Bomedemstat
Based on 5 publication(s) in Google Scholar
Bomedemstat (IMG-7289) is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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: 99.43%
- CAS 番号: 1990504-34-1
- 分子式: C28H34FN7O2
- 分子量:519.61
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
MedChemExpress(MCE)の使用を引用している文献 Bomedemstat
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生物活性
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KDM1/LSD1 |
Bomedemstat selectively inhibits proliferation and induces apoptosis of Jak2V617F cells by concomitantly increasing expression and methylation of p53[1].
Bomedemstat (50 nM-1 μM; 96 h) enhances survival, induces apoptosis via BCL-XL and PUMA in a TP53-dependent manner, and leads to cell cycle arrest[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SET-2 cells
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Concentration:50 nM, 100 nM, and 1 μM
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Incubation Time:96 hours
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Result:Decreased levels of the antiapoptotic protein BCL-XL and increased levels of the pro-apoptotic protein PUMA.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mx-Jak2V617F mice[1]
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Dosage:45 mg/kg
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Administration:Oral gavage; 45 mg/kg; once daily; 56 days
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Result:Reduced splenomegaly significantly with a few treated mice normalizing their spleen weight, the 56-day course led to partial restoration of lymph follicles and spleen architecture by histological examination.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1990504-34-1
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性状 Solid
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分子量 519.61
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分子式 C28H34FN7O2
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Color White to off-white
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SMILES
O=C(N1CCN(CC1)C)[C@@H](NC(C2=CC=C(N3C=CN=N3)C=C2)=O)CCCN[C@H]4[C@@](C5=CC=C(C=C5)F)([H])C4
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別名
IMG-7289
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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 In solvent -80°C 6 months -20°C 1 month
Publications (5)
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Journal Impact Factor
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Most Recent
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Nature
Perturbing LSD1 and WNT rewires transcription to synergistically induce AML differentiation. [Abstract]2025 Jun;642(8067):508-518. PMID: 40240608 -
Nat Commun
Copy number amplification of FLAD1 promotes the progression of triple-negative breast cancer through lipid metabolism. [Abstract]2025 Feb 1;16(1):1241. PMID: 39890808 -
Proc Natl Acad Sci U S A
2025 May 20;122(20):e2425812122. PMID: 40366693 -
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bioRxiv
Spatially-Resolved Multiomic Atlas of Leiomyosarcoma Identifies Two Clinically Relevant Epigenetically-Driven Cell States. [Abstract]2026 May 26:2026.05.22.726988. PMID: 42244620
溶剤 & 溶解度
DMSO : ≥ 100 mg/mL (192.45 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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. 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. 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)
純度とドキュメンテーション
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データシート (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Jonas S Jutzi,et al. LSD1 Inhibition Prolongs Survival in Mouse Models of MPN by Selectively Targeting the Disease Clone. Hemasphere.2018 Jun 8;2(3):e54. [Content Brief]
[2]. Yuan Fang, et al. LSD1/KDM1A inhibitors in clinical trials: advances and prospects. J Hematol Oncol. 2019 Dec 4;12(1):129. [Content Brief]
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. 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 | 1.9245 mL | 9.6226 mL | 19.2452 mL | 48.1130 mL |
| 5 mM | 0.3849 mL | 1.9245 mL | 3.8490 mL | 9.6226 mL | |
| 10 mM | 0.1925 mL | 0.9623 mL | 1.9245 mL | 4.8113 mL | |
| 15 mM | 0.1283 mL | 0.6415 mL | 1.2830 mL | 3.2075 mL | |
| 20 mM | 0.0962 mL | 0.4811 mL | 0.9623 mL | 2.4057 mL | |
| 25 mM | 0.0770 mL | 0.3849 mL | 0.7698 mL | 1.9245 mL | |
| 30 mM | 0.0642 mL | 0.3208 mL | 0.6415 mL | 1.6038 mL | |
| 40 mM | 0.0481 mL | 0.2406 mL | 0.4811 mL | 1.2028 mL | |
| 50 mM | 0.0385 mL | 0.1925 mL | 0.3849 mL | 0.9623 mL | |
| 60 mM | 0.0321 mL | 0.1604 mL | 0.3208 mL | 0.8019 mL | |
| 80 mM | 0.0241 mL | 0.1203 mL | 0.2406 mL | 0.6014 mL | |
| 100 mM | 0.0192 mL | 0.0962 mL | 0.1925 mL | 0.4811 mL |