中文名 | MI 2 (MALT1 inhibitor) |
英文名 | 2-chloro-N-(4-(5-(3,4-dichlorophenyl)-3-(2-methoxyethoxy)-1H-1,2,4-triazol-1-yl)phenyl)acetamide |
别名 | MI 2 MALT1抑制剂 2-氯-N-[4-[5-(3,4-二氯苯基)-3-(2-甲氧基乙氧基)-1H-1,2,4-三唑-1-基]苯基]乙酰胺 |
英文别名 | MI-2 CHD-4 MALT1 inhibitor MI-2 MI 2 (MALT1 inhibitor) TELOMERASE INHIBITOR II, SODIUM SALT 5'-D(ATGAAAATCAGGGTTAGG)-3', SODIUM SALT 2-chloro-N-(4-(5-(3,4-dichlorophenyl)-3-(2-methoxyethoxy)-1H-1,2,4-triazol-1-yl)phenyl)acetamide 2-Chloro-N-[4-[5-(3,4-dichlorophenyl)-3-(2-methoxyethoxy)-1H-1,2,4-triazol-1-yl]phenyl]-Acetamide |
CAS | 1047953-91-2 |
化学式 | C19H17Cl3N4O3 |
分子量 | 455.72 |
溶解度 | DMSO: ≥ 46 mg/mL母液保存:分装冻存,避免反复冻融;-20℃,1个月;-80℃,6个月(稀释后溶液温度低保存可能会析出,尽量现用现配)细胞实验:先用DMSO溶解:再用培养基进行稀释,稀释过程建议分段进行,避免浓度变化过快导致化合物析出。若稀释过程中出现化合物析出的情况, 可采用超声的方法使其复溶。在稀释时要确保工作液中 DMSO 的终浓度尽量在0.1%以下,最高不要超过0.5%,并设置相应浓度的DMSO对照组。动物实验:先用DMSO溶解:再用水或者生理盐水等去稀释,稀释过程建议分段进行,避免浓度变化过快导致化合物析出。若稀释过程中出现化合物析出的情况, 可采用超声的方法使其复溶。可以通过添加助溶剂来帮助溶解,比如植物油、Tween80、甘油、羧甲基纤维素钠和PEG400等。具体方式请参考文献。悬浊液可用于口服和腹腔注射,不会影响产品活性。 |
存储条件 | -20°C |
产品用途 | MI-2 MALT1 inhibitor, also known as MI-2, is a MALT1 inhibitor (IC50 = 5.84 μM). MI-2 binds directly to MALT1 and irreversibly suppresses protease function. Decreases NF-κB activity induced by MALT1. Mucosa-associated-lymphoid-tissue lymphoma-translocation gene 1 (MALT1), a paracaspase and essential regulator for nuclear factor kB (NF-κB) activation, plays an important role in innate and adaptive immunity. Suppression of MALT1 protease activity with small molecule inhibitors showed promising efficacies in subtypes of B cell lymphoma and improvement in experimental autoimmune encephalomyelitis model. |
靶点 | MALT1 |
参考资料 展开查看 | 1: Fusco R, Siracusa R, D'Amico R, Cordaro M, Genovese T, Gugliandolo E, Peritore AF, Crupi R, Di Paola R, Cuzzocrea S, Impellizzeri D. Mucosa-Associated Lymphoid Tissue Lymphoma Translocation 1 Inhibitor as a Novel Therapeutic Tool for Lung Injury. Int J Mol Sci. 2020 Oct 20;21(20):7761. doi: 10.3390/ijms21207761. PMID: 33092214; PMCID: PMC7589767. 2: Wang R, Zhang H, Xu J, Zhang N, Pan T, Zhong X, Zhang H, Yin L, Yao Y, Wu Q, Li Z, Liu X, Xu K, Niu M. MALT1 Inhibition as a Therapeutic Strategy in T-Cell Acute Lymphoblastic Leukemia by Blocking Notch1-Induced NF-κB Activation. Front Oncol. 2020 Sep 23;10:558339. doi: 10.3389/fonc.2020.558339. PMID: 33072583; PMCID: PMC7538650. 3: Ishikawa C, Mori N. MALT-1 as a novel therapeutic target for adult T-cell leukemia. Eur J Haematol. 2020 Oct;105(4):460-467. doi: 10.1111/ejh.13467. Epub 2020 Jul 24. PMID: 32574386. 4: Liu X, Yue C, Shi L, Liu G, Cao Q, Shan Q, Wang Y, Chen X, Li H, Wang J, Gao S, Niu M, Yu R. MALT1 is a potential therapeutic target in glioblastoma and plays a crucial role in EGFR-induced NF-κB activation. J Cell Mol Med. 2020 Jul;24(13):7550-7562. doi: 10.1111/jcmm.15383. Epub 2020 May 25. PMID: 32452133; PMCID: PMC7339184. 5: Izumi K, Nishikori M, Yuan H, Otsuka Y, Nakao K, Takaori-Kondo A. Establishment and characterization of a MALT lymphoma cell line carrying an API2-MALT1 translocation. Genes Chromosomes Cancer. 2020 Sep;59(9):517-524. doi: 10.1002/gcc.22855. Epub 2020 May 6. PMID: 32348592. 6: Dezorella N, Ashkenazi |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.194 ml | 10.972 ml | 21.943 ml |
5 mM | 0.439 ml | 2.194 ml | 4.389 ml |
10 mM | 0.219 ml | 1.097 ml | 2.194 ml |
5 mM | 0.044 ml | 0.219 ml | 0.439 ml |
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