Chelerythrine chloride
Based on 20 publication(s) in Google Scholar
Chelerythrine chloride is a potent, cell-permeable inhibitor of protein kinase C, with an IC50 of 660 nM. Chelerythrine chloride inhibits the Bcl-XL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaces Bax from Bcl-XL. Chelerythrine chloride induces apoptosis and autophagy.
For research use only. We do not sell to patients.
- Purity : 99.11%
- CAS No.: 3895-92-9
- Formula: C21H18ClNO4
- Molecular Weight:383.82
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Chelerythrine chloride
More- Cell Commun Signal. 2021 Oct 11;19(1):103. [Abstract]
- J Headache Pain. 2022 Mar 8;23(1):35. [Abstract]
- Phytother Res. 2023 Oct;37(10):4674-4689. [Abstract]
- J Pineal Res. 2026 Mar;78(2):e70135. [Abstract]
- Cancer Cell Int. 2023 Jun 17;23(1):117. [Abstract]
- Nutrients. 2025 Nov 12;17(22):3534. [Abstract]
- Front Pharmacol. 2021 May 13:12:655726. [Abstract]
- Sci Rep. 2017 Aug 23;7(1):9201. [Abstract]
- J Inflamm Res. 2025 Mar 20:18:4213-4231. [Abstract]
- Front Physiol. 2021 Oct 28;12:770430. [Abstract]
- FASEB J. 2019 Dec;33(12):13644-13659. [Abstract]
- Cytokine. 2024 Oct:182:156717. [Abstract]
- Fishes. 2022, 7(5), 229.
- Vet Microbiol. 2026 May:316:110992. [Abstract]
- Biochem Biophys Res Commun. 2024 Dec 20:739:150914. [Abstract]
- Planta Med. 2024 Jun;90(7-08):523-533. [Abstract]
- Bull Sib Med. 2025.
- University of Pennsylvania. 2026.
- Heliyon. 2024 Jul 28;10(15):e35368. [Abstract]
- Research Square Preprint. 2020 Oct.
Customer Validation & Images
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Histological Imaging/Staining
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Biological Activity
Description
IC50 & Target
[5]|
PKC 660 nM (IC50) |
PKA 0.17 mM (IC50) |
TPK 0.1 mM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| A2780 | IC50 |
4.63 μM
Compound: chelerythrine
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In vitro cytotoxicity for human ovarian tumor A2780 cells
In vitro cytotoxicity for human ovarian tumor A2780 cells
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[PMID: 15999988] |
| Astrocyte | EC50 |
1.531 μM
Compound: 36
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Antiproliferative activity against mouse astrocyte cells by MTT assay
Antiproliferative activity against mouse astrocyte cells by MTT assay
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[PMID: 17417631] |
| HCT-116 | IC50 |
2.13 μM
Compound: 1a
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Antiproliferative activity against human HCT116 cells assessed as inhibition of cell viability after 48 hrs by MTT assay
Antiproliferative activity against human HCT116 cells assessed as inhibition of cell viability after 48 hrs by MTT assay
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[PMID: 26026362] |
| HeLa | IC50 |
1.24 μg/mL
Compound: 5, chelerythrine
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Growth inhibition of human HeLa S3 cells after 72 hrs
Growth inhibition of human HeLa S3 cells after 72 hrs
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[PMID: 10395504] |
| HL-60 | IC50 |
2.99 μM
Compound: 1a
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Antiproliferative activity against human HL60 cells assessed as inhibition of cell viability after 48 hrs by WST-1 assay
Antiproliferative activity against human HL60 cells assessed as inhibition of cell viability after 48 hrs by WST-1 assay
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[PMID: 26026362] |
| Panel NCI-60 (60 carcinoma cell lines) | GI50 |
188 nM
Compound: chelerythrine
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Growth inhibitory activity against human cancer cell line in the NCI's anticancer drug screening program
Growth inhibitory activity against human cancer cell line in the NCI's anticancer drug screening program
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[PMID: 15743190] |
In Vitro
