Mepazine hydrochloride

SKU: orb1909004

Description

Mepazine hydrochloride (Pecazine hydrochloride) is a potent and selective MALT1 protease inhibitor. It demonstrates anticancer activity by suppressing RANKL-induced osteoclastogenesis in vitro and inhibiting tumor growth in models of pancreatic cancer in vivo.

Research Area

Cell Biology, Immunology & Inflammation

Key Properties

• CAS Number: 2975-36-2
• MW: 346.92
• Purity: 99.91% (May vary between batches)
• Formula: C₁₉H₂₃ClN₂S
• SMILES: Cl.S1C=2C=CC=CC2N(C=3C=CC=CC13)CC4CN(C)CCC4
• Target: MALT,Apoptosis
• Solubility: DMSO:40 mg/mL (115.3 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.77 mM);H2O:1 mg/mL (2.88 mM)

Bioactivity

• Target IC50:
  GSTMALT1 FL:0.83 μM|GSTMALT1 325-760:0.42 μM
• In Vivo:
  Mepazine hydrochloride and thioridazine could also exert effects on lymphoma growth in vivo in a murine DLBCL xenogeneic tumor model. Starting 1 day after injection, the mice were treated by intraperitoneal (i.p.) administration of solvent or either Mepazine hydrochloride (16 mg/kg) or thioridazine (12 mg/kg). In control-treated mice, massive tumors grew from both DLBCL cell lines within 3 weeks of transplantation. Daily administration of Mepazine hydrochloride or thioridazine strongly impaired the expansion of the ABC-DLBCL cell line OCI-Ly10. Mepazine hydrochloride and thioridazine strongly reduced the progression of OCI-Ly10 tumors while having no effect on the growth of Su-DHL-6 tumors in this setting.
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• In Vitro:
  Mepazine hydrochloride was most effective in inhibiting GSTMALT1 FL and GSTMALT1 325-760 with IC50 values of 0.83 and 0.42 μM. Mepazine hydrochloride had the strongest effects and MALT1 activity was reduced by at least 75% in all ABC-DLBCL cells at 10 μM. Mepazine hydrochloride and thioridazine treatment led to a significant decrease of IL-2 secretion in PBMCs.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

MALT1, Pecazine hydrochloride

Compound Identifiers

PubChem CID

102907