Clerodin
Clerodin (3-Deoxycaryoptinol) is a natural diterpenoid compound that can be isolated from traditional Chinese medicinal plants such as Clerodendrum infortunatum. Clerodin exhibits caspase-3 regulation, apoptosis induction, cell cycle arrest, ROS induction and glutathione depletion effects, along with anti-cancer and antifeedant activities. It shows selective cytotoxicity against leukemia cells and breast cancer cells, but has no obvious toxicity to normal human blood cells and lymphocytes. Clerodin also reduces the feeding behavior of Helicoverpa armigera larvae on cabbage leaf discs, but has no significant contact toxicity to these larvae. Clerodin can be used in research related to acute monocytic leukemia and human breast cancer.
For research use only. We do not sell to patients.
- CAS No.: 464-71-1
- Formula: C24H34O7
- Molecular Weight:434.52
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
All Caspase Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
Caspase 3 |
Caspase-7 |
In Vitro
Clerodin (60 μM) increases caspase-3 protein levels 5-fold and decreases Bcl-2 protein levels in human monocytic leukemia (THP-1) cells[1].
Clerodin (60 μM) induces a dose-dependent increase in cleaved caspase-3 activation (2 to 4-fold) in human monocytic leukemia (THP-1) cells[1].
Clerodin (60 μM) induces apoptosis-related morphological changes including nuclear condensation and apoptotic body formation in human monocytic leukemia (THP-1) cells[1].
Clerodin (60 μM) induces significant apoptosis in human monocytic leukemia (THP-1) cells, with 86.6% of cells in early or late apoptotic stages[1].
Clerodin (60 μM; 18 h) significantly upregulates caspase-3 gene expression 6-fold without altering Bcl-2 gene expression in human monocytic leukemia (THP-1) cells[1].
Clerodin (60 μM) increases intracellular ROS levels by ≥80% in human monocytic leukemia (THP-1) cells[1].
Clerodin significantly reduces reduced glutathione (GSH) levels and increases oxidized glutathione (GSSG) levels in human breast carcinoma MCF-7 cells, disrupting redox homeostasis[2].
Clerodin binds with highest affinity to human farnesyltransferase (PDB ID 1JCQ, ΔG = -8.2 kcal/mol) and second-highest affinity to human phosphoinositide 3-kinase (PDB ID 4FLH, ΔG = -7.9 kcal/mol), with weaker binding to other tested human cancer-related proteins[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human monocytic leukemia (THP-1) cells
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Concentration:60 μM
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Incubation Time:18 h
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Result:Caused a significant 6-fold upregulation of caspase-3 gene expression (p<0.01) compared to untreated controls.
Showed no significant change in Bcl-2 gene expression relative to controls.
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Cell Line:human breast carcinoma MCF-7 cells, normal human lymphocyte cells (HLCs)
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Concentration:0.5-100 μg/mL
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Incubation Time:24 h
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Result:Inhibited MCF-7 cell viability in a concentration-dependent manner, with an IC50 value of 30.88 μg/mL.
Showed 51% cell viability in HLCs at 25 μg/mL and 28% cell viability at 100 μg/mL.
Exhibited minimal toxicity to HLCs at concentrations up to 50 μg/mL.
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Cell Cytotoxicity Assay
- Mammalian live/dead viability and cytotoxicity staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- ROS/oxidative-stress fluorescent staining
- Apoptosis Solutions
- Protocol for Cell Cycle
- Breast Cancer Modeling
- Cell Viability Determination by MTT Colorimetric Assay
Chemical Information
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CAS No. 464-71-1
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Molecular Weight 434.52
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Formula C24H34O7
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SMILES
CC(OC[C@]12[C@]3(CCC[C@]1([H])[C@]([C@@H](C[C@@H]2OC(C)=O)C)([C@]4([H])C[C@]5([H])[C@](OC=C5)([H])O4)C)CO3)=O
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Synonyms
3-Deoxycaryoptinol
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Nagaraj B, et al. Clerodane diterpene 3-deoxycaryoptinol (Clerodin) selectively induces apoptosis in human monocytic leukemia (THP-1) cells and upregulates apoptotic protein caspase-3. Free radical biology & medicine. 2024 Nov 20;225:925-932. [Content Brief]
[2]. Pakrashy S, et al. Bioinformatics and Network Pharmacology of the First Crystal Structured Clerodin: Anticancer and Antioxidant Potential against Human Breast Carcinoma Cell. ACS omega. 2022 Dec 27;7(51):48572-48582. [Content Brief]
[3]. Abbaszadeh G, et al. Insecticidal and antifeedant activities of clerodane diterpenoids isolated from the Indian bhant tree, Clerodendron infortunatum, against the cotton bollworm, Helicoverpa armigera. Journal of insect science (Online). 2014 Feb 26;14:29. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Clerodin Related Classifications
HY-N20639 Related Classifications
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