Chelerythrine inhibits the BclXL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaces Bax, a BH3-containing protein, from BclXL. Mammalian cells treated with Chelerythrine undergoes apoptosis with characteristic features that suggest involvement of the mitochondrial pathway[1]. Chelerythrine treatment inhibits LPS-induced TNF-α level and NO production in LPS-induced murine peritoneal macrophages through selective inhibition of p38 mitogen-activated protein kinase (MAPK) and extracellular signal-regulated protein kinases 1 and 2 (ERK1/2) activation. Moreover, the effects of chelerythrine on NO and cytokine TNF-α production can possibly be explained by the role of p38 MAPK and ERK1/2 in the regulation of inflammatory mediators expression[2]. Chelerythrine shows cytotoxic effect on the human monocytic leukaemia cells with LD50 value of 3.46 μM. Two hours after LPS stimulation, cells influenced by sanguinarine and Chelerythrine significantly decline the CCL-2 expression by a factors of 3.5 and 1.9[3]. Chelerythrine chloride significantly enhances the phosphorylation of ERK1/2 in a dose-dependent manner. In addition, chelerythrine chloride inhibits the phosphorylation of p38[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3895-92-9
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Appearance Solid
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Molecular Weight 383.82
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Formula C21H18ClNO4
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Color Yellow to orange
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SMILES
C[N+]1=CC2=C(C(OC)=CC=C2C3=C1C4=CC5=C(OCO5)C=C4C=C3)OC.[Cl-]
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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
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (20)
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Journal Impact Factor
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Most Recent
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Cell Commun Signal
Zinc-mediated activation of CREB pathway in proliferation of pulmonary artery smooth muscle cells in pulmonary hypertension. [Abstract]2021 Oct 11;19(1):103. PMID: 34635097 -
J Headache Pain
Calcitonin gene-related peptide receptor antagonist BIBN4096BS regulates synaptic transmission in the vestibular nucleus and improves vestibular function via PKC/ERK/CREB pathway in an experimental chronic migraine rat model. [Abstract]2022 Mar 8;23(1):35. PMID: 35260079 -
Phytother Res
Chelerythrine chloride inhibits the progression of colorectal cancer by targeting cancer-associated fibroblasts through intervention with WNT10B/β-catenin and TGFβ2/Smad2/3 axis. [Abstract]2023 Oct;37(10):4674-4689. PMID: 37402476 -
J Pineal Res
Melatonin Enhances the Myometrial Contraction Through MT2-PKC-NRF2/MAFF Signaling Pathway in Sows. [Abstract]2026 Mar;78(2):e70135. PMID: 41854048 -
Cancer Cell Int
High FAAP24 expression reveals poor prognosis and an immunosuppressive microenvironment shaping in AML. [Abstract]2023 Jun 17;23(1):117. PMID: 37328842 -
Nutrients
2025 Nov 12;17(22):3534. PMID: 41305585
Chelerythrine chloride purchased from MedChemExpress. Usage Cited in: Nutrients. 2025 Nov 12;17(22):3534. [Abstract]
The PKC protein expression in the Chelerythrine (0-8μM)-treated groups gradually decreased with increasing dose.
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Front Pharmacol
Propofol Inhibits Ischemia/Reperfusion-Induced Cardiotoxicity Through the Protein Kinase C/Nuclear Factor Erythroid 2-Related Factor Pathway. [Abstract]2021 May 13:12:655726. PMID: 34054535 -
Sci Rep
Neuroprotective Effects of CGP3466B on Apoptosis Are Modulated by Protein-L-isoaspartate (D-aspartate) O-methyltransferase/Mst1 Pathways after Traumatic Brain Injury in Rats. [Abstract]2017 Aug 23;7(1):9201. PMID: 28835703
Chelerythrine chloride purchased from MedChemExpress. Usage Cited in: Sci Rep. 2017 Aug 23;7(1):9201. [Abstract]
CGP3466B upregulates PCMT1 expression and inhibits cleaved-Mst1 activation at 24 h after TBI. Chelerythrine activates the Mst1 without regulating PCMT1 protein level. (a) Western blot assay for the expression of PCMT1. (b) Western blot assay for the expression of Mst1 and cleaved-Mst1.
