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Merck
CN

5.00500

MALT1 Inhibitor II, Mepazine Hydrochloride

别名:

MALT1 Inhibitor II, Mepazine Hydrochloride, 10-((1-Methylpiperidin-3-yl)methyl)-10H-phenothiazine, Hydrochloride, 10-((1-Methyl-3-piperidyl)methyl)phenothiazine, Hydrochloride, 10-((1-Methyl-3-piperidinyl)methyl)-10H-phenothiazine, Hydrochloride, MALT-1 Inhibitor II, Mucosa-Associated Lymphoid tis

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经验公式(希尔记法):
C19H23ClN2S
化学文摘社编号:
分子量:
346.92
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
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InChI

1S/C19H22N2S.Cl/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;

InChI key

ZGQUIYCUOPQIDJ-UHFFFAOYSA-N

assay

≥97% (HPLC)

form

powder

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
desiccated (hygroscopic)
protect from light

color

gray to off-white

solubility

H2O: 2.5 mg/mL
DMSO: 25 mg/mL

storage temp.

−20°C

Quality Level

Biochem/physiol Actions

Cell permeable: yes
Primary Target
MALT1

Disclaimer

Toxicity: Standard Handling (A)

General description

Mepazine hydrochloride is a cell-permeable phenothiazine derivative that inhibits mucosa-associated lymphoid tis 1(MALT1). It does not inhibit the caspase 3 or 8 proteolytic activity in a reversible and non-competitive manner. It blocks anti-CD3/CD28-stimulated IL-6 production in primary murine CD4+ T-cell and human peripheral blood mononuclear cell (PBMC) cultures. Mepazine has been observed to inhibit the MALT1 activity in activated B cell-like diffuse large B cell lymphoma (ABC-DLBCL)and RelB cleavage, resulting in effective blockage of nuclear factor (NF-κB)-dependent interleukin-6, 10 as well as anti-apoptoticB-cell lymphoma - extra-large (Bcl-xL) and FLIP-L expression. Mepazineshows ABC-DLBCL-selective cytotoxicity over GCB-DLBCL both in cultures in vitro and in mice in vivo.

Other Notes

The molecular weight for this compound isbatch-specific due to variable water content. Please refer to the vial label orthe certificate of analysis for the batch-specific molecular weight. Themolecular weight provided represents the baseline molecular weight withoutwater.

Physical form

Supplied as a hydrochloride salt.

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

pictograms

Exclamation mark

signalword

Warning

hcodes

Hazard Classifications

Acute Tox. 4 Oral

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

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Leonie Konczalla et al.
International journal of cancer, 146(6), 1618-1630 (2019-07-11)
MALT1 is a key mediator of NF-κB signaling and a main driver of B-cell lymphomas. Remarkably, MALT1 is expressed in the majority of pancreatic ductal adenocarcinomas (PDACs) as well, but absent from normal exocrine pancreatic tissue. Following, MALT1 shows off
Conor Mc Guire et al.
Journal of neuroinflammation, 11, 124-124 (2014-07-22)
The paracaspase mucosa-associated lymphoid tissue lymphoma translocation protein 1 (MALT1) is crucial for lymphocyte activation through signaling to the transcription factor NF-κB. Besides functioning as a scaffold signaling protein, MALT1 also acts as a cysteine protease that specifically cleaves a

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