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上海源葉生物科技有限公司
主營產(chǎn)品： S30260異硫氰酸胍,30259鹽酸胍,嗜熱菌蛋白酶 |
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- 何小姐
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- 86-021-61559134
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- 15921386130
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- 產(chǎn)品描述：
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.
- 靶點： MALT1
- 體外研究： MALT1 inhibitor MI-2 (1-1000 nM; 48 hours) selectively suppresses MALT1-dependent DLBCL cell lines, and the GI50 in HBL-1, TMD8, OCI-Ly3, and OCI-Ly10 cells is 0.2, 0.5, 0.4, and 0.4 µM, respectively.
MALT1 inhibitor MI-2 (62-1000 nM; 24 hours) causes a dose-dependent decrease in MALT1-mediated cleavage.
- 體內(nèi)研究： MALT1 inhibitor MI-2 (25 mg/kg; i.p.; daily for 14 days) profoundly suppresses the growth of both the TMD8 and HBL-1 ABC-DLBCL xenografts.
- 細(xì)胞實驗： 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.(Only for Reference) Cell lines: 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.
- 參考文獻(xiàn)：
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
- 溶解度： DMSO: ≥ 46 mg/mL
母液保存：分裝凍存，避免反復(fù)凍融；-20℃，1個月；-80℃，6個月（稀釋后溶液溫度低保存可能會析出，盡量現(xiàn)用現(xiàn)配）
細(xì)胞實驗:先用DMSO溶解：再用培養(yǎng)基進(jìn)行稀釋，稀釋過程建議分段進(jìn)行，避免濃度變化過快導(dǎo)致化合物析出。若稀釋過程中出現(xiàn)化合物析出的情況， 可采用超聲的方法使其復(fù)溶。在稀釋時要確保工作液中 DMSO 的終濃度盡量在0.1%以下，不要超過0.5%，并設(shè)置相應(yīng)濃度的DMSO對照組。
動物實驗：先用DMSO溶解：再用水或者生理鹽水等去稀釋，稀釋過程建議分段進(jìn)行，避免濃度變化過快導(dǎo)致化合物析出。若稀釋過程中出現(xiàn)化合物析出的情況， 可采用超聲的方法使其復(fù)溶?？梢酝ㄟ^添加助溶劑來幫助溶解，比如植物油、Tween80、甘油、羧甲基纖維素鈉和PEG400等。具體方式請參考文獻(xiàn)。懸濁液可用于口服和腹腔注射，不會影響產(chǎn)品活性。
- 保存條件： -20℃
- 配置溶液濃度參考：
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 50 mM 0.044 ml 0.219 ml 0.439 ml
- 注意：部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的性，僅供客戶參考交流研究之用。
