity against human Col2 cells Cytotoxicity against human Col2 cells	[PMID: 7931367]
HEK293	EC₅₀	7.3 μM Compound: 12	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]
HT	ED₅₀	10.1 μg/mL Compound: hispidulin	Cytotoxicity against human HT cells Cytotoxicity against human HT cells	[PMID: 10579870]
HT-1080	ED₅₀	5.2 μg/mL Compound: hispidulin	Cytotoxicity against human HT1080 cells Cytotoxicity against human HT1080 cells	[PMID: 7931367]
Huh-7	CC₅₀	>50 μM Compound: 14	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	36.3 μM Compound: 14	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]
KB	ED₅₀	18.8 μg/mL Compound: hispidulin	Cytotoxicity against human KB cells Cytotoxicity against human KB cells	[PMID: 10579870]
KB	ED₅₀	22 μg/mL Compound: NSC-122415	Cytotoxicity against human KB cells Cytotoxicity against human KB cells	[PMID: 469554]
KB	ED₅₀	5.6 μg/mL Compound: hispidulin	Cytotoxicity against human KB cells Cytotoxicity against human KB cells	[PMID: 7931367]
KB	ED₅₀	96 μg/mL Compound: 6	Cytotoxicity against human KB cells Cytotoxicity against human KB cells	10.1021/np50005a002
KB-V1	ED₅₀	1.3 μg/mL Compound: hispidulin	Cytotoxicity against human multidrug-resistant KB-V1+ cells in presence of vinblastine Cytotoxicity against human multidrug-resistant KB-V1+ cells in presence of vinblastine	[PMID: 10579870]
KB-V1	ED₅₀	2.8 μg/mL Compound: hispidulin	Cytotoxicity against human KBV1 cells Cytotoxicity against human KBV1 cells	[PMID: 7931367]
KB-V1	ED₅₀	8.7 μg/mL Compound: hispidulin	Cytotoxicity against human multidrug-resistant KBV1 cells in absence of vinblastine Cytotoxicity against human multidrug-resistant KBV1 cells in absence of vinblastine	[PMID: 10579870]
LNCaP	ED₅₀	7.1 μg/mL Compound: hispidulin	Cytotoxicity against hormone-dependent human LNCaP cells Cytotoxicity against hormone-dependent human LNCaP cells	[PMID: 10579870]
Lu1	ED₅₀	>20 μg/mL Compound: hispidulin	Cytotoxicity against human Lu1 cells Cytotoxicity against human Lu1 cells	[PMID: 10579870]
Lu1	ED₅₀	17.6 μg/mL Compound: hispidulin	Cytotoxicity against human Lu1 cells Cytotoxicity against human Lu1 cells	[PMID: 7931367]
MDCK	CC₅₀	172.46 μM Compound: 3	Cytotoxicity against MDCK cells by MTT assay Cytotoxicity against MDCK cells by MTT assay	[PMID: 18640042]
MOLM-13	IC₅₀	6.4 μM Compound: NSC122415	Cytotoxicity against human MOLM-13 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human MOLM-13 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 33026809]
MOLM-13	IC₅₀	7 μM Compound: 40	Cytotoxicity against human MOLM-13 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Cytotoxicity against human MOLM-13 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 33393294]
MV4-11	IC₅₀	6.8 μM Compound: 40	Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 33393294]
MV4-11	IC₅₀	8.2 μM Compound: NSC122415	Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 33026809]
P388	ED₅₀	0.8 μg/mL Compound: hispidulin	Cytotoxicity against mouse P388 cells Cytotoxicity against mouse P388 cells	[PMID: 7931367]
SK-MEL-2	ED₅₀	11.5 μg/mL Compound: hispidulin	Cytotoxicity against human SK-MEL-2 cells Cytotoxicity against human SK-MEL-2 cells	[PMID: 7931367]
U-373MG ATCC	ED₅₀	8.8 μg/mL Compound: hispidulin	Cytotoxicity against human U373 cells Cytotoxicity against human U373 cells	[PMID: 10579870]
ZR-75-1	ED₅₀	1.2 μg/mL Compound: hispidulin	Cytotoxicity against hormone-dependent human ZR751 cells Cytotoxicity against hormone-dependent human ZR751 cells	[PMID: 10579870]

In Vitro

Hispidulin induces cell death in a dose- and time-dependent manner in HepG2 cells. Hispidulin induces apoptosis through mitochondrial dysfunction, which is characterized by decreased Bcl-2/Bax ratio, disrupted mitochondrial membrane potential and increased release of cytochrome C and activated capase-3^[2].

