Cat. No.: HY-N0516

Casticin

(Synonyms: Vitexicarpin)

6 Cited Publications

Customer Review

Based on 6 publication(s) in Google Scholar

Casticin is a methyoxylated flavonol isolated from Vitex rotundifolia, with antimitotic and anti-inflammatory effect. Casticin inhibits the activation of STAT3.

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

Purity: 99.68%
CAS No.: 479-91-4
Formula: C₁₉H₁₈O₈
Molecular Weight:374.34

Storage:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Casticin Chemical Structure

CAS No.: 479-91-4

Size

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Top Publications Citing

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 (6)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Casticin is a methyoxylated flavonol isolated from Vitex rotundifolia, with antimitotic and anti-inflammatory effect. Casticin inhibits the activation of STAT3.

IC₅₀ & Target

STAT3^[3]

All STAT Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
Col2	ED₅₀	12.7 μg/mL Compound: 1	Cytotoxicity against human Col2 cells Cytotoxicity against human Col2 cells	[PMID: 12828478]
HCT-116	GI₅₀	119 ng/mL Compound: 9	Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 11975496]
HUVEC	ED₅₀	0.6 μg/mL Compound: 1	Cytotoxicity against HUVEC Cytotoxicity against HUVEC	[PMID: 12828478]
KB	ED₅₀	0.2 μg/mL Compound: 1	Cytotoxicity against human KB cells Cytotoxicity against human KB cells	[PMID: 12828478]
KB	IC₅₀	97 nM Compound: 10, casticin, vitexicarpin	Cytotoxicity against human KB cells after 72 hrs by MTS assay Cytotoxicity against human KB cells after 72 hrs by MTS assay	[PMID: 20356063]
LNCaP	ED₅₀	0.5 μg/mL Compound: 1	Cytotoxicity against human LNCAP cells Cytotoxicity against human LNCAP cells	[PMID: 12828478]
Lu1	ED₅₀	0.8 μg/mL Compound: 1	Cytotoxicity against human Lu1 cells Cytotoxicity against human Lu1 cells	[PMID: 12828478]
PC-12	GI₅₀	114 ng/mL Compound: 9	Cytotoxicity against rat PC12 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against rat PC12 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 11975496]
RAW264.7	IC₅₀	21.4 μM Compound: 24	Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production after 24 hrs by Griess method Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production after 24 hrs by Griess method	[PMID: 24035341]
TERT-RPE1	ED₅₀	0.2 μg/mL Compound: 1	Cytotoxicity against human telomerase reverse transcriptase expressing RPE1 cells Cytotoxicity against human telomerase reverse transcriptase expressing RPE1 cells	[PMID: 12828478]

In Vitro

Casticin (0.2-1.0 μM) dose-dependently inhibits the proliferation of KB cells, with an IC₅₀ of 0.23 μM on day 3, while shows no significant inhibition on 3T3 Swiss Albino and TIG-103 cells. Casticin (0.6 μM) alters spindle morphology with partial mitotic spindle breakdown or with disordered spindles^[1]. Casticin (0-40 μM) dose-dependently inhibits the proliferation of LX2 cells. Casticin (40 μM) suppresses L02 cells proliferation and induces apoptosis. Casticin inhibits fibrotic effects of TGF-β1 on ECM deposition in LX2 cells by evaluating the mRNA levels of TGF-β, collagen α1(I), MMP-2, MMP-9, TIMP-1 and TIMP-2^[2]. Casticin (0-8 μM) reduces the viability of 786-O, YD-8, and HN-9 cells, but shows no significant effect on that of the normal HEL 299 cells. Casticin (5 μM) increases cleavage caspase-3 and PPAR, diminishes the levels of B-cell lymphoma-extra large (Bcl-xl), Bcl-2, IAP-1/-2, vascular endothelial growth factor (VEGF), matrix metallopeptidase 9 (MMP-9), and cyclooxygenase 2 (COX-2) proteins in 786-O, YD-8, and HN-9 cells. Casticin (5 μM) also promotes apoptotic cell death, inhibits constitutively active STAT3 in tumor cells, modulates STAT3 activation by altering the activity of upstream STAT3 regulators, and abrogates IL-6-induced STAT3 activation. In addition, Casticin (2.5 μM) enhances the effect of ionizing radiation in 786-O cells and potentiates the therapeutic effect of radiotherapy^[3].

