Casticin (Synonyms: Vitexicarpin)

Name: Casticin
Brand: MedChemExpress
SKU: HY-N0516
Rating: 5.0 (6 reviews)

Cat. No.: HY-N0516 Purity: 99.68%: Data Sheet
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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.

CAS No. : 479-91-4

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	Get quote
200 mg	Get quote

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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Casticin:

Casticin (Standard) Get quote

6 Publications Citing Use of MCE Casticin

Cell Proliferation/Viability Assay

Cell Imaging/Staining

Apoptosis Analysis

: 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.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

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]

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.

Molecular Weight

374.34

Formula

C₁₉H₁₈O₈

CAS No.

479-91-4

Appearance

Solid

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

Structure Classification

Initial Source

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)

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.68%

Select Batch:

Data Sheet (282 KB) SDS (393 KB)

COA (251 KB) HNMR (246 KB) LCMS (107 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]

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

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

Casticin Related Classifications

Inflammation/Immunology

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Casticin479-91-4VitexicarpinSTATInhibitorinhibitorinhibit

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Casticin (Synonyms: Vitexicarpin)

Customer Review

Other Forms of Casticin:

Casticin Related Antibodies

6 Publications Citing Use of MCE Casticin

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All STAT Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Casticin Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Casticin Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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