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

In Vivo

Hispidulin shows significant inhibitory effect on mice tumor size^[2].
Hispidulin treatment effectively prevents ovariectomy-induced body weight loss and attenuates ovariectomy-induced bone loss. Hispidulin treatment also decreases trabecular spacing in ovariectomy mice^[3].
Intraperitoneally administering hispidulin(10 or 50mg/ kg) to rats 30 min before intraperitoneally injecting kainic acid (15mg/kg) increases seizure latency and decreases seizure score. In addition, hispidulin substantially attenuates kainic acid-induced hippocampal neuronal cell death, and this protective effect is accompanied by the suppression of microglial activation and the production of proinflammatory cytokines such as interleukin-1β, interleukin-6, and tumor necrosis factor-α in the hippocampus^[4].

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

Chemical Information

CAS No. 1447-88-7
Appearance Solid
Molecular Weight 300.26
Formula C₁₆H₁₂O₆
Color Light yellow to yellow
SMILES

O=C1C=C(C2=CC=C(O)C=C2)OC3=CC(O)=C(OC)C(O)=C13
Synonyms

Dinatin
Structure Classification
- Flavonoids
- Flavones
- Phenols
- Polyphenols
Initial Source
- Plants
- Labiatae
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Publications (7)

All Cell Proliferation/Viability AssayCell Migration/Invasion AssayWBFlow CytometryBio/Physico-chemical Assay

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Journal Impact Factor

Acta Pharm Sin B

Chrysin serves as a novel inhibitor of DGK α/FAK interaction to suppress the malignancy of esophageal squamous cell carcinoma (ESCC). [Abstract]

2021 Jan;11(1):143-155. PMID: 33532186
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
J Transl Med

Hispidulin suppresses osteosarcoma by directly targeting FABP4 to disrupt lipid metabolism and inhibit the PI3K/AKT pathway. [Abstract]

2025 Oct 7;23(1):1062. PMID: 41057878

Hispidulin purchased from MedChemExpress. Usage Cited in: J Transl Med. 2025 Oct 7;23(1):1062. [Abstract]

Human osteosarcoma MG63 and 143B cells treated with various concentrations (20–60 µM) of HIS (Hispidulin) for 24, 48, and 72 h, as determined by the CCK-8 assay.

Hispidulin purchased from MedChemExpress. Usage Cited in: J Transl Med. 2025 Oct 7;23(1):1062. [Abstract]

The effects of HIS (Hispidulin) (7.5-30 µM) on the migration and invasion abilities of MG63 and 143B cells were examined by Transwell assays.

Hispidulin purchased from MedChemExpress. Usage Cited in: J Transl Med. 2025 Oct 7;23(1):1062. [Abstract]

Hispidulin (HIS) (7.5-15 µM; 48 h). Western blot analysis of the expression levels of G2/M phase-related proteins (CDK1, Cyclin B1), apoptosis-related protein (Bcl-2), and epithelial-mesenchymal transition (EMT)-related proteins (E-cadherin, N-cadherin, Vimentin) in MG63 and 143B cells. β-actin served as a loading control.

Hispidulin purchased from MedChemExpress. Usage Cited in: J Transl Med. 2025 Oct 7;23(1):1062. [Abstract]

Apoptosis in MG63 and 143B cells after HIS (Hispidulin) (7.5-30 µM; 48 h) treatment was detected by Annexin V-FITC/PI double staining followed by flow cytometry.

