Importazole
(Synonyms: IPZ) 目录号 : GC19199
Importazole是一种小分子抑制剂，能够抑制转运受体Importin-β的功能，可用于评估细胞周期特定阶段Importin-β/RanGTP通路的功能。
Cas No.:662163-81-7
Sample solution is provided at 25 µL, 10mM.
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Importazole, a small molecule inhibitor of the transport receptor importin-β, can be used to assess the function of the importin-β/RanGTP pathway at specific stages of the cell cycle[1].
In vitro, Importazole (10μM; 24h) treatment reduced the nuclear localization of IRF1 in Ca9-22 cells[2]. Blocking p85β nuclear translocation by Importazole enhances Alpelisib efficacy against PIK3CA-helical-domain-mutant tumors[3]. Inhibition of the nuclear transport protein Importin-β with Importazole (40µM; 4h) in MAC-T cells reduces ribotoxin-induced nuclear localization of IGFBP-3[4].
In vivo, Combination of Importazole (6.25mg/kg; 3 weeks; i.p.) and Alpelisib (p110α-specific inhibitor) significantly inhibited the growth of DLD1 cells, DLD1 xenograft tumors, and two patient-derived xenograft tumors harboring a PIK3CA E545K mutation[3]. Pharmacological inhibition of KPNB1 using the specific inhibitor Importazole (20mg/kg/3 times a week; 2 weeks; i.p.) significantly reduced tumor burden and prolonged survival in MLL-AF9-induced Acute myeloid leukemia (AML) mice[5].
References:
[1] Soderholm JF, Bird SL, Kalab P, et al. Importazole, a small molecule inhibitor of the transport receptor importin-β. ACS Chem Biol. 2011 Jul 15;6(7):700-8.
[2] Yoshino H, Sato Y, Nakano M. KPNB1 Inhibitor Importazole Reduces Ionizing Radiation-Increased Cell Surface PD-L1 Expression by Modulating Expression and Nuclear Import of IRF1. Curr Issues Mol Biol. 2021 May 19;43(1):153-162.
[3] He B, Li X, Yao M, et al. Blocking p85β nuclear translocation by importazole enhances Alpelisib efficacy against PIK3CA-helical-domain-mutant tumors. Biochem Biophys Res Commun. 2025 Feb 8;748:151324.
[4] Agostini-Dreyer A, Jetzt AE, Skorupa J, et al. IGFBP-3 Induced by Ribotoxic Stress Traffics From the Endoplasmic Reticulum to the Nucleus in Mammary Epithelial Cells. J Endocr Soc. 2018 Dec 24;3(3):517-536.
[5] Xie Y, Zhao R, Zheng Y, et al. Targeting KPNB1 suppresses AML cells by inhibiting HMGB2 nuclear import. Oncogene. 2025 Jun;44(21):1646-1661. doi: 10.1038/s41388-025-03340-0. Epub 2025 Mar 13.
Importazole是一种小分子抑制剂，能够抑制转运受体Importin-β的功能，可用于评估细胞周期特定阶段Importin-β/RanGTP通路的功能[1]。
体外实验中，Importazole（10μM; 24小时）处理降低了Ca9-22细胞中IRF1的核定位[2]。通过Importazole阻断p85β的核转位可以增强Alpelisib（PIK3CA螺旋结构域突变肿瘤的抑制剂）的疗效[3]。在MAC-T细胞中，使用Importazole（40µM; 4小时）抑制核转运蛋白Importin-β可以减少核糖体毒素诱导的IGFBP-3的核定位[4]。
体内实验中，Importazole（6.25mg/kg; 3周; 腹腔注射）与Alpelisib（p110α特异性抑制剂）的联合使用显著抑制了DLD1细胞、DLD1异种移植瘤以及携带PIK3CA E545K突变的两种患者来源异种移植瘤的生长[3]。使用特异性抑制剂Importazole对KPNB1进行药理学抑制，显著减少了MLL-AF9诱导的急性髓系白血病（AML）小鼠模型中的肿瘤负荷，并延长了小鼠的生存期[5]。
| Cell experiment [1]: | |
Cell lines | Human HNSCC Ca9-22 cells |
Preparation Method | Cells were seeded onto glass slides, incubated for 6h, and then treated with Importazole (10μM; 24h) and/or X-ray irradiation (X-ray irradiation was performed at 1h after Importazole administration). The treated cells were fixed for 15min with 4% paraformaldehyde in Ca2+ and Mg2+-free PBS and then blocked with blocking buffer (3% bovine serum albumin (BSA)/0.3% Triton X-100 in PBS) for 60min at room temperature. The coverslips were then incubated overnight with IRF1 primary antibody diluted to 1:300 with antibody dilution buffer (1% BSA/0.3% Triton X-100 in PBS). After incubation, the samples were washed 3 times and incubated with AlexaFluor 488®-conjugated anti-rabbit IgG secondary antibody diluted to 1:400 with antibody dilution buffer for 1h at room temperature in the dark. After washing 3 times, the samples were mounted using Mounting Medium with DAPI and examined under an LSM 710 laser-scanning microscope. |
Reaction Conditions | 10μM; 24h |
Applications | Importazole treatment reduced the nuclear localization of IRF1 in Ca9-22 cells. |
| Animal experiment [2]: | |
Animal models | 6- weeks old female NON SCID mice |
Preparation Method | For xenograft animal models, Importazole was dissolved in the solvent solution containing 5% DMSO, 40% PEG-400, 5% Tween-80, and 50% H2O. Subcutaneous tumors were generated bilaterally with DLD1 cells or small pieces of PDX tumors (2×2 mm3). Once tumor sizes reached 100-150mm3, mice were randomly assigned into four groups (5 mice per group), including vehicle group, Alpelisib group (BYL719, 12.5mg/kg, oral gavage), Importazole group (IPZ, 6.25mg/kg, intraperitoneal injection), Alpelisib plus Importazole group. Mice were treated five times per week for 3 weeks. |
Dosage form | 6.25mg/kg; 3 weeks; i.p. |
Applications | Combination of Importazole and Alpelisib (p110α-specific inhibitor) significantly inhibited the growth of DLD1 cells, DLD1 xenograft tumors, and two patient-derived xenograft tumors harboring a PIK3CA E545K mutation. |
References: | |
| Cas No. | 662163-81-7 | SDF | |
| 别名 | IPZ | ||
| Canonical SMILES | CC(NC1=C2C=CC=CC2=NC(N3CCCC3)=N1)C4=CC=CC=C4 | ||
| 分子式 | C20H22N4 | 分子量 | 318.42 |
| 溶解度 | DMSO : ≥ 33 mg/mL (103.64 mM) | 储存条件 | Store at -20°C |
| General tips | 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°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1405 mL | 15.7025 mL | 31.4051 mL |
| 5 mM | 0.6281 mL | 3.1405 mL | 6.281 mL |
| 10 mM | 0.3141 mL | 1.5703 mL | 3.1405 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.50%
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