1. MAPK/ERK Pathway
    TGF-beta/Smad
    Epigenetics
    Autophagy
  2. p38 MAPK
    PKC
    Autophagy

Chelerythrine Chloride 

Cat. No.: HY-12048 Purity: >98.0%
Data Sheet SDS Handling Instructions

Chelerythrine Chloride is a potent, cell-permeable inhibitor of protein kinase C and mitogen-activated protein kinase (MAPK), with IC50 of 660 nM for PKC, competitive with respect to the phosphate acceptor and non-competitive with respect to ATP.

For research use only. We do not sell to patients.
Chelerythrine Chloride Chemical Structure

Chelerythrine Chloride Chemical Structure

CAS No. : 3895-92-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 79 In-stock
5 mg USD 72 In-stock
10 mg USD 108 In-stock
50 mg USD 360 In-stock
100 mg USD 660 In-stock
200 mg   Get quote  
500 mg   Get quote  

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    Chelerythrine Chloride purchased from MCE. Usage Cited in: Sci Rep. 2017 Aug 23;7(1):9201.

    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.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Chelerythrine Chloride is a potent, cell-permeable inhibitor of protein kinase C and mitogen-activated protein kinase (MAPK), with IC50 of 660 nM for PKC, competitive with respect to the phosphate acceptor and non-competitive with respect to ATP.

    IC50 & Target

    IC50: 600 nM (protein kinase C)

    In Vitro

    Chelerythrine inhibits the BclXL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaced 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].

    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].

    References
    Preparing Stock Solutions
    Concentration Volume 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.
    Cell Assay
    [1]

    Chelerythrine is dissolved in DMSO.

    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]

    Chelerythrine chloride is formulated in PBS containing 1% DMSO.

    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
    Molecular Weight

    383.82

    Formula

    C₂₁H₁₈ClNO₄

    CAS No.

    3895-92-9

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 3.9 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: >98.0%

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    Product Name:
    Chelerythrine Chloride
    Cat. No.:
    HY-12048
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