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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
Antipsychotic with (sub-) nanomolar affinity for dopamine and α-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 resp.).
Recently, Thioridazine was found to inhibit full length recombinant MALT1 (IC50 3.43 μM). It inhibits anti-apoptotic NF-κB signaling and elicits toxic effects selectively on MALT1-dependent ABC-DLBCL cells. Additionally, it suppresses tumor growth activity by targeting the PI3K/Akt/mTOR/p70S6K signaling pathway.
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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