Cat. No.: HY-12048

Chelerythrine chloride

19 Cited Publications

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Based on 19 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.

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Pureté: 99.11%
CAS No.: 3895-92-9
Formule: C₂₁H₁₈ClNO₄
Masse moléculaire:383.82

Stockage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Chelerythrine chloride Chemical Structure

CAS No.: 3895-92-9

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (19)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
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Activité biologique

Description

IC₅₀ & Target^[5]

PKC

660 nM (IC₅₀)

PKA

0.17 mM (IC₅₀)

TPK

0.1 mM (IC₅₀)

Voir tous les produits spécifiques à Isoform PKC :

Voir tous les produits spécifiques à Isoform Bcl-2 Family :

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	4.63 μM Compound: chelerythrine	In vitro cytotoxicity for human ovarian tumor A2780 cells In vitro cytotoxicity for human ovarian tumor A2780 cells	[PMID: 15999988]
Astrocyte	EC₅₀	1.531 μM Compound: 36	Antiproliferative activity against mouse astrocyte cells by MTT assay Antiproliferative activity against mouse astrocyte cells by MTT assay	[PMID: 17417631]
HCT-116	IC₅₀	2.13 μM Compound: 1a	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	[PMID: 26026362]
HeLa	IC₅₀	1.24 μg/mL Compound: 5, chelerythrine	Growth inhibition of human HeLa S3 cells after 72 hrs Growth inhibition of human HeLa S3 cells after 72 hrs	[PMID: 10395504]
HL-60	IC₅₀	2.99 μM Compound: 1a	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	[PMID: 26026362]
Panel NCI-60 (60 carcinoma cell lines)	GI₅₀	188 nM Compound: chelerythrine	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	[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.

In Vivo

Chelerythrine displays significant anti-inflammatory?effects in experimentally induced?mice?endotoxic?shock?model in vivo through inhibition of LPS-induced tumor necrosis factor-alpha (TNF-α) level and nitric oxide (NO) production in serum^[2]. Chelerythrine chloride (5 mg/kg/day, i.p.) induces apoptosis of RCC cells without significant toxicity to mice. Chelerythrine Chloride treatment leads to a dose-dependent accumulation of p53^[4].

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

Chemical Information

CAS No. 3895-92-9
Appearance Solid
Masse moléculaire 383.82
Formule C₂₁H₁₈ClNO₄
Color Yellow to orange
SMILES

C[N+]1=CC2=C(C(OC)=CC=C2C3=C1C4=CC5=C(OCO5)C=C4C=C3)OC.[Cl-]
Structure Classification
- Alkaloids
- Isoquinoline Alkaloids
Initial Source
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (19)

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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
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
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
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

Dietary Copper on the Onset of Puberty in Rats: Possible Mechanism. [Abstract]

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.
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
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
J Inflamm Res

FLI1 Induces Plaque Psoriasis and Its Inhibition Attenuates Disease Progression. [Abstract]

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.
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.
Cytokine

Chelerythrine ameliorates Aspergillus fumigatus keratitis through suppressing the LOX-1/p38 MAPK signaling pathway. [Abstract]

2024 Jul 26:182:156717. PMID: 39067394
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
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
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
Fishes

2022, 7(5), 229.
Biochem Biophys Res Commun

Chelerythrine inhibits NR2B NMDA receptor independent of PKC activity. [Abstract]

2024 Oct 29:739:150914. 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
Bull Sib Med

2025.
Research Square Preprint

2020 Oct.

Solvant et solubilité

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)

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

2.6054 mL

13.0269 mL

26.0539 mL

5 mM

0.5211 mL

2.6054 mL

5.2108 mL

10 mM

0.2605 mL

1.3027 mL

2.6054 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 (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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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: ≥ 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.

Protocol 2

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

Solubility: ≥ 0.44 mg/mL (1.15 mM); Clear solution

This protocol yields a clear solution of ≥ 0.44 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 (4.4 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 3

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.

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

Protocole

Cell Assay^[1]

Cell viability is evaluated via MTT assay. Cells (2×10³ HEK-293 cells/well and 3×10³ SW-839 cells/well) in 100 µL medium are seeded into 96-well plates, and incubated for 12 h. Next, the medium in each well is replaced with medium containing various concentrations of Chelerythrine Chloride, and the cells are incubated at 37°C for an additional 24 and 48 h. Subsequently, 20 µL MTT (5 mg/mL) is added to each well. Following an additional incubation at 37°C for 4 h, the supernatant is removed, and 100 µL DMSO is added to each well. The absorbance values (read at 540 nm) are determined using the iMark™ Microplate Absorbance Reader. The data are analyzed using Microplate Manager software (ver. 6.3; 1689520).

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

Animal Administration^[1]

A total of 5×10⁶ SW-839 cells are mixed with Matrigel^®, and injected subcutaneously into the flanks of 14 5-week-old male BALB/c nude mice. The mice are maintained in 18×30-cm cages containing three mice each, at a temperature of 22°C using a 12 h light/dark cycle. Food and water is available ad libitum. The mice are randomLy divided into two groups (n=7). As previously described, the mice are administrated with chelerythrine chloride at a dose of 5 mg/kg/day via intraperitoneal injection for 5 weeks, with the first injection of chelerythrine chlorideurring 24 h after injection with the SW-839 cells. The control mice are administered with the same volume of PBS containing 1% DMSO. The volume and weight of the mouse tumors are measured once a week. All the mice are sacrificed 36 days subsequent to inoculation of the cancer cells, when the tumors are resected.

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (282 KB)
SDS (420 KB)
- English - EN (420 KB)
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- Deutsch - DE (420 KB)
- Norwegian - NO (420 KB)
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- Italian - IT (420 KB)
- Portuguese - PT (420 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)
Instruction de manipulation (2659 KB)

Références

[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]

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	2.6054 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

Keywords

Chelerythrine chloride

19 Cited Publications

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Chelerythrine chloride

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Publications Citing Use of MedChemExpress (MCE) Chelerythrine chloride

Voir tous les produits spécifiques à Isoform PKC

Voir tous les produits spécifiques à Isoform Bcl-2 Family

Activité biologique

Chemical Information

Publications (19)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Chelerythrine chloride Related Classifications

Cat. No.: HY-12048