Chelerythrine chloride

Cat. No.: HY-12048 Purity: 98.86%: FAQs
Data Sheet SDS COA Handling Instructions

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.

Chelerythrine chloride Chemical Structure

CAS No. : 3895-92-9

Size	Price	Stock	Quantity
Solution
10 mM * 1 mL in DMSO	USD 87	In-stock	Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL ready for reconstitution	USD 87	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 79	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 119	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 396	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 726	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 12 publication(s) in Google Scholar

Other Forms of Chelerythrine chloride:

Chelerythrine Get quote

11 Publications Citing Use of MCE Chelerythrine chloride

: Chelerythrine chloride purchased from MCE. 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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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[5]

PKC

660 nM (IC₅₀)

PKA

0.17 mM (IC₅₀)

TPK

0.1 mM (IC₅₀)

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].

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].

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

Molecular Weight

383.82

Appearance

Solid

Formula

C₂₁H₁₈ClNO₄

CAS No.

3895-92-9

SMILES

C[N+]1=CC2=C(C(OC)=CC=C2C3=C1C4=CC5=C(OCO5)C=C4C=C3)OC.[Cl-]

Structure Classification

Initial Source

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility

In Vitro:

DMSO : 4.35 mg/mL (11.33 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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.

In Vivo:

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
2.

Add each solvent one by one: 10% DMSO 90% corn oil
Solubility: ≥ 0.44 mg/mL (1.15 mM); Clear solution
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

*All of the co-solvents are available by MCE.

Purity & Documentation

Purity: 98.86%

Select Batch:

Data Sheet (282 KB) SDS (421 KB)

COA (251 KB) LCMS (265 KB)

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]

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