2. Anti-infection Epigenetics TGF-beta/Smad Apoptosis Autophagy
  3. Beta-lactamase PKC Bcl-2 Family Apoptosis Autophagy
  4. Chelerythrine

Chelerythrine is a natural alkaloid, acts as a potent and selective Ca2+/phospholopid-dependent PKC antagonist, with an IC50 of 0.7 μM. Chelerythrine has antitumor, antidiabetic and anti-inflammatory activity. Chelerythrine inhibits the BclXL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaces Bax from BclXL. Chelerythrine triggers apoptosis and autophagy.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Chelerythrine chloride) usually boasts enhanced water solubility and stability.

For research use only. We do not sell to patients.

Chelerythrine Chemical Structure

Chelerythrine Chemical Structure

CAS No. : 34316-15-9

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Chelerythrine Related Antibodies

Top Publications Citing Use of Products

    Chelerythrine 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.

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    Metallo-β-lactamase

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    PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKC-ι ℩ PKCι

    View All Bcl-2 Family Isoform Specific Products:

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    Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

    • Biological Activity

    • Purity & Documentation

    • References

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    Description

    Chelerythrine is a natural alkaloid, acts as a potent and selective Ca2+/phospholopid-dependent PKC antagonist, with an IC50 of 0.7 μM[1]. Chelerythrine has antitumor, antidiabetic and anti-inflammatory activity[2]. Chelerythrine inhibits the BclXL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaces Bax from BclXL. Chelerythrine triggers apoptosis and autophagy[3][4].

    IC50 & Target[1]

    PKC

    0.7 μM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    A549 IC50
    7.73 μM
    Compound: Chelerythrine
    Cytotoxicity against human A549 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    Cytotoxicity against human A549 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    		[PMID: 27561984]
    HUVEC IC50
    4.93 μM
    Compound: Chelerythrine
    Cytotoxicity against HUVEC assessed as reduction in cell viability after 24 hrs by MTT assay
    Cytotoxicity against HUVEC assessed as reduction in cell viability after 24 hrs by MTT assay
    		[PMID: 27561984]
    MKN-45 IC50
    12.7 μM
    Compound: Chelerythrine
    Cytotoxicity against human MKN45 cells assessed as decrease in cell viability after 48 hrs by MTT assay
    Cytotoxicity against human MKN45 cells assessed as decrease in cell viability after 48 hrs by MTT assay
    		[PMID: 27887841]
    NB-4 IC50
    1.49 μM
    Compound: Chelerythrine
    Cytotoxicity against human NB4 cells assessed as decrease in cell viability after 48 hrs by MTT assay
    Cytotoxicity against human NB4 cells assessed as decrease in cell viability after 48 hrs by MTT assay
    		[PMID: 27887841]
    NCI-H1299 IC50
    4.28 μM
    Compound: Chelerythrine
    Cytotoxicity against human NCI-H1299 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    Cytotoxicity against human NCI-H1299 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    		[PMID: 27561984]
    NCI-H292 IC50
    4.96 μM
    Compound: Chelerythrine
    Cytotoxicity against human NCI-H292 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    Cytotoxicity against human NCI-H292 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    		[PMID: 27561984]
    NCI-H460 IC50
    5.14 μM
    Compound: Chelerythrine
    Cytotoxicity against human NCI-H460 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    Cytotoxicity against human NCI-H460 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    		[PMID: 27561984]
    In Vitro

    Chelerythrine (48 h) inhibits the growth of L-1210 cells (IC50: 0.53 uM )[1].
    Chelerythrine (0-20 μM, 24 h) inhibits cell viability, induces apoptosis and autophagy in A549 and NCI-H1299 cells[4].
    Chelerythrine (0-5 μM, 24 or 48 h) induces apoptosis in BclXL-overexpressing SH-SY5Y cells[3].
    Chelerythrine (2.5-10 μM, 16 h) induces mitochondrial depolarization (decrease in mitochondrial potential) in SH-SY5Y cells, and stimulates release of CytC from isolated mitochondria[4].
    Chelerythrine (0-100 ng/mL, 24 h) reduces the LPS induced production of NO and TNF-α in primary macrophages[5].
    Chelerythrine (MIC: 0.156 mg/mL) shows antibacterial activities against Gram-positive bacteria, Staphylococcus aureus (SA), MRSA, and extended spectrum β-lactamase S. aureus (ESBLs-SA)[6].

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

    Chelerythrine Related Antibodies

    Western Blot Analysis[4]

    Cell Line: A549 and NCI-H1299 cells
    Concentration: 10, 15, 20 μM
    Incubation Time: 24 h
    Result: Induced expression of LC3-II in a beclin 1-dependent way.
    In Vivo

    Chelerythrine (5 mg/kg, i.p., daily) attenuates partial unilateral ureteral obstruction (UUO) induced kidney injury, and restores renal function in neonatal rats[2].
    Chelerythrine (1-10 mg/kg, i.p., at 24 and 1 h before injection of 100 μg/kg LPS) shows anti-inflammatory effects (increased survival rate, decreased serum nitrite and TNF-α level) in LPS induced mice endotoxic shock model[5].

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

    Animal Model: Unilateral ureteral obstruction (UUO) induced neonatal rats[2]
    Dosage: 5 mg/kg
    Administration: i.p., daily
    Result: Attenuated kidney injury (Increased kidney weight and restored renal function).
    Inhibited UUO-induced upregulated kidney injury molecule-1 expression, apoptosis, and renal fibrosis.
    Molecular Weight

    348.37

    Formula

    C21H18NO4
    CAS No.
    SMILES

    C[N+]1=CC2=C(OC)C(OC)=CC=C2C(C=CC3=C4)=C1C3=CC5=C4OCO5
    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.
    Purity & Documentation
    References
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    Chelerythrine Related Classifications

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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Chelerythrine34316-15-9Beta-lactamasePKCBcl-2 FamilyApoptosisAutophagyβ-lactamaseProtein kinase CNSCLCantitumorantidiabeticanti-inflammatoryendotoxic shockA549NCI-H1299Inhibitorinhibitorinhibit

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