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Thioridazine hydrochloride
- NSC 186060
- Parent CAS: 50-52-2
- Soluble in water and DMSO
- MF: C21H26N2S2.HCl
- MW: 407.04
Description
Thioridazine hydrochloride is a phenothiazine antipsychotic with high affinity for dopamine D2/D3/D4 and α1-adrenergic receptors (Ki of 0.4 nM, 1.5 nM, 1.5 nM, 3.2 nM, 2.4 nM for D2, D3, D4, α1A, and α1B respectively). It has also been reported to inhibit full-length recombinant MALT1 with IC50 of 3.43 µM and to suppress NF-κB signaling in MALT1-dependent ABC-DLBCL cells. Additionally, it suppresses tumor growth activity by targeting the PI3K/Akt/mTOR/p70S6K signaling pathway.
Thioridazine is pharmacologically relevant across CNS receptor biology and oncology repurposing research. Its multi-target profile enables studies of dopamine receptor antagonism, MALT1-dependent lymphoma survival and PI3K/Akt/mTOR pathway modulation.
Key Features
- Dopamine D2/D3/D4 receptor antagonist
- High affinity for α1-adrenergic receptors
- Reported MALT1 inhibitory activity
- Modulates NF-κB and PI3K/Akt/mTOR-associated survival signaling
Applications
- Antipsychotic receptor pharmacology
- MALT1-dependent lymphoma research
- NF-κB pathway studies
- Multi-target drug repurposing models
More Information
| Parent CAS No. | 50-52-2 |
|---|---|
| Chemical Name | 10-(2-(1-methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine hydrochloride |
| SMILES | C1=C2C(SC3=C(N2CCC2CCCCN2C)C=CC=C3)=CC=C1SC.Cl |
| MFCD | MFCD00012655 |
| InChi | InChI=1S/C21H26N2S2.ClH/c1-22-13-6-5-7-16(22)12-14-23-18-8-3-4-9-20(18)25-21-11-10-17(24-2)15-19(21)23;/h3-4,8-11,15-16H,5-7,12-14H2,1-2H3;1H |
| InChiKey | NZFNXWQNBYZDAQ-UHFFFAOYSA-N |
| CID | 66062 |
| Short Description | MALT1 inhibitor; DA antag. |
References
- D. Nagel et al. Pharmacologic Inhibition of MALT1 Protease by Phenothiazines as a Therapeutic Approach for the Treatment of Aggressive ABC-DLBCL. Canc. Cell 2012, 22, 825–837.
- S. Kang et al. Thioridazine induces apoptosis by targeting the PI3K/Akt/mTOR pathway in cervical and endometrial cancer cells. Apoptosis. 2012, 17, 989–997.
- RM Young & LM Staudt. A New “Brew” of MALT1 Inhibitors. Cancer Cell, 2012, 22(6), 706-707.
- DJ Burgess. Anticancer drugs: Assault on MALT1. Nature Reviews Drug Discovery, 2013, 12(2), 100-101.
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