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

In Vivo

Casticin (20 mg/kg, p.o.) has toxic effect on the liver in mice with CCl4-and BDL-induced hepatic injury. Casticin attenuates liver fibrosis induced by CCl4 or BDL in vivo. Casticin inhibits HSC activation and collagen matrix expression by blocking TGF-β/Smad signaling in vivo^[2].

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

Chemical Information

CAS No. 479-91-4
Appearance Solid
Molecular Weight 374.34
Formula C₁₉H₁₈O₈
Color Light yellow to yellow
SMILES

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

Vitexicarpin
Structure Classification
- Flavonoids
- Flavones
Initial Source
- Plants
- Labiatae
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (6)

All Cell Proliferation/Viability AssayCell Imaging/StainingApoptosis Analysis

Sort by:

Journal Impact Factor

Phytomedicine

Vitexicarpin suppresses malignant progression of colorectal cancer through affecting c-Myc ubiquitination by targeting IMPDH2. [Abstract]

2024 Sep:132:155833. PMID: 39008915
J Ethnopharmacol

Integrating bioinformatic analysis, network pharmacology, molecular docking and experimental validation to explore the mechanism of Tian Long Cha against influenza virus. [Abstract]

2025 Jun 12:349:119964. PMID: 40368255
Biochem Pharmacol

Lysine methylation-mediated SMYD2 degradation by casticin sensitizes non-small-cell lung cancer cells to osimertinib therapy. [Abstract]

2026 Jan;243(Pt 2):117562. PMID: 41314435
Rheumatology (Oxford)

Autophagy inhibitors block pathogenic NET release in immune-mediated inflammatory disease without impairing host defence. [Abstract]

2025 Aug 13:keaf437. PMID: 40802538
Genes (Basel)

Casticin Impacts Key Signaling Pathways in Colorectal Cancer Cells Leading to Cell Death with Therapeutic Implications. [Abstract]

2022 May 3;13(5):815. PMID: 35627200

Casticin purchased from MedChemExpress. Usage Cited in: Genes (Basel). 2022 May 3;13(5):815. [Abstract]

Cytotoxicity of Casticin on HCT116 cell line; for concentrations beginning 1 µM onwards when compared to control.

Casticin purchased from MedChemExpress. Usage Cited in: Genes (Basel). 2022 May 3;13(5):815. [Abstract]

Representative image of the control cultures and cultures from Casticin (5 µM) treatment for 48 h.

Casticin purchased from MedChemExpress. Usage Cited in: Genes (Basel). 2022 May 3;13(5):815. [Abstract]

Total number of apoptotic cells increased significantly in Casticin (5 μM)-treated group.
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

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (267.14 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

2.6714 mL

13.3568 mL

26.7137 mL

5 mM

0.5343 mL

2.6714 mL

5.3427 mL

10 mM

0.2671 mL

1.3357 mL

2.6714 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 6.25 mg/mL (16.70 mM); Clear solution

This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

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]

LX-2 cells or L02 cells are plated at a density of 5 × 10³ cells per well in a 96-well plate and treated with Casticin (0-40 μM) for 48 h in growth medium containing serum. Cell proliferation is determined using a CCK-8 assay kit^[2].