Hispidulin purchased from MedChemExpress. Usage Cited in: J Transl Med. 2025 Oct 7;23(1):1062. [Abstract]

Changes in intracellular free fatty acid (FFA) concentration and fatty acid synthase (FASN) activity in MG63 and 143B cells after HIS (Hispidulin) (15 µM; 48 h) treatment.
Ind Crops Prod

2025 Dec 11;239:122458.
Int J Mol Sci

Hesperetin from Root Extract of Clerodendrum petasites S. Moore Inhibits SARS-CoV-2 Spike Protein S1 Subunit-Induced NLRP3 Inflammasome in A549 Lung Cells via Modulation of the Akt/MAPK/AP-1 Pathway. [Abstract]

2022 Sep 7;23(18):10346. PMID: 36142258
University of Edinburgh

2025 May 29.

Solvent & Solubility

In Vitro:

DMSO : 62.5 mg/mL (208.15 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

3.3304 mL

16.6522 mL

33.3045 mL

5 mM

0.6661 mL

3.3304 mL

6.6609 mL

10 mM

0.3330 mL

1.6652 mL

3.3304 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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 (6.93 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 (6.93 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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (6.93 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, 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: 50% PEG300 50% Saline

Solubility: 10 mg/mL (33.30 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]

HepG2 cells are treated with different concentrations of hispidulin (50, 100, 200 μM) for 24, 48 and 72 h. Following treatment, cells are further incubated with MTT reagents at 37°C for 4 h before DMSO is added, to dissolve farmazan crystals, and absorbance is measured at 570 nm in a microplate reader^[2].

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

Animal Administration^[2]

Mice: Tumor are established in mice. Mice are treated with DMSO or Hispidulin at a dosage of 10, 20 or 40 mg/kg/day for 35 days. The body weight of tumour-bearing mice is recorded every week and tumour volume is calculated ^[2].

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 (279 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 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]. Chao SW, et al. Total Synthesis of Hispidulin and the Structural Basis for Its Inhibition of Proto-oncogene KinasePim-1. J Nat Prod. 2015 Aug 28;78(8):1969-76. [Content Brief]

[2]. Gao H, et al. Hispidulin induces apoptosis through mitochondrial dysfunction and inhibition of P13k/Akt signalling pathway in HepG2 cancer cells. Cell Biochem Biophys. 2014 May;69(1):27-34. [Content Brief]

[3]. Zhou R, et al. Hispidulin exerts anti-osteoporotic activity in ovariectomized mice via activating AMPK signaling pathway. Cell Biochem Biophys. 2014 Jun;69(2):311-7. [Content Brief]

[4]. Lin TY, et al. Protective effect of hispidulin on kainic acid-induced seizures and neurotoxicity in rats. Eur J Pharmacol. 2015 May 15;755:6-15. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.3304 mL	16.6522 mL	33.3045 mL	83.2612 mL
	5 mM	0.6661 mL	3.3304 mL	6.6609 mL	16.6522 mL
	10 mM	0.3330 mL	1.6652 mL	3.3304 mL	8.3261 mL
	15 mM	0.2220 mL	1.1101 mL	2.2203 mL	5.5507 mL
	20 mM	0.1665 mL	0.8326 mL	1.6652 mL	4.1631 mL
	25 mM	0.1332 mL	0.6661 mL	1.3322 mL	3.3304 mL
	30 mM	0.1110 mL	0.5551 mL	1.1101 mL	2.7754 mL
	40 mM	0.0833 mL	0.4163 mL	0.8326 mL	2.0815 mL
	50 mM	0.0666 mL	0.3330 mL	0.6661 mL	1.6652 mL
	60 mM	0.0555 mL	0.2775 mL	0.5551 mL	1.3877 mL
	80 mM	0.0416 mL	0.2082 mL	0.4163 mL	1.0408 mL
	100 mM	0.0333 mL	0.1665 mL	0.3330 mL	0.8326 mL

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Publications Citing Use of MedChemExpress (MCE) Hispidulin

All Pim Isoforms

Biological Activity

Chemical Information

Publications (7)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Hispidulin Related Classifications

HY-N1950 Related Classifications