受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C19H17Cl3N4O3 |
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分子量 | 455.72 | CAS No. | 1047953-91-2 | ||||
Solubility (25°C)* | 体外 | DMSO | 91 mg/mL (199.68 mM) | ||||
Ethanol | 22 mg/mL (48.27 mM) | ||||||
Water | Insoluble | ||||||
体内 (毎回新しく調製した物を用意してください) |
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* <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. |
製品説明 | MI-2 (MALT1 inhibitor) is an irreversible MALT1 inhibitor with IC50 of 5.84 μM. |
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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] |
キナーゼアッセイ | High-Throughput Screening for MALT1 Proteolytic Activity Inhibitors | |
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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. |
Data from [Data independently produced by , , Oncogenesis, 2017, 6(7):e365]
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。
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