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

Animal Administration^[2]

Mice^[2]
Male mice 6-8 weeks of age weighing 20-30 g are kept in a temperature-controlled room with an alternating 12 h dark and light cycle. A total of 32 mice are divided randomly into four groups of 8 animals each: control, Casticin, CCl4, and CCl4 + Casticin. To induce liver fibrosis, CCl4 dissolved in olive oil (20%) is injected intraperitoneally into mice (1.0 mL/kg body weight) in the CCl4 and CCl4 + Casticin groups twice a week for six weeks. Mice in the control group and Casticin group are injected with an equivalent volume of olive oil. Casticin is dissolved in 0.25% Tween-80. After treatment with CCl4 or olive oil for six weeks, mice in the Casticin group and CCl4 + Casticin group receives Casticin (20 mg/kg) by gastric gavage daily for two weeks, and the other two groups are given the equivalent volume of 0.25% Tween-80. After the eight week intervention period, mice are euthanatized under 3% pentobarbital sodium anesthesia (40 mg/kg ip), and the livers and blood from all animals are collected. Serum is obtained by centrifugation (1600 g, 15 min) and stored at −20°C for further examination^[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 (282 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)
- Korean - KR (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]. Kobayakawa J, et al. G2-M arrest and antimitotic activity mediated by casticin, a flavonoid isolated from Viticis Fructus (Vitex rotundifolia Linne fil.). Cancer Lett. 2004 May 10;208(1):59-64. [Content Brief]

[2]. Zhou L, et al. Casticin attenuates liver fibrosis and hepatic stellate cell activation by blocking TGF-β/Smad signaling pathway. Oncotarget. 2017 Apr 27;8(34):56267-56280. [Content Brief]

[3]. Lee JH, et al. Casticin inhibits growth and enhances ionizing radiation-induced apoptosis through the suppression of STAT3 signaling cascade. J Cell Biochem. 2018 Dec 5. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6714 mL	13.3568 mL	26.7137 mL	66.7842 mL
	5 mM	0.5343 mL	2.6714 mL	5.3427 mL	13.3568 mL
	10 mM	0.2671 mL	1.3357 mL	2.6714 mL	6.6784 mL
	15 mM	0.1781 mL	0.8905 mL	1.7809 mL	4.4523 mL
	20 mM	0.1336 mL	0.6678 mL	1.3357 mL	3.3392 mL
	25 mM	0.1069 mL	0.5343 mL	1.0685 mL	2.6714 mL
	30 mM	0.0890 mL	0.4452 mL	0.8905 mL	2.2261 mL
	40 mM	0.0668 mL	0.3339 mL	0.6678 mL	1.6696 mL
	50 mM	0.0534 mL	0.2671 mL	0.5343 mL	1.3357 mL
	60 mM	0.0445 mL	0.2226 mL	0.4452 mL	1.1131 mL
	80 mM	0.0334 mL	0.1670 mL	0.3339 mL	0.8348 mL
	100 mM	0.0267 mL	0.1336 mL	0.2671 mL	0.6678 mL

Keywords

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

Casticin

Differentiation Inducing Compound Library

Medicine Food Homology Compound Library

Traditional Chinese Medicine Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Flavonoids Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Obesity Compound Library

Transcription Factor-Targeted Library

Anti-Cancer Natural Product Library

Anti-inflammatory Traditional Chinese Medicine Active Compound Library

Plant-Sourced Natural Product Library

Human Metabolite Library

Cancer Stem Cells Compound Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Natural Product Library Plus

Bioactive Compound Library

Miao Ethnicity Medicine Compound Library

Tibetan Medicine Compound Library

Heat-Clearing and Detoxification Traditional Chinese Medicine Compound Library

RO5 Drug-like Natural Product Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

High-Throughput Natural Product Library

Ancient Chinese Classical Formulas Traditional Chinese Medicine Active Compound Library

Mass Spectrometry Human Metabolite Library

Antitussive and Antiasthmatic Traditional Chinese Medicine Active Compound Library

Diarrhea-Related Traditional Chinese Medicine Active Compound Library

Posttranslational Modification Library

Mongolian Medicine Compound Library

Tonifying Traditional Chinese Medicine Monomer Compound Library

Mass Spectrometry Natural Product Library

Natural Product and Natural Product-Like Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Stem Cell Signaling Compound Library

Natural Product Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Publications Citing Use of MedChemExpress (MCE) Casticin

All STAT Isoforms

Biological Activity

Chemical Information

Publications (6)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Casticin Related Classifications

HY-N0516 Related Classifications