INH154
Based on 3 publication(s) in Google Scholar
INH154 is a highly potent inhibitor for Nek2 and Hec1 binding (INH), with IC50s of 200 nM and 120 nM for INH in Hela and MB468 cells.
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- 純度: 99.89%
- CAS 番号: 1587705-63-2
- 分子式: C22H24N4OS
- 分子量:392.52
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
MedChemExpress(MCE)の使用を引用している文献 INH154
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生物活性
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NEK2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
0.2 μM
Compound: 4; INH154
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Antiproliferative activity against human HeLa cells measured after 4 days by XTT assay
Antiproliferative activity against human HeLa cells measured after 4 days by XTT assay
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[PMID: 32113126] |
| MDA-MB-468 | IC50 |
0.12 μM
Compound: 4; INH154
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Antiproliferative activity against human MDA-MB-468 cells measured after 4 days by XTT assay
Antiproliferative activity against human MDA-MB-468 cells measured after 4 days by XTT assay
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[PMID: 32113126] |
INH154 is highly potent in treating breast tumors with co-elevated expression of Hec1 and Nek2. INH154 is the most potent inhibitor of tumor cell growth. The IC50 values of INH154 in HeLa and MDA-MB-468 cancer cells are 0.20 and 0.12 μM, respectively. INH154 also suppresses the growth of leukemia, osteosarcoma, and glioblastoma cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 1587705-63-2
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性状 Solid
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分子量 392.52
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分子式 C22H24N4OS
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Color Light yellow to yellow
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SMILES
O=C(C1=CC=NC=C1)NC2=NC(C3=C(C)C=C(N4CCCCC4)C=C3C)=CS2
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Adv Sci (Weinh)
GNL3 Orchestrates AR Transcriptional Programs to Drive Castration-Resistant Prostate Cancer and Immune Evasion. [Abstract]2026 Mar 2:e16411. PMID: 41772945 -
Cell Rep Med
High NEK2 expression in myeloid progenitors suppresses T cell immunity in multiple myeloma. [Abstract]2023 Oct 17;4(10):101214. PMID: 37794587 -
Eur J Haematol
2026 Jan 23. PMID: 41577570
溶剤 & 溶解度
DMSO : 83.33 mg/mL (212.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 6.25 mg/mL (15.92 mM); Clear solution
This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
プロトコル
Mice[1]
Human triple negative breast cancer MDA-MB-468 cells, which expressed high levels of both Hec1 and Nek2, are used to test the efficacy of tumor growth in mouse xenograft. While tumor volumes reach ~100mm3, mice are randomly divided into 5 treatment groups and began to receive thrice-weekly intraperitoneal (i.p.) injections of vehicle control, 10 mg/kg INH41, 50 mg/kg INH41, 5 mg/kg INH154 or 20 mg/kg INH154. Treatment is continued for 6.5 weeks and the tumor sizes were measured[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5476 mL | 12.7382 mL | 25.4764 mL | 63.6910 mL |
| 5 mM | 0.5095 mL | 2.5476 mL | 5.0953 mL | 12.7382 mL | |
| 10 mM | 0.2548 mL | 1.2738 mL | 2.5476 mL | 6.3691 mL | |
| 15 mM | 0.1698 mL | 0.8492 mL | 1.6984 mL | 4.2461 mL | |
| 20 mM | 0.1274 mL | 0.6369 mL | 1.2738 mL | 3.1846 mL | |
| 25 mM | 0.1019 mL | 0.5095 mL | 1.0191 mL | 2.5476 mL | |
| 30 mM | 0.0849 mL | 0.4246 mL | 0.8492 mL | 2.1230 mL | |
| 40 mM | 0.0637 mL | 0.3185 mL | 0.6369 mL | 1.5923 mL | |
| 50 mM | 0.0510 mL | 0.2548 mL | 0.5095 mL | 1.2738 mL | |
| 60 mM | 0.0425 mL | 0.2123 mL | 0.4246 mL | 1.0615 mL | |
| 80 mM | 0.0318 mL | 0.1592 mL | 0.3185 mL | 0.7961 mL | |
| 100 mM | 0.0255 mL | 0.1274 mL | 0.2548 mL | 0.6369 mL |