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Purity: ≥98%
Chelerythrine chloride (NSC-36405; NSC36405), a benzophenanthridine alkaloid extracted from the plant Greater celandine (Chelidonium majus), is a potent, cell-permeable, selective protein kinase C inhibitor with an IC50 of 660 nM.
| ln Vitro |
Chelerythrine displaces the BH3-containing protein Bax from BclXL and inhibits the BclXL-Bak BH3 peptide binding with an IC50 of 1.5 μM. Loaded cells treated with chelerythrine underwent cell engraftment, which was characterized by mitochondrial involvement [1]. Chelidonine treatment activates and inhibits LPS-induced TNF-α levels and LPS-induced mouse peritoneal giant cells by blocking p38 mitogen protein activator (MAPK) and extracellular signal regulatory protein activator 1 and 2 (ERK1/2). Furthermore, the control of intermediate mediator expression by p38 MAPK and ERK1/2 may account for the effects of chelerythrine on the generation of NO and the cytokine TNF-α [2]. With an LD50 value of 3.46 μM, erythrine is cytotoxic to human monocyte leukocytes. Cells exposed to sanguinarine and chelerythrine dramatically decreased the expression of CCL-2 by 3.5 and 1.9 times, respectively, two hours after LPS stimulation [3]. In a dose-dependent way, chelidonine chloride markedly increased ERK1/2 phosphorylation. Furthermore, p38 phosphorylation can be inhibited by chelerythrine chloride [4].
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| ln Vivo |
Chelerythrine inhibits the production of nitric oxide (NO) and tumor necrosis factor-α (TNF-α) in the serum when exposed to LPS, thereby exhibiting significant anti-inflammatory effects in an in vivo experimentally induced mouse endotoxic shock model [2]. When administered intraperitoneally, chelerythrine chloride (5 mg/kg/day) causes RCC cells to undergo apoptosis without causing considerable harm to mice. P53 accumulates in response to cholerylthrine chloride treatment in a dose-dependent manner [4].
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| 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 |
| Molecular Formula |
C21H18NO4.HCL
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| Molecular Weight |
384.83
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| CAS # |
3895-92-9
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| Related CAS # |
Chelerythrine;34316-15-9
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| SMILES |
[Cl-].O1C([H])([H])OC2=C1C([H])=C1C(=C2[H])C([H])=C([H])C2=C3C([H])=C([H])C(=C(C3=C([H])[N+](C([H])([H])[H])=C21)OC([H])([H])[H])OC([H])([H])[H]
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| Chemical Name |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.44 mg/mL (1.15 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 4.4 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 0.44 mg/mL (1.15 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 4.4 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: ≥ 0.43 mg/mL (1.12 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5986 mL | 12.9928 mL | 25.9855 mL | |
| 5 mM | 0.5197 mL | 2.5986 mL | 5.1971 mL | |
| 10 mM | 0.2599 mL | 1.2993 mL | 2.5986 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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