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Chelerythrine Chloride (Synonyms: Broussonpapyrine chloride, NSC 646662)

Katalog-Nr.GC13065

Potent inhibitor of PKC and Bcl-xL

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Chelerythrine Chloride Chemische Struktur

Cas No.: 3895-92-9

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10mM (in 1mL DMSO)
78,00 $
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5mg
43,00 $
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10mg
69,00 $
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50mg
238,00 $
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100mg
380,00 $
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment:

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).

Animal experiment:

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.

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.
[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.
[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
[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.
[5]. Chan SL, et al.Identification of chelerythrine as an inhibitor of BclXL function.J Biol Chem. 2003 Jun 6;278(23):20453-6.
[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.

Background

Chelerythrine is a potent, selective antagonist of PKC (protein kinase C) with IC50 value of 0.66 μM.[1]

The alkaloid chelerythrine is a highly specific inhibitor that acts at the regulatory domain of the kinase.[2] It is also a competitive inhibitor with respect to the phosphate acceptor and a non-competitive inhibitor with respect to ATP.[1] Chelerythrine induced a dose-dependent decrease in the cell viability with IC50 value of 2.6 μM measured by MTT reduction assay.[3] Chelerythrine is also a selective and strong inhibitor of Bcl-xL functions and induced cell death in MEF cells with IC50 value of 1.1 μM.[4] Chelerythrine activated MEKK1- and MKK4-dependent JNK1 and p38 pathways then mediated the induction of apoptosis.[5] Chelerythrine stimulated apoptosis in the in vivo rat experiments (5 mg/kg) by inducing the generation of reactive oxygen species.[6] Chelerythrine also has widespread physiological effects on primarily antimicrobial and anti-inflammatory.

References:
1. J. M. Herbert, J. M. Augereau, J. Gleye and J. P. Maffrand, Biochem Biophys Res Commun 1990, 172, 993-999.
2. W. D. Jarvis, A. J. Turner, L. F. Povirk, R. S. Traylor and S. Grant, Cancer Res 1994, 54, 1707-1714.
3. J. Vrba, P. Dolezel, J. Vicar, M. Modriansky and J. Ulrichova, Toxicol In Vitro 2008, 22, 1008-1017.
4. M. Vogler, K. Weber, D. Dinsdale, I. Schmitz, K. Schulze-Osthoff, M. J. Dyer and G. M. Cohen, Cell Death Differ 2009, 16, 1030-1039.
5. R. Yu, S. Mandlekar, T. H. Tan and A. N. Kong, J Biol Chem 2000, 275, 9612-9619.
6. S. Yamamoto, K. Seta, C. Morisco, S. F. Vatner and J. Sadoshima, J Mol Cell Cardiol 2001, 33, 1829-1848.

Chemical Properties

Cas No. 3895-92-9 SDF
Überlieferungen Broussonpapyrine chloride, NSC 646662
Chemical Name 1,2-dimethoxy-12-methyl-[1,3]benzodioxolo[5,6-c]phenanthridin-12-ium
Canonical SMILES C[N+]1=C2C(=C3C=CC(=C(C3=C1)OC)OC)C=CC4=CC5=C(C=C42)OCO5.[Cl-]
Formula C21H18ClNO4 M.Wt 383.83
Löslichkeit ≥ 19.2 mg/mL in DMSO, ≥ 9.45 mg/mL in EtOH with ultrasonic and warming Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.6053 mL 13.0266 mL 26.0532 mL
5 mM 0.5211 mL 2.6053 mL 5.2106 mL
10 mM 0.2605 mL 1.3027 mL 2.6053 mL
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