Bioactivity | Chlorpromazine hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride also can inhibit clathrin-mediated endocytosis[1][2][3][4][5]. |
Target | D2 dopamine receptors; 5-HT2A. |
Invitro | Chlorpromazine hydrochloride (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 hydrochloride (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 hydrochloride (20 μM) causes inhibition of cell cycle progression[2].Chlorpromazine hydrochloride (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 hydrochloride (3, 10, 20, 40, 60 µM) blocks the hNav1.7 current in a concentration-dependent manner[4].Chlorpromazine hydrochloride blocks HERG potassium channels with an IC50 value of 21.6 µM and a Hill coefficient of 1.11[5]. Cell Proliferation Assay[2] Cell Line: |
In Vivo | Chlorpromazine hydrochloride (20 mg/kg; i.p.; single daily for 7 days) inhibits xenograft tumor growth in nude mouse[2]. Animal Model: |
Name | Chlorpromazine hydrochloride |
CAS | 69-09-0 |
Formula | C17H20Cl2N2S |
Molar Mass | 355.33 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, sealed storage, away from moisture and light *该产品在溶液状态不稳定,建议您现用现配,即刻使用。 |
Reference | [1]. Kamgar-Dayhoff P, et al. Multifaceted effect of chlorpromazine in cancer: implications for cancer treatment. Oncotarget. 2021 Jul 6;12(14):1406-1426. [2]. Shin SY, et al. The antipsychotic agent chlorpromazine induces autophagic cell death by inhibiting the Akt/mTOR pathway in human U-87MG glioma cells. Carcinogenesis. 2013 Sep;34(9):2080-9. [3]. Yang Z, et al. Cancer cell-intrinsic XBP1 drives immunosuppressive reprogramming of intratumoral myeloid cells by promoting cholesterol production. Cell Metab. 2022 Nov 2:S1550-4131(22)00461-2. [4]. Lee SJ, et al. Mechanism of inhibition by chlorpromazine of the human pain threshold sodium channel, Nav1.7. Neurosci Lett. 2017 Feb 3;639:1-7. [5]. Thomas D, et al. The antipsychotic drug chlorpromazine inhibits HERG potassium channels. Br J Pharmacol. 2003 Jun;139(3):567-74. [6]. Suzuki H, et al. Comparison of the anti-dopamine D₂ and anti-serotonin 5-HT(2A) activities of chlorpromazine, bromperidol, haloperidol and second-generation antipsychotics parent compounds and metabolites thereof. J Psychopharmacol. 2013 Apr;27(4):396-400. |