| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
DB1976 is a traditional heterocyclic dilabel, or single heteroatom, that exhibits high selectivity and affinity for AT-rich sequences that are frequently present in PU.1's homologous DNA binding site. When applied to PU.1-negative HEK293 cells, DB1976 has an IC50 value of 2.4 μM and suppresses PU.1-dependent reporter gene transactivation in a dose-dependent manner [3]. Treatment with DB1976 significantly inhibited the development of PU.1 URE–/– AML cells (IC50 of 105 μM), but had no effect on normal hematopoietic cells (IC50 of 334 μM) at identical dosages [3]. In mouse PU.1 URE–/– AML cells, DB1976 administration led to a 1.6-fold increase in apoptotic cells; same effects were noted in human MOLM13 cells [3]. When compared to cells treated with a vehicle, DB1976 treatment significantly decreased the number of viable cells (primary human AML cells) (mean reduction of 81%) and the clonogenic capability (mean reduction of 36%). The apoptotic cell fraction is increased by DB1976 by an average of 1.5 times [3].
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| References |
[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.
[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. [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. |
| Molecular Formula |
C20H18CL2N8SE
|
|---|---|
| Molecular Weight |
520.276519298553
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| Exact Mass |
520.019
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| CAS # |
2369663-93-2
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| Related CAS # |
DB1976;1557397-51-9
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| PubChem CID |
146014497
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
8
|
| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
31
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| Complexity |
604
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ZXDJCXGSFWTRMS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H16N8Se.2ClH/c21-17(22)9-1-3-11-13(7-9)27-19(25-11)15-5-6-16(29-15)20-26-12-4-2-10(18(23)24)8-14(12)28-20;;/h1-8H,(H3,21,22)(H3,23,24)(H,25,27)(H,26,28);2*1H
|
| Chemical Name |
2-[5-(6-carbamimidoyl-1H-benzimidazol-2-yl)selenophen-2-yl]-3H-benzimidazole-5-carboximidamide;dihydrochloride
|
| Synonyms |
DB 1976 HCl; DB-1976 HCl
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~62.5 mg/mL (~120.13 mM)
H2O : ~18.33 mg/mL (~35.23 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.00 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.00 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9220 mL | 9.6102 mL | 19.2204 mL | |
| 5 mM | 0.3844 mL | 1.9220 mL | 3.8441 mL | |
| 10 mM | 0.1922 mL | 0.9610 mL | 1.9220 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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