9-ING-41 是一种基于马来酰亚胺的 ATP 竞争性和选择性的糖原合酶激酶-3β (GSK-3β) 抑制剂，IC50为 0.71 μM。9-ING-41 显著导致癌细胞的细胞周期停滞，自噬和凋亡。9-ING-41 具有抗癌活性，并具有增强化疗药物抗肿瘤作用的潜力。
| 生物活性 | 9-ING-41 is a maleimide-based ATP-competitive and selectiveglycogen synthase kinase-3β (GSK-3β)inhibitor with anIC50of 0.71 μM. 9-ING-41 significantly leads to cell cycle arrest,autophagyandapoptosisincancercells. 9-ING-41 has anticancer activity and has the potential for enhancing the antitumor effects of chemotherapeutic drugs[1][2][3][4]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | 9-ING-41 (2, 4 μM; 48 hours) decreases neuroblastoma cell viability induces apoptosis[2].
9-ING-41 (1, 2 μM; 24 hours) is a potent cell cycle-blocking agent for lymphoma cells[2].
9-ING-41 (10 μM; for 72 hours) increases the expression of LC3, an autophagy marker[3].
9-ING-41 (compound 26; 5 μM; for 6, 12, 24, 36 h) results in a pronounced decrease in NFκB-mediated expression of XIAP, the most potent antiapoptotic protein, leading to subsequent apoptosis in BXPC3 pancreatic cancer cells[1].
9-ING-41 (0.5, 1.0, 1.5, 2.0 μM) inhibits the proliferation rate of all TCL and MCL lines with concentrations as low as 1.0 mM[2].
9-ING-41 (10 μM; for 72 hours) causes cell cycle blockage at G2/M after 24 hours. 9-ING-41 treatment induces apoptotic cell death in bladder cancer cells[3].
9-ING-41 (25 μM; for 96 hours) significantly decreases expression of Cdk1 and Cyclin B1 proteins and leads to a decreased expression of antiapoptotic molecules, Bcl-2 and XIAP[3].
9-ING-41 (0.1-1 μM) inhibits GSK-3 leading to a decreased expression of the NF-κB target XIAP and significant apoptosis in neuroblastoma cells as shown by PARP cleavage, an apoptosis marker[4].
Cell Viability Assay[2] | Cell Line: | TCL and MCL lines | | Concentration: | 2, 4 μM | | Incubation Time: | 48 hours | | Result: | Induced apoptosis. |
Cell Cycle Analysis[2] | Cell Line: | Lymphoma cells (Jeko, Mino, and OCI-Ly cell lines) | | Concentration: | 1, 2 μM | | Incubation Time: | 24 hours | | Result: | Led to cell cycle arrest in G2/M. |
Cell Autophagy Assay[3] | Cell Line: | T24 cancer cells | | Concentration: | 25 μM | | Incubation Time: | 24 hours | | Result: | Showed extensive vacuolation and formation of autophagosome like structures in the cytoplasm.
Showed an increased expression of LC3, an autophagy marker. |
Western Blot Analysis[4] | Cell Line: | SK-N-DZ and SK-N-BE neuroblastoma cells | | Concentration: | 0.1, 1 μM | | Incubation Time: | 48 hours | | Result: | Inhibited GSK-3 leading to a decreased expression of the NF-κB target XIAP. |
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体内研究
(In Vivo) | 9-ING-41 (40 mg/kg/every other day; for 17 days) has single-agent antitumor activity in a mouse model of MCL[2].
| Animal Model: | NSG (NOD.Cg-PrkdcscidIl2rgtm1Wjl/SzJ) mice[2] | | Dosage: | 40 mg/kg | | Administration: | Every other day; for 17 days | | Result: | Had single-agent antitumor activity in a mouse model of MCL. |
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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 : 50 mg/mL(123.66 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.4731 mL | 12.3655 mL | 24.7310 mL | | 5 mM | 0.4946 mL | 2.4731 mL | 4.9462 mL | | 10 mM | 0.2473 mL | 1.2366 mL | 2.4731 mL |
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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 (6.18 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (6.18 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 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。 *以上所有助溶剂都可在本网站选购。
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