1. GPCR/G Protein Neuronal Signaling Metabolic Enzyme/Protease Autophagy
  2. Dopamine Receptor Cytochrome P450 Autophagy 5-HT Receptor
  3. Chlorpromazine

Chlorpromazine is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine also can inhibit clathrin-mediated endocytosis.

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CAS 番号 : 50-53-3

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カスタマーレビュー

Based on 128 publication(s) in Google Scholar

Other Forms of Chlorpromazine:

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顧客検証

Flow Cytometry
IF

    Chlorpromazine purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2025 Oct 21;10(1):349.  [Abstract]

    Analysis of the cellular uptake pathways of OVA PCD. Ethamilamiline (EIPA), genistein (GEN), and chlorpromazine (CPZ) (10 μM for 12 h)were used to inhibit macropinocytosis, caveolin-mediated endocytosis, and clathrin-mediated endocytosis, respectively.

    Chlorpromazine purchased from MedChemExpress. Usage Cited in: Adv Mater. 2025 Jan 10:e2415030.  [Abstract]

    FCM analysis of F/G/H‐GNC internalization by 4T1 cells pre‐treated with various endocytosis inhibitors (n = 3). EIPA: 5‐(N‐ethyl‐N‐isopropyl)‐amiloride, 50 µM; Dyna: dynasore, 50 µg/mL; Me‐β‐CD: methyl‐β‐cyclodextrin, 2.5 mg/mL; CPZ: Chlorpromazine, 10 µg/mL; Cyto D: Cytochalasin D, 2.5 µg/mL; Noco: Nocodazole, 5 µM.

    Chlorpromazine purchased from MedChemExpress. Usage Cited in: Cell Metab. 2024 Jun 18:S1550-4131(24)00189-X.  [Abstract]

    To clarify the possible pathways responsible for EV uptake by CAFs, BMDM-derived EVs were labeled with DiO, and m-CAFs were labeled with DiL. Chlorpromazine (50 μM, 1h) was used to block EV uptake by m-CAFs.

    Chlorpromazine purchased from MedChemExpress. Usage Cited in: Cell Metab. 2022 Dec 6;34(12):2018-2035.e8.  [Abstract]

    Bone marrow cells cultured in medium containing 10 ng/mL GM-CSF for 3 days were treated with 2 μg PKH67-labeled sEVs with or without Amiloride (10 μM), Chlorpromazine (10 μM), or EIPA (5 μM) for 1 h. The median fluorescence intensity (MFI) of PKH67 was assessed by flow cytometry.

    Chlorpromazine purchased from MedChemExpress. Usage Cited in: Commun Biol. 2022 Nov 14;5(1):1248.  [Abstract]

    Chlorpromazine (CPZ) (10 µM; 30 min) remarkably decreases the cellular internalization of FITC-P-LPK in HCT116 cells. Chlorpromazine can inhibit clathrin-mediated endocytosis. The fluorescence intensity is observed by confocal microscopy and detected using a multi-well plate reader.
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    • 参考文献

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    製品説明

    Chlorpromazine is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine also can inhibit clathrin-mediated endocytosis[1][2][3][4][5].

    IC50 & Target

    5-HT2A Receptor

     

