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

It is advisable to consider the salt form (Chelerythrine chloride) that retains the same biological activity.

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CAS No. : 34316-15-9

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Top Publications Citing Use of Products

    Chelerythrine purchased from MedChemExpress. Usage Cited in: Nutrients. 2025 Nov 12;17(22):3534.  [Abstract]

    The PKC protein expression in the Chelerythrine (0-8μM)-treated groups gradually decreased with increasing dose.

    Chelerythrine purchased from MedChemExpress. Usage Cited in: J Inflamm Res. 2025 Mar 20:18:4213-4231.  [Abstract]

    CLT (Chelerythrine chloride, 5 and 8 μM) downregulated the expression of FLI1 in HEL cells, as determined via Western blotting.

    Chelerythrine purchased from MedChemExpress. Usage Cited in: J Inflamm Res. 2025 Mar 20:18:4213-4231.  [Abstract]

    The effect of Chelerythrine (CLT, 5 and 8 μM) on FLI1 downregulation was significantly diminished in the scrambled control cells versus FLI1 knockdown HEL cells.

    Chelerythrine purchased from MedChemExpress. Usage Cited in: J Inflamm Res. 2025 Mar 20:18:4213-4231.  [Abstract]

    IMQ administration. Images in the top showed significant attenuation in IMQ-induced psoriasis following CLT (Chelerythrine chloride, 4 mg/kg) treatment. H&E staining analysis of the dorsal skin of the IMQ group on day 7 revealed significant epidermal hyperplasia, increased acanthosis, parakeratosis, telangiectasia, and inflammatory cell infiltration. CLT injection significantly reversed these histological changes caused by IMQ, showing less parakeratosis and less epidermal thickening than the IMQ group.

    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.
    • Biological Activity

    • 순도&문서

    • References

    • 고객리뷰

    제품 설명

    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
    A2780/Taxol IC50
    0.4 μM
    Compound: 5
    Antiproliferative activity against human A2780T cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
    Antiproliferative activity against human A2780T cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
    [PMID: 39213483]
    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]
    A549/TR IC50
    0.4 μM
    Compound: 5
    Antiproliferative activity against human A549/Taxol cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
    Antiproliferative activity against human A549/Taxol cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
    [PMID: 39213483]
    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]
    LoVo IC50
    0.4 μM
    Compound: 5
    Antiproliferative activity against human LoVo cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
    Antiproliferative activity against human LoVo cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
    [PMID: 39213483]
    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]
    PC-3 IC50
    0.4 μM
    Compound: 5
    Antiproliferative activity against human PC-3 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
    Antiproliferative activity against human PC-3 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
    [PMID: 39213483]
    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.

    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.
    분자량

    348.37

    화학식

    C21H18NO4

    CAS No.
    SMILES

    C[N+]1=CC2=C(OC)C(OC)=CC=C2C(C=CC3=C4)=C1C3=CC5=C4OCO5

    Structure Classification
    Initial Source
    선적

    Room temperature in continental US; may vary elsewhere.

    보관

    Please store the product under the recommended conditions in the Certificate of Analysis.

    순도&문서
    References
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    상품명:
    Chelerythrine
    Cat. No.:
    HY-N2359
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