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J Inflamm Res
2025 Mar 20:18:4213-4231. PMID: 40129872
Chelerythrine chloride purchased from MedChemExpress. Usage Cited in: J Inflamm Res. 2025 Mar 20:18:4213-4231. [Abstract]
CLT (Chelerythrine chloride, 5 and 8 μM) downregulated the expression of FLI1 in HEL cells, as determined via Western blotting.
Chelerythrine chloride purchased from MedChemExpress. Usage Cited in: J Inflamm Res. 2025 Mar 20:18:4213-4231. [Abstract]
The effect of Chelerythrine (CLT, 5 and 8 μM) on FLI1 downregulation was significantly diminished in the scrambled control cells versus FLI1 knockdown HEL cells.
Chelerythrine chloride purchased from MedChemExpress. Usage Cited in: J Inflamm Res. 2025 Mar 20:18:4213-4231. [Abstract]
IMQ administration. Images in the top showed significant attenuation in IMQ-induced psoriasis following CLT (Chelerythrine chloride, 4 mg/kg) treatment. H&E staining analysis of the dorsal skin of the IMQ group on day 7 revealed significant epidermal hyperplasia, increased acanthosis, parakeratosis, telangiectasia, and inflammatory cell infiltration. CLT injection significantly reversed these histological changes caused by IMQ, showing less parakeratosis and less epidermal thickening than the IMQ group.
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Front Physiol
Roles of Endothelial Motilin Receptor and Its Signal Transduction Pathway in Motilin-Induced Left Gastric Artery Relaxation in Dogs. [Abstract]2021 Oct 28;12:770430. PMID: 34777026 -
FASEB J
EphrinB2/ephB2-mediated myenteric synaptic plasticity: mechanisms underlying the persistent muscle hypercontractility and pain in postinfectious IBS. [Abstract]2019 Dec;33(12):13644-13659. PMID: 31601124 -
Cytokine
Chelerythrine ameliorates Aspergillus fumigatus keratitis through suppressing the LOX-1/p38 MAPK signaling pathway. [Abstract]2024 Oct:182:156717. PMID: 39067394 -
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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 -
Biochem Biophys Res Commun
2024 Dec 20:739:150914. PMID: 39536412 -
Planta Med
Novel Approaches for the Analysis and Isolation of Benzylisoquinoline Alkaloids in Chelidonium majus. [Abstract]2024 Jun;90(7-08):523-533. PMID: 38843792 -
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Heliyon
Pan-cancer investigation of RFX family and associated genes identifies RFX8 as a therapeutic target in leukemia. [Abstract]2024 Jul 28;10(15):e35368. PMID: 39170430 -
Solvent & Solubility
In Vitro:
DMSO : 4.35 mg/mL (11.33 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.44 mg/mL (1.15 mM); Clear solution
This protocol yields a clear solution of ≥ 0.44 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (4.4 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.43 mg/mL (1.12 mM); Clear solution
This protocol yields a clear solution of ≥ 0.43 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (4.3 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
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 (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocols
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Autophagy
Autophagy is a process in which eukaryotic cells use lysosomes to degrade their own cytoplasmic proteins and damaged organelles under the regulation of autophagy related gene (Atg). Microtubule-associated proteins light chain 3 (LC3) is recognized as autophagy marker, which transfers from cytoplasmic LC3 (LC3-I) to membrane type (LC3-II). LC3-II/I ratio could be detected by Western Blot and fluorescence microscopy.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Lysosome and acidic-vesicle live-cell staining
