| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
MALT1 (mucosa-associated lymphoid tissue lymphoma translocation protein 1). Pecazine is a potent and selective MALT1 protease inhibitor with IC50 values of 0.83 μM for GSTMALT1 full length and 0.42 μM for GSTMALT1 325-760. MALT1 is a paracaspase that plays a critical role in the NF-κB signaling pathway, particularly in B-cell and T-cell receptor signaling. By inhibiting MALT1, Pecazine may modulate immune responses and inflammation. Pecazine also exhibits dopamine receptor modulation activity and is commonly explored as a neuroactive agent. The compound has been found to exhibit various biological activities, including anti-inflammatory, anti-tumor, and anti-microbial activities. Its mechanism of action involves the inhibition of various enzymes and signaling pathways that are involved in cell proliferation and inflammation. Pecazine is a phenothiazine derivative with central nervous system activity.
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| ln Vitro |
Mepazine (5–20 μM; 4 days) dramatically reduces the viability of activated B-cell subtypes of diffuse large B-cell lymphoma (ABCDLBCL) cells, but has no effect on GCB-DLBCL cells [1].
Pecazine is a potent and selective MALT1 protease inhibitor with IC50 values of 0.83 μM for GSTMALT1 full length and 0.42 μM for GSTMALT1 325-760. The compound has been found to exhibit various biological activities, including anti-inflammatory, anti-tumor, and anti-microbial activities. Pecazine's mechanism of action involves the inhibition of various enzymes and signaling pathways involved in cell proliferation and inflammation. The compound is commonly explored as a neuroactive agent, particularly in studies related to dopamine receptor modulation and psychotropic drug mechanisms. Pecazine's diverse biological activities make it a valuable tool for studying inflammation, cancer, and neurological disorders. |
| ln Vivo |
Using a murine DLBCL xenograft tumor model, mepazine (16 mg/kg; i.p.) inhibits growth and causes apoptosis in the ABC-DLBCL cell line OCI-Ly10 in NOD/scid IL-2Rgnull (NSG) mice. Expanding the ABC-DLBCL cell line OCI-Ly10 is significantly hindered by the daily treatment of mepazine [1].
Pecazine has been studied in vivo for its effects on MALT1-mediated pathways, inflammation, and neurological function. The compound's potent and selective MALT1 inhibition suggests it would be effective in modulating immune responses in vivo. Pecazine's anti-inflammatory, anti-tumor, and anti-microbial activities have been evaluated in preclinical models. The compound is commonly explored as a neuroactive agent in studies related to dopamine receptor modulation and psychotropic drug mechanisms. Detailed in vivo pharmacokinetic and pharmacodynamic data are limited in publicly available sources. Pecazine is a phenothiazine derivative widely utilized in pharmacological and biochemical research. |
| Enzyme Assay |
MALT1 protease activity assays are performed using recombinant MALT1 protein (full length or truncated) and a fluorogenic peptide substrate. The enzyme is incubated with the substrate in assay buffer (50 mM Tris-HCl pH 7.5, 150 mM NaCl, 0.1% Triton X-100, 1 mM DTT) at 37°C for 30-60 minutes. The cleavage of the substrate generates a fluorescent signal measured at appropriate wavelengths. Pecazine is serially diluted in DMSO and added to the reaction mixture. The IC50 for Pecazine is 0.83 μM for GSTMALT1 full length and 0.42 μM for GSTMALT1 325-760. Each concentration is tested in duplicate, and IC50 values are calculated by non-linear regression analysis. Appropriate positive controls (e.g., known MALT1 inhibitors) and vehicle controls are included to validate the assay.
