MI-2 (MALT1 inhibitor)

製品コードS7429 バッチS742901

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C19H17Cl3N4O3
分子量 455.72 CAS No. 1047953-91-2
Solubility (25°C)* 体外 DMSO 91 mg/mL (199.68 mM)
Ethanol 21 mg/mL (46.08 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 MI-2 (MALT1 inhibitor) is an irreversible MALT1 inhibitor with IC50 of 5.84 μM.
in vitro MI-2 inhibits MALT1 functions in ABC-DLBCL cell lines with excellent cell penetration. MI-2 produces selective growth inhibition for MALT1-dependent cell lines with GI50 of 0.2, 0.5, 0.4, and 0.4 礛 in HBL-1, TMD8, OCI-Ly3, and OCI-Ly10 cells, whereas the ABC-DLBCL MALT1-independent cell lines, U2932 and HLY-1, and the two GCB-DLBCL cell lines were resistant. [1]
in vivo MI-2 (350 mg/kg) is nontoxic to mice. MI-2 (25 mg/kg/day i.p.) profoundly suppresses the growth of both the TMD8 and HBL-1 ABC-DLBCL xenografts, whereas it has no effect on the growth of OCI-Ly1 tumors. [1]

プロトコル(参考用のみ)

キナーゼアッセイ High-Throughput Screening for MALT1 Proteolytic Activity Inhibitors
Ac-LRSR-AMC is used as substrate and reactions are measured with excitation/emission wavelengths of 360/465 nm. Two time points are measured for each reaction to eliminate false positives due to compound autofluorescence. The final percent inhibition is calculated with the formula {[fluorescencetest compound (T2-T1)-fluorescenceneg ctrl (T2-T1)]/[fluorescencepos ctrl (T2-T1)-fluorescenceneg ctrl (T2-T1)]} × 100, where Z-VRPR-FMK (300 nM) is used as positive control and buffer only as negative control. The positive hits are validated in concentration-response experiments within a dose range of 0.122–62.5 µM to determine IC50 of the compounds. Activity is validated using recombinant full-length wild-type MALT1.
細胞アッセイ 細胞株 MALT1-independent cell lines: U2932 and HLY-1, and the two GCB-DLBCL cell lines; MALT1-dependent cell lines: HBL-1, TMD8, OCI-Ly3, and OCI-Ly10 cells.
濃度 ~5 μM
反応時間 48 hours
実験の流れ Cell proliferation is determined by ATP quantification using a luminescent method and trypan blue dye exclusion. Standard curves for each cell line are calculated by plotting the cell number (determined using trypan blue) against their luminescence values, and cell number is calculated accordingly. Cell viability in drug-treated cells is normalized to their respective controls (fractional viability), and results are given as 1-fractional viability. CompuSyn software is used to determine GI25 and GI50 values.
動物実験 動物モデル SCID NOD.CB17-Prkdcscid/J mice bearing human HBL-1, TMD8, or OCI-Ly1 xenograft.
投薬量 25 mg/kg/day
投与方法 i.p.

カスタマーフィードバック

Data from [Data independently produced by , , Oncogenesis, 2017, 6(7):e365]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Cotargeting of BTK and MALT1 overcomes resistance to BTK inhibitors in mantle cell lymphoma [ J Clin Invest, 2023, 133(3)e165694] PubMed: 36719376
Proteolytic Activity of the Paracaspase MALT1 Is Involved in Epithelial Restitution and Mucosal Healing [ Int J Mol Sci, 2023, 24(8)7402] PubMed: 37108564
Inhibition of Histone H3 Lysine-27 Demethylase Activity Relieves Rheumatoid Arthritis Symptoms via Repression of IL6 Transcription in Macrophages [ Front Immunol, 2022, 13:781364] PubMed: 35296093
MLL1 inhibition reduces IgM levels in Waldenström macroglobulinemia [ Leuk Res, 2022, 116:106841] PubMed: 35462170
Extrinsic interactions in the microenvironment in vivo activate an antiapoptotic multidrug-resistant phenotype in CLL [ Blood Adv, 2021, 5(17):3497-3510] PubMed: 34432864
Inhibition of MALT1 Alleviates Spinal Ischemia/Reperfusion Injury-Induced Neuroinflammation by Modulating Glial Endoplasmic Reticulum Stress in Rats [ J Inflamm Res, 2021, 14:4329-4345] PubMed: 34511971
Copanlisib synergizes with conventional and targeted agents including venetoclax in B- and T-cell lymphoma models. [ Blood Adv, 2020, 4(5):819-829] PubMed: 32126142
Deubiquitinases Maintain Protein Homeostasis and Survival of Cancer Cells upon Glutathione Depletion. [ Cell Metab, 2019, 29(5):1166-1181] PubMed: 30799286
Antiapoptotic properties of MALT1 protease are associated with redox homeostasis in ABC-DLBCL cells. [ Mol Carcinog, 2019, 58(12):2340-2352] PubMed: 31556968
Glutaminolysis Mediated by MALT1 Protease Activity Facilitates PD-L1 Expression on ABC-DLBCL Cells and Contributes to Their Immune Evasion. [ Front Oncol, 2018, 8:632] PubMed: 30619766

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。