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.
For research use only. We do not sell to patients.
- Purity : 99.43%
- CAS No.: 1990504-34-1
- Formula: C28H34FN7O2
- Molecular Weight:519.61
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Bomedemstat
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Biological Activity
Description
IC50 & Target
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KDM1/LSD1 |
In Vitro
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.
In Vivo
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.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1990504-34-1
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Appearance Solid
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Molecular Weight 519.61
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Formula 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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Synonyms
IMG-7289
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
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
Solvent & Solubility
In Vitro:
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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: ≥ 5 mg/mL (9.62 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (9.62 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
In Vivo Dissolution Calculator
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.
Purity & Documentation
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Data Sheet (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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Handling Instructions (2659 KB)
References
[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 |
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| 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 |
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