Lysosome and acidic-vesicle live-cell staining detects acidic intracellular compartments by using membrane-permeant acidotropic probes that accumulate in low-pH vesicles, including lysosomes, late endosomes, autolysosomes, and acidic phagosomes. LysoTracker staining is commonly used as an intensity-based readout of acidic lysosomal compartment abundance or enlargement, while acridine orange produces green fluorescence in less concentrated compartments and red fluorescence after concentration-dependent accumulation in acidic vesicular organelles. Loss or reduction of acridine-orange red signal can be used as a readout of lysosomal membrane permeabilization or reduced acidic-vesicle integrity. This protocol is designed for live cultured cells and can be adapted for fluorescence microscopy, high-content imaging, plate-reader readout, or flow cytometry when the selected literature supports the readout. Because these dyes report acidotropic accumulation rather than lysosome identity alone,
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Macroautophagy Solutions
Macroautophagy is a conserved lysosome-dependent degradation pathway in which cytoplasmic material is sequestered into double-membrane autophagosomes and delivered to lysosomes for degradation and recycling. The pathway supports cellular homeostasis during nutrient limitation, organelle stress, protein-aggregate accumulation, infection, differentiation, and tissue remodeling by coupling cargo sequestration, autophagosome maturation, lysosomal fusion, and degradation of cargo-derived macromolecules. The core molecular sequence includes initiation by nutrient- and stress-regulated autophagy machinery, autophagosome nucleation, LC3/ATG8-family conjugation to autophagosomal membranes, cargo selection through receptors such as SQSTM1/p62, autophagosome-lysosome fusion, and lysosomal degradation. LC3 was identified as a mammalian homolog of yeast Atg8 that localizes to autophagosomal membranes after processing, and p62/SQSTM1 was shown to connect ubiquitinated cargo with autophagic degradati
Purity & Documentation
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Data Sheet (282 KB)
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SDS (420 KB)
- English - EN (420 KB)
- Français - FR (420 KB)
- Deutsch - DE (420 KB)
- Norwegian - NO (420 KB)
- Español - ES (420 KB)
- Swedish - SV (420 KB)
- Italian - IT (420 KB)
- Korean - KR (420 KB)
- Portuguese - PT (420 KB)
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Handling Instructions (2659 KB)
References
[1]. Li W, et al. Effect of Chelerythrine Against Endotoxic Shock in Mice and Its Modulation of Inflammatory Mediators in Peritoneal Macrophages Through the Modulation of Mitogen-Activated Protein Kinase (MAPK) Pathway. Inflammation. 2012 Jul 24. [Content Brief]
[2]. Pencikova K, et al. Investigation of sanguinarine and chelerythrine effects on LPS-induced inflammatory gene expression in THP-1 cell line. Phytomedicine. 2012 Jul 15;19(10):890-5. Epub 2012 May 14. [Content Brief]
[3]. Chen XM, et al. Chelerythrine chloride induces apoptosis in renal cancer HEK-293 and SW-839 cell lines. Oncol Lett. 2016 Jun;11(6):3917-3924 [Content Brief]
[4]. Herbert JM, et al. Chelerythrine is a potent and specific inhibitor of protein kinase C. Biochem Biophys Res Commun. 1990 Nov 15;172(3):993-9. [Content Brief]
[5]. Chan SL, et al.Identification of chelerythrine as an inhibitor of BclXL function.J Biol Chem. 2003 Jun 6;278(23):20453-6. [Content Brief]
[6]. Tang ZH, et al.Induction of reactive oxygen species-stimulated distinctive autophagy by chelerythrine in non-small cell lung cancer cells.Redox Biol. 2017 Aug;12:367-376. [Content Brief]
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6054 mL | 13.0269 mL | 26.0539 mL | 65.1347 mL |
| 5 mM | 0.5211 mL | 2.6054 mL | 5.2108 mL | 13.0269 mL | |
| 10 mM | 0.2605 mL | 1.3027 mL | 2.6054 mL | 6.5135 mL |
Chelerythrine chloride Related Classifications
HY-12048 Related Classifications
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