    Cellular Effect
    Cell Line Type Value Description References
    CHO IC50
    3.4 μM
    Compound: chlorpromazine
    Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
    Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
    [PMID: 23812503]
    CHO-K1 IC50
    1 nM
    Compound: Chlorpromazine
    Antagonist activity against human recombinant dopmaine D2L receptor expressed in CHOK1 cells assessed as reduction in apomorphine-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method
    Antagonist activity against human recombinant dopmaine D2L receptor expressed in CHOK1 cells assessed as reduction in apomorphine-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method
    [PMID: 25557493]
    CHO-K1 IC50
    1 nM
    Compound: Chlorpromazine
    Antagonist activity at human dopamine D2 receptor expressed in CHOK1 cells assessed as inhibition of apomorphine-induced calcium mobilization by radiometric and luminescence plate counting method
    Antagonist activity at human dopamine D2 receptor expressed in CHOK1 cells assessed as inhibition of apomorphine-induced calcium mobilization by radiometric and luminescence plate counting method
    [PMID: 25557493]
    Cortical neurone IC50
    13.8 μM
    Compound: Chlorpromazine
    Neurotoxicity in rat cortical neuron assessed as inhibition of neurite total length per neuron incubated for 72 hrs by Hoechst 33342 staining based ArrayScan analysis
    Neurotoxicity in rat cortical neuron assessed as inhibition of neurite total length per neuron incubated for 72 hrs by Hoechst 33342 staining based ArrayScan analysis
    [PMID: 31841637]
    Cortical neurone IC50
    7.99 μM
    Compound: Chlorpromazine
    Neurotoxicity in rat cortical neuron assessed as inhibition of valid neuron count incubated for 72 hrs by Hoechst 33342 staining based ArrayScan analysis
    Neurotoxicity in rat cortical neuron assessed as inhibition of valid neuron count incubated for 72 hrs by Hoechst 33342 staining based ArrayScan analysis
    [PMID: 31841637]
    Cortical neurone IC50
    9.022 μM
    Compound: Chlorpromazine
    Neurotoxicity in rat cortical neuron assessed as inhibition of neurite outgrowth by measuring mean neurite average length incubated for 72 hrs by Hoechst 33342 staining based ArrayScan analysis
    Neurotoxicity in rat cortical neuron assessed as inhibition of neurite outgrowth by measuring mean neurite average length incubated for 72 hrs by Hoechst 33342 staining based ArrayScan analysis
    [PMID: 31841637]
    HEK293 IC50
    27 μM
    Compound: chlorpromazine
    Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
    Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
    [PMID: 18788725]
    HaCaT IC50
    36.1 μM
    Compound: CPZ
    Phototoxicity in human HaCaT cells assessed as reduction in cell viability preincubated for 60 mins followed by 7.5 J/cm2 UVA irradiation and measured after 24 hrs by neutral red uptake assay
    Phototoxicity in human HaCaT cells assessed as reduction in cell viability preincubated for 60 mins followed by 7.5 J/cm2 UVA irradiation and measured after 24 hrs by neutral red uptake assay
    [PMID: 29604584]
    HeLa IC50
    4.3 μM
    Compound: Chlorpromazine
    TP_TRANSPORTER: inhibition of TEA uptake in OCT1-expressing HeLa cells
    TP_TRANSPORTER: inhibition of TEA uptake in OCT1-expressing HeLa cells
    [PMID: 12606755]
    Macrophage cell line CC50
    22.24 μM
    Compound: CPZ
    Cytotoxicity in human monocyte-derived macrophages assessed as reduction in cell viability incubated for 3 days by alamar blue dye based assay
    Cytotoxicity in human monocyte-derived macrophages assessed as reduction in cell viability incubated for 3 days by alamar blue dye based assay
    [PMID: 28964936]
    NCI-H1650 GI50
    30.3 μM
    Compound: Chlorpromazine
    Cytotoxicity against human NCI-H1650 cells assessed as growth inhibition after 48 hrs by MTT assay
    Cytotoxicity against human NCI-H1650 cells assessed as growth inhibition after 48 hrs by MTT assay
    [PMID: 26372073]
    NHDF IC50
    25.5 μM
    Compound: CPZ
    Phototoxicity in human NHDF cells assessed as reduction in cell viability preincubated for 60 mins followed by 5 J/cm2 UVA irradiation and measured after 24 hrs by neutral red uptake assay
    Phototoxicity in human NHDF cells assessed as reduction in cell viability preincubated for 60 mins followed by 5 J/cm2 UVA irradiation and measured after 24 hrs by neutral red uptake assay
    [PMID: 29604584]
    NIH3T3 IC50
    0.93 μg/mL
    Compound: Chlorpromazine
    Phototoxicity against BALB/c mouse 3T3 cells assessed as reduction in cell viability preincubated for 1 hr followed by 5 J/cm2 irradiation and subsequent replacement of medium without compound and measured after 24 hrs by neutral red dye based assay
    Phototoxicity against BALB/c mouse 3T3 cells assessed as reduction in cell viability preincubated for 1 hr followed by 5 J/cm2 irradiation and subsequent replacement of medium without compound and measured after 24 hrs by neutral red dye based assay
    [PMID: 38128906]
    NIH3T3 IC50
    45.08 μg/mL
    Compound: Chlorpromazine
    Dark toxicity against BALB/c mouse 3T3 cells assessed as reduction in cell viability incubated for 1 hr by neutral red dye based assay
    Dark toxicity against BALB/c mouse 3T3 cells assessed as reduction in cell viability incubated for 1 hr by neutral red dye based assay
    [PMID: 38128906]
    ScN2a EC50
    2 μM
    Compound: Chlorpromazine
    Half maximal inhibition of Prion protein PrPsc formation was assayed in ScN2a cells
    Half maximal inhibition of Prion protein PrPsc formation was assayed in ScN2a cells
    [PMID: 12904059]
    Sf21 IC50
    122.3 μM
    Compound: Chlorpromazine
    Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
    Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
    [PMID: 21965623]
    Sf21 IC50
    147.6 μM
    Compound: Chlorpromazine
    Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
    Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
    [PMID: 21965623]
    Vero IC50
    26.52 μg/mL
    Compound: CPZ
    Cytotoxicity against African green monkey Vero cells assessed as decrease in cell viability incubated for 72 hrs by resazurin assay
    Cytotoxicity against African green monkey Vero cells assessed as decrease in cell viability incubated for 72 hrs by resazurin assay
    [PMID: 32526553]
    WI-38 CC50
    10.34 μM
    Compound: Chlorpromazine
    Cytotoxicity against human WI38 cells assessed as reduction in cellular DNA level preincubated for 2 hrs before viral infection measured after 7 days by real time PCR assay
    Cytotoxicity against human WI38 cells assessed as reduction in cellular DNA level preincubated for 2 hrs before viral infection measured after 7 days by real time PCR assay
    [PMID: 17893158]
    WI-38 EC50
    7.6 μM
    Compound: Chlorpromazine
    Antiviral activity against BKV Gardner ATCC VR837 infected in human WI38 cells assessed as reduction in viral DNA level preincubated for 2 hrs before viral infection measured after 7 days by real time PCR assay
    Antiviral activity against BKV Gardner ATCC VR837 infected in human WI38 cells assessed as reduction in viral DNA level preincubated for 2 hrs before viral infection measured after 7 days by real time PCR assay
    [PMID: 17893158]
    体外実験