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| Cell Assay |
Cell viability assay [1]
Cell Types: ABC-DLBCL cell line (HBL1, OCI-Ly3, U2932, TMD8, OCI-Ly10) and GCB-DLBCL cell line (BJAB, Su-DHL-6, Su-DHL-4) Tested Concentrations: 5, 10 and 20 μM Incubation Duration: 4 days Experimental Results: Caused a decrease in the viability of HBL1, OCI-Ly3, U2932 and TMD8 cells in ABC-DLBCL cells, but had no significant effect on GCB-DLBCL cells. Cellular MALT1 inhibition is evaluated in immune cell lines (e.g., Jurkat T cells, Raji B cells). Cells are cultured in appropriate media (e.g., RPMI-1640 with 10% FBS) at 37°C with 5% CO₂ and treated with Pecazine at concentrations ranging from 0.1 to 10 μM for 1-24 hours. MALT1 activity in cell lysates is measured using enzymatic assays with fluorogenic substrates. NF-κB activation is assessed by measuring phosphorylation of IκBα or nuclear translocation of NF-κB by Western blotting or immunofluorescence. Cytokine production (e.g., IL-2, IL-6, TNF-α) is measured by ELISA. Cell viability is assessed using MTT or LDH assays. Each experiment includes vehicle controls (DMSO) and appropriate positive controls (e.g., known MALT1 inhibitors). |
| Animal Protocol |
Animal/Disease Models: 6 to 8 weeks old female NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG) mice with murine DLBCL xenogeneic tumor model [1]
Doses: 400 μg per animal (25 g), equivalent to approximately 16 mg/ Kilogram. Mode of Route of Administration: intraperitonealadministration; continuous administration every 24 hrs (hrs (hours)) starting 1 or 12 days after transplantation; Daily administration Experimental Results: Daily administration strongly impaired the expansion of the ABC-DLBCL cell line OCI-Ly10. In vivo studies of Pecazine are conducted in animal models of inflammation, cancer, and neurological disorders. The compound is administered orally or intraperitoneally at doses determined by preclinical studies. Pecazine is formulated in appropriate vehicles (e.g., DMSO/PEG300/Tween 80). Disease progression is monitored by clinical scores, tumor growth, or behavioral assessments. Tissue samples are collected for histopathological analysis and biochemical assays (MALT1 activity, NF-κB activation, cytokine levels). Sample sizes typically range from 6-10 animals per group. |
| ADME/Pharmacokinetics |
Molecular Weight: 310.5. Formula: C19H22N2S. CAS No.: 60-89-9. Appearance: Solid. IUPAC Name: 10-[(1-methyl-3-piperidinyl)methyl]phenothiazine. Synonyms: Mepazine. Purity: Typically ≥98%. Solubility: DMSO. Storage: Typically at -20°C. Pecazine is a potent and selective MALT1 protease inhibitor with IC50 values of 0.83 μM and 0.42 μM. Pecazine exhibits anti-inflammatory, anti-tumor, and anti-microbial activities.
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| Toxicity/Toxicokinetics |
No comprehensive toxicology data are publicly available for Pecazine. The compound is intended for research use only and has not undergone full preclinical toxicology evaluation required for clinical development. As a MALT1 inhibitor, potential toxicities may include effects on immune function and NF-κB signaling. As a phenothiazine derivative, Pecazine may have central nervous system effects, including sedation and extrapyramidal symptoms. Standard toxicity studies would include acute toxicity assessment in rodents, repeated dose toxicity studies (14-day and 28-day), and genotoxicity screening (Ames test, micronucleus assay). Pecazine is for research use only and not for human therapeutic use.
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| References | |
| Additional Infomation |
Pecazine belongs to the phenothiazine class of compounds.
Pecazine is also known as Mepazine. Its IUPAC name is 10-[(1-methyl-3-piperidinyl)methyl]phenothiazine. Synonyms: Mepazine, mepazine monohydrochloride, mepazine ion(1+), pecazin. Pecazine is a potent and selective MALT1 protease inhibitor with IC50 values of 0.83 μM and 0.42 μM. Pecazine exhibits various biological activities, including anti-inflammatory, anti-tumor, and anti-microbial activities. Pecazine is commonly explored as a neuroactive agent in studies related to dopamine receptor modulation and psychotropic drug mechanisms. No clinical trials have been reported for this compound. Pecazine is for research use only. |
| Molecular Formula |
C19H22N2S
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| Molecular Weight |
310.46
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| Exact Mass |
310.15
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| CAS # |
60-89-9
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| Related CAS # |
Mepazine hydrochloride;2975-36-2
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| PubChem CID |
6075
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| Appearance |
Light yellow to light brown ointment
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| Density |
1.159 g/cm3
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| Boiling Point |
444.4ºC at 760 mmHg
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| Flash Point |
222.6ºC
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| Index of Refraction |
1.627
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| LogP |
4.634
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
22
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| Complexity |
352
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN1CCCC(CN2C3=C(C=CC=C3)SC3C2=CC=CC=3)C1
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| InChi Key |
CBHCDHNUZWWAPP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H22N2S/c1-20-12-6-7-15(13-20)14-21-16-8-2-4-10-18(16)22-19-11-5-3-9-17(19)21/h2-5,8-11,15H,6-7,12-14H2,1H3
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| Chemical Name |
10-[(1-methylpiperidin-3-yl)methyl]phenothiazine
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| Synonyms |
P-391; P 391; Pecazine
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~322.10 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (16.11 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 5 mg/mL (16.11 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2210 mL | 16.1051 mL | 32.2103 mL | |
| 5 mM | 0.6442 mL | 3.2210 mL | 6.4421 mL | |
| 10 mM | 0.3221 mL | 1.6105 mL | 3.2210 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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