MG-101 (ALLN) 是半胱氨酸蛋白酶的抑制剂,抑制钙蛋白酶 I,钙蛋白酶 II,组织蛋白酶 B 和组织蛋白酶 L,其Ki值分别为 190,220,150 和 500 pM。MG-101 诱导细胞凋亡,抑制结肠肿瘤生长,可用于结肠癌的研究。
生物活性 | MG-101 (ALLN) is an inhibitor ofcysteine proteaseswhich inhibits calpain I, calpain II,cathepsin Bandcathepsin LwithKis of 190, 220, 150 and 500 pM, respectively. MG-101 inducesapoptosisand inhibits tumor growth, it can be used for the research of coloncancer[1]. |
体外研究 (In Vitro) | MG-101 (0-26 μM; 24 h) affects the growth of colon cancer HCT116 cells[1].MG-101 (0-26 μM; 24 h) induces apoptosis of various cancer cells[1].MG-101 (0-26 μM; 24 h) induces Bax-dependent apoptosis in HCT116 cells[1].
Cell Viability Assay[1] Cell Line: | HCT116 cell line | Concentration: | 0-26 μM | Incubation Time: | 24 hours | Result: | Anchorage-independently and significantly decreased the viability of HCT116 cells. |
Western Blot Analysis[1] Cell Line: | HCT116, RKO, SW480 and HepG2 cell lines | Concentration: | 0-26 μM | Incubation Time: | 24 hours | Result: | Dose-dependently decreased the concentration of pro-caspase 3 and increased the concentration of cleaved-PARP in HCT116 cells. Induced apoptosis of HCT116, RKO, SW480 and HepG2 cells. |
Western Blot Analysis[1] Cell Line: | HCT116, HCT116/p53-/-and HCT116/Bax-/-cell lines | Concentration: | 0-26 μM | Incubation Time: | 24 hours | Result: | Induced apoptosis via a Bax-dependent manner, but not via a p53-dependent manner. |
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体内研究 (In Vivo) | MG-101 (10 mg/kg; i.p. once daily for 15 days) inhibits tumor growth in nude mice[1].
Animal Model: | Female athymic nude mice with HCT116 cells injection[1] | Dosage: | 10 mg/kg | Administration: | Intraperitoneal injection; 10 mg/kg once daily; for 15 days | Result: | Significantly decreased tumor weight and volume of treated mice at day 26 compared to control mice, and showed no effect on body weights. |
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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 : 16.67 mg/mL(43.46 mM;Need ultrasonic) 配制储备液 1 mM | 2.6074 mL | 13.0368 mL | 26.0736 mL | 5 mM | 0.5215 mL | 2.6074 mL | 5.2147 mL | 10 mM | 0.2607 mL | 1.3037 mL | 2.6074 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: ≥ 1.67 mg/mL (4.35 mM); Clear solution
此方案可获得 ≥ 1.67 mg/mL (4.35 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 16.7 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% (20%SBE-β-CDin saline) Solubility: 1.67 mg/mL (4.35 mM); Suspended solution; Need ultrasonic
此方案可获得 1.67 mg/mL (4.35 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例,取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 1.67 mg/mL (4.35 mM); Clear solution
此方案可获得 ≥ 1.67 mg/mL (4.35 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 16.7 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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