    Chlorpromazine (0, 10, 20, 40 μM; 0, 24, 48 h) inhibits growth of U-87MG glioma cells in a dose- and time- dependent manner[2].
    Chlorpromazine (20 μM; 0, 12, 24, 48 h) decreases the levels of cyclin A and cyclin B1 in U-87MG glioma cells, 12 h later[2].
    Chlorpromazine (20 μM) causes inhibition of cell cycle progression[2].
    Chlorpromazine (10 μM; 1 h) significantly suppresses the sEV internalization and dramatically reduces MDSCs in sEV-treated bone marrow cells (MDSCs can significantly suppress the immune cell response, causing immunosuppression in cancer cells)[3].
    Chlorpromazine (3, 10, 20, 40, 60 μM) blocks the hNav1.7 current in a concentration-dependent manner[4].
    Chlorpromazine blocks HERG potassium channels with an IC50 value of 21.6 μM and a Hill coefficient of 1.11[5].

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

    Cell Proliferation Assay[2]

    Cell Line: U-87MG glioma cells
    Concentration: 0, 10, 20, 40 μM
    Incubation Time: 0, 24, 48 h
    Result: Showed anti-proliferative activity in a dose- and time-dependent manner.

    Immunofluorescence[3]

    Cell Line: Bone marrow cells (sEV-treated)
    Concentration: 10 µM
    Incubation Time: 1 h
    Result: Reduced MDSCs and suppressed the sEV internalization.

    Western Blot Analysis[2]

    Cell Line: U-87MG glioma cells
    Concentration: 20 μM
    Incubation Time: 0, 12, 24, 48 h
    Result: Decreased the levels of cyclin A and cyclin B1 12 h later, whereas levels of cyclin D1, proliferating cell nuclear antigen and GAPDH remained unchanged.
    体内実験

    Chlorpromazine (20 mg/kg; i.p.; single daily for 7 days) inhibits xenograft tumor growth in nude mouse[2].

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

    Animal Model: 5- to 6-week-old athymic nude mice bearing intracranial U-87MG xenograft tumors[2].
    Dosage: 20 mg/kg
    Administration: Injected intraperitoneally; single daily for 7 days
    Result: Inhibited tumor growth on day 17.
    分子量

    318.86

    分子式

    C17H19ClN2S

    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CN(C)CCCN1C2=C(C=CC=C2)SC3=CC=C(Cl)C=C13

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件

    4°C, protect from light, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

    溶剤 & 溶解度
    体外: 

    DMSO : 100 mg/mL (313.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.1362 mL 15.6809 mL 31.3617 mL
    5 mM 0.6272 mL 3.1362 mL 6.2723 mL
    10 mM 0.3136 mL 1.5681 mL 3.1362 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
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    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (7.84 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (7.84 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
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    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 99.75%

    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.1362 mL 15.6809 mL 31.3617 mL 78.4043 mL
    5 mM 0.6272 mL 3.1362 mL 6.2723 mL 15.6809 mL
    10 mM 0.3136 mL 1.5681 mL 3.1362 mL 7.8404 mL
    15 mM 0.2091 mL 1.0454 mL 2.0908 mL 5.2270 mL
    20 mM 0.1568 mL 0.7840 mL 1.5681 mL 3.9202 mL
    25 mM 0.1254 mL 0.6272 mL 1.2545 mL 3.1362 mL
    30 mM 0.1045 mL 0.5227 mL 1.0454 mL 2.6135 mL
    40 mM 0.0784 mL 0.3920 mL 0.7840 mL 1.9601 mL
    50 mM 0.0627 mL 0.3136 mL 0.6272 mL 1.5681 mL
    60 mM 0.0523 mL 0.2613 mL 0.5227 mL 1.3067 mL
    80 mM 0.0392 mL 0.1960 mL 0.3920 mL 0.9801 mL
    100 mM 0.0314 mL 0.1568 mL 0.3136 mL 0.7840 mL
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    製品名:
    Chlorpromazine
    製品番号:
    HY-12708
    数量:
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