IDB-001
Based on 1 Customer Validation
IDB-001 is a human ribosomal peptidyl transferase center (PTC) inhibitor that induces conformational changes and blocks translational elongation in specific sequence contexts through complementary interactions with Asp/Glu residues in nascent polypeptides. IDB-001 preferentially stalls ribosomes at positions containing acidic peptide motifs, thereby inhibiting cancer cell proliferation, and activates the integrated stress response via eIF2α phosphorylation at high concentrations. In addition, IDB-001 mildly triggers ribotoxic stress responses through phosphorylation of JNK and p38. IDB-001 has been applied to mechanistic studies of triple-negative breast cancer.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.48%
- CAS 番号: 3079913-81-5
- 分子式: C19H29N3O4
- 分子量:363.45
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保管条件:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
IDB-001 (10 μM; 60 min) induces translation elongation defects characterized by context-dependent stalling, preferentially targeting nascent polypeptide chains with an acidic residue at the -1 position, and elicits mild ribosome collisions upstream of stalling sites in HCC-1143 triple-negative breast cancer cells[1].
IDB-001 potently and specifically inhibits in vitro translation of reporter gene constructs containing acidic tetrameric sequences, exhibiting a biochemical selectivity window of at least 15-fold across different nascent peptide motifs. Its activity against the FTED motif is 3-fold higher than that of IDB-002 (HY-P991496), and its activity against the DDEY motif is 6-fold higher than that of IDB-002[1].
IDB-001 (50 μM; 30 min) induces a conformational change in the aspartic acid at position -1 of the nascent peptide chain to form a stable salt bridge, and triggers specific structural rearrangement of ribosomal RNA residues, thereby constricting the peptidyl transferase center and regulating the channel volume in human ribosome-nascent chain complexes containing MYC-derived QEDE peptides[1].
IDB-001 inhibits cancer cell proliferation, with an EC50 ranging from 0.663 μM (in HCC-1143 triple-negative breast cancer cells) to 5.440 μM (in MRC-5 fibroblasts). It exhibits the strongest activity against HCC-1143 cells among human cancer cell lines and fibroblast cell lines[1].
IDB-001 (10 μM; 2-8 h) induces a moderate ribotoxic stress response in MCF7 breast cancer cells: weak phosphorylation of JNK and p38 occurs after 2 h of treatment, while the integrated stress response is activated via eIF2α phosphorylation after 8 h of treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:22Rv1, HCC-1143, LS411N, MCF7, MRC-5
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Concentration:dose-response curve
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Incubation Time:72 h
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Result:Inhibited cell proliferation with EC50 values of 4.983 μM (22Rv1 prostate cancer cells), 0.663 μM (HCC-1143 triple-negative breast cancer cells), 4.233 μM (LS411N colorectal cancer cells), 1.364 μM (MCF7 HR+/HER2- breast cancer cells), and 5.440 μM (MRC-5 fibroblast cells).
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Cell Line:MCF7
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Concentration:10 μM
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Incubation Time:0, 15 min, 2 h, 4 h, 8 h
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Result:Did not induce detectable JNK phosphorylation at 15 min.
Caused modest phosphorylation of JNK and p38 after 2 h, though the magnitude was significantly lower than that observed for IDB-002.
Induced phosphorylation of eIF2α after 8 h of treatment.
化学情報
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CAS 番号 3079913-81-5
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性状 Solid-Liquid Mixture
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分子量 363.45
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分子式 C19H29N3O4
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Color White to off-white
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SMILES
O=C(NCC[C@@H]1CCCN1)O[C@H]([C@H](CN2)O)[C@H]2CC3=CC=C(C=C3)OC
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
溶剤 & 溶解度
DMSO : 50 mg/mL (137.57 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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 2.5 mg/mL (6.88 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.88 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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.
純度とドキュメンテーション
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データシート (279 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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7514 mL | 13.7571 mL | 27.5141 mL | 68.7853 mL |
| 5 mM | 0.5503 mL | 2.7514 mL | 5.5028 mL | 13.7571 mL | |
| 10 mM | 0.2751 mL | 1.3757 mL | 2.7514 mL | 6.8785 mL | |
| 15 mM | 0.1834 mL | 0.9171 mL | 1.8343 mL | 4.5857 mL | |
| 20 mM | 0.1376 mL | 0.6879 mL | 1.3757 mL | 3.4393 mL | |
| 25 mM | 0.1101 mL | 0.5503 mL | 1.1006 mL | 2.7514 mL | |
| 30 mM | 0.0917 mL | 0.4586 mL | 0.9171 mL | 2.2928 mL | |
| 40 mM | 0.0688 mL | 0.3439 mL | 0.6879 mL | 1.7196 mL | |
| 50 mM | 0.0550 mL | 0.2751 mL | 0.5503 mL | 1.3757 mL | |
| 60 mM | 0.0459 mL | 0.2293 mL | 0.4586 mL | 1.1464 mL | |
| 80 mM | 0.0344 mL | 0.1720 mL | 0.3439 mL | 0.8598 mL | |
| 100 mM | 0.0275 mL | 0.1376 mL | 0.2751 mL | 0.6879 mL |
IDB-001 関連分類
HY-172815 関連分類
Powered by Bioz
- IDB-001
- 3079913-81-5
- IDB001
- IDB 001
- JNK
- Eukaryotic Initiation Factor (eIF)
- p38 MAPK
- integrated stress response
- human ribosome peptidyl transferase center
- triple-negative breast cancer
- ribosomal RNA
- HCC-1143 triple-negative breast cancer cells
- cancer cell proliferation
- nascent polypeptide
- translation elongation
- MRC-5 fibroblasts
- ribotoxic stress response
- Inhibitor
- inhibitor
- inhibit