DB1976 dihydrochloride
Based on 8 publication(s) in Google Scholar
DB1976 dihydrochloride is a selenophene analog of DB270 and a potent and cell-permeable fully efficacious transcription factor PU.1 inhibitor. DB1976 dihydrochloride potently inhibits PU.1 binding (IC50 of 10 nM) and strongly inhibits the PU.1/DNA complex (with high DB1976-λB affinity, KD of 12 nM) in vitro. DB1976 dihydrochloride has apoptosis-inducing effect.
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- Reinheit: 98.0%
- CAS. Nr.: 2369663-93-2
- Formel: C20H18Cl2N8Se
- Molecular Weight:520.28
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) DB1976 dihydrochloride
More- Signal Transduct Target Ther. 2025 Feb 10;10(1):59. [Abstract]
- Nat Immunol. 2023 Nov;24(11):1839-1853. [Abstract]
- J Nanobiotechnology. 2025 Dec 5. [Abstract]
- Adv Healthc Mater. 2026 Jan 24:e05502. [Abstract]
- Int J Biol Macromol. 2025 Sep;322(Pt 1):146515. [Abstract]
- Cell Rep. 2024 Mar 26;43(3):113964. [Abstract]
- Respir Res. 2023 Jan 25;24(1):32. [Abstract]
- Neurochem Int. 2024 Feb:173:105674. [Abstract]
Biologische Aktivität
Beschreibung
IC50 & Target
IC50: 10 nM (Transcription factor PU.1)[1]
In Vitro
DB1976 is a classic heterocyclic dication (a single heteroatom) with strong affinity and selectivity for AT-rich sequences commonly found in cognate DNA binding sites for PU.1[2].
DB1976 inhibits PU.1-dependent transactivation of the reporter in a dose-dependent manner with an IC50 value of 2.4 μM in PU.1-negative HEK293 cells[3].
DB1976 treatment leads to a profound decrease in the growth of PU.1 URE–/– AML cells (IC50 of 105 μM), while showing little effect on normal hematopoietic cells at similar concentrations (IC50 of 334 μM)[3].
DB1976 treatment leads to a 1.6-fold increase in apoptotic cells in murine PU.1 URE–/– AML cells, and observed similar effects in human MOLM13 cells[3].
DB1976 treatment leads to a significant decrease in the number of viable cells (primary human AML cells) (mean decrease of 81%) and clonogenic capacity (mean decrease of 36%) compared with vehicle-treated cells. The apoptotic cell fraction increased on average by 1.5-fold with DB1976[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 2369663-93-2
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Appearance Solid
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Molecular Weight 520.28
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Formel C20H18Cl2N8Se
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Color Brown to black
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SMILES
N=C(C1=CC=C2N=C(C3=CC=C(C4=NC5=CC=C(C(N)=N)C=C5N4)[Se]3)NC2=C1)N.[H]Cl.[H]Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
Publications (8)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Spatiotemporal transcriptomics elucidates the pathogenesis of fulminant viral myocarditis. [Abstract]2025 Feb 10;10(1):59. PMID: 39924580 -
Nat Immunol
APOE4 impairs the microglial response in Alzheimer's disease by inducing TGFβ-mediated checkpoints. [Abstract]2023 Nov;24(11):1839-1853. PMID: 37749326 -
J Nanobiotechnology
Folate-modified biomimetic nanovesicles loaded with a PU.1 inhibitor alleviate atherosclerosis by suppressing inflammation. [Abstract]2025 Dec 5. PMID: 41345629 -
Adv Healthc Mater
One Stone, Four Birds: Multiple Modulation of Infarct Microenvironment-Based ROS-Responsive Hydrogel for Cardiac Repair. [Abstract]2026 Jan 24:e05502. PMID: 41580910 -
Int J Biol Macromol
EgG1Y162 protein from Echinococcus granulosus modulates the immune functions of mouse splenic lymphocytes and regulates Th9 cells. [Abstract]2025 Sep;322(Pt 1):146515. PMID: 40769342 -
Cell Rep
Nuclear microRNA-mediated transcriptional control determines adult microglial homeostasis and brain function. [Abstract]2024 Mar 26;43(3):113964. PMID: 38489263 -
Respir Res
2023 Jan 25;24(1):32. PMID: 36698141 -
Neurochem Int
M2a macrophages regulate fibrosis and affect the outcome after stroke via PU.1/mTOR pathway in fibroblasts. [Abstract]2024 Feb:173:105674. PMID: 38184171
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 50 mg/mL (96.10 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 18.33 mg/mL (35.23 mM; Need ultrasonic)
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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: 2.5 mg/mL (4.81 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Reinheit & Dokumentation
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Data Sheet (274 KB)
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SDS (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)
Verweise
[1]. Munde M, et al. Structure-dependent inhibition of the ETS-family transcription factor PU.1 by novel heterocyclic diamidines. Nucleic Acids Res. 2014 Jan;42(2):1379-90. [Content Brief]
[2]. Stephens DC, et al. Pharmacologic efficacy of PU.1 inhibition by heterocyclic dications: a mechanistic analysis. Nucleic Acids Res. 2016 May 19;44(9):4005-13. [Content Brief]
[3]. Antony-Debré I, et al. Pharmacological inhibition of the transcription factor PU.1 in leukemia. J Clin Invest. 2017 Dec 1;127(12):4297-4313. [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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 1.9220 mL | 9.6102 mL | 19.2204 mL | 48.0510 mL |
| 5 mM | 0.3844 mL | 1.9220 mL | 3.8441 mL | 9.6102 mL | |
| 10 mM | 0.1922 mL | 0.9610 mL | 1.9220 mL | 4.8051 mL | |
| 15 mM | 0.1281 mL | 0.6407 mL | 1.2814 mL | 3.2034 mL | |
| 20 mM | 0.0961 mL | 0.4805 mL | 0.9610 mL | 2.4026 mL | |
| 25 mM | 0.0769 mL | 0.3844 mL | 0.7688 mL | 1.9220 mL | |
| 30 mM | 0.0641 mL | 0.3203 mL | 0.6407 mL | 1.6017 mL | |
| DMSO | 40 mM | 0.0481 mL | 0.2403 mL | 0.4805 mL | 1.2013 mL |
| 50 mM | 0.0384 mL | 0.1922 mL | 0.3844 mL | 0.9610 mL | |
| 60 mM | 0.0320 mL | 0.1602 mL | 0.3203 mL | 0.8009 mL | |
| 80 mM | 0.0240 mL | 0.1201 mL | 0.2403 mL | 0.6006 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
DB1976 dihydrochloride Related Classifications
HY-135797A Related Classifications
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