Mepazine HCl | MALT1 protease inhibitor

CAS:
 2975-36-2
Catalog Number:
 10-4059
Mepazine chemical structure

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Mepazine (2975-36-2) was originally used clinically as a tranquilizer and antipsychotic medication.  It has more recently been identified as a potent (IC50 = 830 nM) MALT1 protease inhibitor.1 It inhibited anti-apoptotic NF-kB signaling and decreased IL-2 production in diffuse large B cell lymphoma leading to apoptosis both in vitro and in vivo. Mepazine reduced proliferation and increased apoptosis in pancreatic ductal adenocarcinoma cells.2 It was also able to reverse epithelial-to-mesenchymal transition in TNBC leading to reduced metastatic disease.3 Mepazine also prevented the development of DSS-induced experimental colitis via inhibition of NF-kB and NLRP3 inflammasome activation.4 It also alleviated cytokine storm in a mouse model of acute T-cell activation.5

References/Citations:

  1. Nagel et al. (2012) Pharmacological Inhibition of MALT1 Protease by Phenothiazines as a Therapeutic Approach for the Treatment of Aggressive ABC-DLBCL; Cancer Cell 22 P825
  2. Konczalla et al. (2020) Biperiden and mepazine effectively inhibit MALT1 activity and tumor growth in pancreatic cancer; Int.  J. Cancer 146 1618
  3. Lee et al. (2022) MALT1 is a Targetable Driver of Epithelial-to-Mesenchymal Transition in Claudin-Low, Triple-Negative Breast Cancer; Mol.  Cancer Res. 20 373
  4. Liu et al. (2016) MALT1 inhibitors prevent the development of DSS-induced experimental colitis in mice via inhibiting NF-kappaB and NLRP3 inflammasome activation; Oncotarget 7 30536
  5. Dumont et al. (2020) A AMLT1 inhibitor suppresses human myeloid DC, effector T-cell and B-cell responses and retains Th1/regulatory T-cell homeostasis; PLoS One 15 e0222548
2975-36-2, 60-89-9, MALT1 inhibitor, MALT1 protease inhibitor, Mepazine HCL supplier, Mepazine hydrochloride supplier, Mepazine supplier
CAS:
2975-36-2
Catalog Number:
10-4059
Activity:
MALT1 protease inhibitor
Chemical Names:
10-[(1-Methylpiperidin-3-yl)methyl]phenothiazine hydrochloride
Alternate Name:
Pecazine hydrochloride
Molecular Weight:
346.92
Molecular Formula:

C19H22N2S·HCl

Solubility:
Soluble in DMSO (50 mg/ml); water (2 mg/ml)
Physical Properties:
Off-white solid
Purity:

>98% HPLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for up to 2 years when stored as supplied @ -20°C. Solutions in DMSO or water may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

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Mepazine (2975-36-2) was originally used clinically as a tranquilizer and antipsychotic medication.  It has more recently been identified as a potent (IC50 = 830 nM) MALT1 protease inhibitor.1 It inhibited anti-apoptotic NF-kB signaling and decreased IL-2 production in diffuse large B cell lymphoma leading to apoptosis both in vitro and in vivo. Mepazine reduced proliferation and increased apoptosis in pancreatic ductal adenocarcinoma cells.2 It was also able to reverse epithelial-to-mesenchymal transition in TNBC leading to reduced metastatic disease.3 Mepazine also prevented the development of DSS-induced experimental colitis via inhibition of NF-kB and NLRP3 inflammasome activation.4 It also alleviated cytokine storm in a mouse model of acute T-cell activation.5

References/Citations:

  1. Nagel et al. (2012) Pharmacological Inhibition of MALT1 Protease by Phenothiazines as a Therapeutic Approach for the Treatment of Aggressive ABC-DLBCL; Cancer Cell 22 P825
  2. Konczalla et al. (2020) Biperiden and mepazine effectively inhibit MALT1 activity and tumor growth in pancreatic cancer; Int.  J. Cancer 146 1618
  3. Lee et al. (2022) MALT1 is a Targetable Driver of Epithelial-to-Mesenchymal Transition in Claudin-Low, Triple-Negative Breast Cancer; Mol.  Cancer Res. 20 373
  4. Liu et al. (2016) MALT1 inhibitors prevent the development of DSS-induced experimental colitis in mice via inhibiting NF-kappaB and NLRP3 inflammasome activation; Oncotarget 7 30536
  5. Dumont et al. (2020) A AMLT1 inhibitor suppresses human myeloid DC, effector T-cell and B-cell responses and retains Th1/regulatory T-cell homeostasis; PLoS One 15 e0222548

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