MALT1 inhibitor MI-2 是一种MALT1抑制剂 (IC50=5.84 μM),MALT1 inhibitor MI-2 直接与 MALT1 结合,不可逆地抑制蛋白酶功能,并伴有 NF-κB 报告子活性抑制、c-REL 核定位抑制和 NF-κB 靶基因下调。MALT1 inhibitor MI-2 对动物无毒。
生物活性 | MALT1 inhibitorMI-2 is aMALT1inhibitor (IC50=5.84 μM).MALT1 inhibitorMI-2 binds directly toMALT1, irreversibly suppresses protease function and is accompanied byNF-κBreporter activity suppression,c-RELnuclear localization inhibition, andNF-κBtarget gene downregulation.MALT1 inhibitorMI-2 shows nontoxic toanimals[1]. |
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体外研究 (In Vitro) | MALT1 inhibitor MI-2 (1-1000 nM; 48 hours) selectively suppresses MALT1-dependent DLBCL cell lines, and the GI50in HBL-1, TMD8, OCI-Ly3, and OCI-Ly10 cells is 0.2, 0.5, 0.4, and 0.4 μM, respectively[1]. MALT1 inhibitor MI-2 (62-1000 nM; 24 hours) causes a dose-dependent decrease in MALT1-mediated cleavage[1].
Cell Proliferation Assay[1] Cell Line: | HBL-1, TMD8, OCI-Ly3, OCI-Ly10 cells | Concentration: | 1, 10, 100, 1000 nM | Incubation Time: | 48 hours | Result: | The GI50in HBL-1, TMD8, OCI-Ly3, and OCI-Ly10 cells was 0.2, 0.5, 0.4, and 0.4 μM, respectively. |
Western Blot Analysis[1] Cell Line: | HBL-1 cells | Concentration: | 62, 125, 250, 500, 1000 nM | Incubation Time: | 24 hours | Result: | Inhibits MALT1 cleavage of CYLD in HBL-1 cells. |
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体内研究 (In Vivo) | 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[1].
Animal Model: | Eight-week-old male SCID NOD (bearing HBL-1 and TMD8 cells)[1] | Dosage: | 25 mg/kg | Administration: | Intraperitoneal injection; daily for 14 days | Result: | Profoundly suppressed the growth of both the TMD8 and HBL-1 ABC-DLBCL xenografts versus vehicle. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : ≥ 46 mg/mL(100.94 mM) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 2.1943 mL | 10.9716 mL | 21.9433 mL | 5 mM | 0.4389 mL | 2.1943 mL | 4.3887 mL | 10 mM | 0.2194 mL | 1.0972 mL | 2.1943 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (5.49 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.49 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (5.49 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.49 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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