DB1055
Based on 1 Customer Validation
DB1055 is a HOXA9 inhibitor that competes with HOXA9 binding to DNA (blocking its DNA interaction activity). DB1055 induces in vitro cell growth reduction, cell apoptosis, and differentiation in human acute myeloid leukemia (AML) cells. DB1055 leads to monocyte-to-macrophage differentiation and exhibits antileukemic activities in a human THP-1 AML in vivo model. DB1055 does not impact human CD34+ bone marrow cells. DB1055 can be used for the research of acute myeloid leukemia[1].
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- Pureté: 99.68%
- CAS No.: 869767-86-2
- Formule: C21H18N6
- Masse moléculaire:354.42
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Stockage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MigA9 | IC50 |
14.09 μM
Compound: DB1055
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Cytotoxicity against mouse MigA9 cells harboring mouse Hoxa9 gene incubated for 72 hrs by MTS assay
Cytotoxicity against mouse MigA9 cells harboring mouse Hoxa9 gene incubated for 72 hrs by MTS assay
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[PMID: 30645099] |
DB1055 (10 µM; days 1-4 post-treatment) inhibits proliferation of THP-1 cells[1].
DB1055 (1.5-5 µM; 14-day) dose-dependently inhibits colony formation by THP-1 cells[1].
DB1055 (5-15 µM; 7-day) induces cell death in THP-1 cells in a concentration-dependent manner[1].
DB1055 (5-15 µM; 7-day) induces apoptotic cell death in THP-1 cells in a concentration-dependent manner[1].
DB1055 (5 µM; 3-day and 6-day) induces morphological features of differentiation in THP-1 cells[1].
DB1055 (5-15 µM; 7-day) induces myeloid differentiation in THP-1 cells, as measured by increased CD11b and CD14 expression, in a concentration-dependent manner[1].
DB1055 (0.1-10 µM; for 15 days) has low toxicity toward normal human CD34+ cell-derived erythroid, myeloid, and megakaryocyte lineages[1].
DB1055 (0.01-10 µM) inhibits HOXA9 binding to the TLR4 and EMP1 gene promoters (IC50 = 0.28 μM (TLR4), 0.18 μM (EMP1))[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:THP-1
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Concentration:10 μM
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Incubation Time:days 1-4 post-treatment
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Result:Significantly reduced the proliferation of THP-1 cells compared to untreated controls, with statistically significant differences observed (p-values indicated by asterisks in the graph).
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Cell Line:THP-1
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Concentration:5 μM,10 μM, 15 μM
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Incubation Time:7-day
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Result:Increased the percentage of Annexin V-positive (apoptotic) THP-1 cells (both PI-positive and PI-negative) in a concentration-dependent manner, with significant increases observed at 10 and 15 μM compared to untreated controls.
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Cell Line:THP-1
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Concentration:5 μM
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Incubation Time:3-day and 6-day
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Result:Induced morphological changes indicative of myeloid differentiation, including cell membrane protrusions (open arrows) and accumulation of phagocytosis vesicles (solid arrows) at both 3 and 6 days post-treatment.
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Cell Line:THP-1
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Concentration:5 μM,10 μM, 15 μM
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Incubation Time:7-day
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Result:Increased the percentage of CD11b-positive, CD14-positive, and CD11b/CD14 double-positive THP-1 cells in a concentration-dependent manner, with significant increases observed at 10 and 15 μM compared to untreated controls.
DB1055 (40 mg/kg; i.p.; on days 1, 3, and 5; for ever 3 weeks) reduces AML-associated splenomegaly and decreases blast cell counts in patient-derived AML xenograft NSG mice[1].
DB1055 (30 mg/kg; i.p.; on days 1, 3, and 5) does not result in a significant decrease in white or red blood cell counts in C57BL/6 mice, indicating that DB1055 does not inhibit normal hematopoiesis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG) mice (6-8-week-old)[1]
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Dosage:20 mg/kg
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Administration:i.p.; on days 1, 3, and 5; for 3 weeks
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Result:Significantly decreased THP-1-induced splenomegaly. Increased hCD11b-positive human THP-1 cells in blood and peritoneal ascites.
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Animal Model:NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG) mice (6-8-week-old)[1]
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Dosage:40 mg/kg
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Administration:i.p.; a total of 3 or 4 treatment cycles were administered, each cycle consisting of 1 week of dosing on days 1, 3, and 5, followed by a 2-week withdrawal period.
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Result:Markedly and significantly reduced AML-associated splenomegaly. Decreased total blast cell count in spleens, bone marrows, and blood.
Chemical Information
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CAS No. 869767-86-2
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Appearance Solid
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Masse moléculaire 354.42
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Formule C21H18N6
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Color White to off-white
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SMILES
N=C(N)C1=CC=CC(=C1)C=2C=CC(=CC2)C3=NC4=CC=C(C=C4N3)C(=N)N
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvant et solubilité
DMSO : ≥ 100 mg/mL (282.15 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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). 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)
Pureté et documentation
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Fiche technique (276 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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Instruction de manipulation (2659 KB)
Références
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 (sealed storage, away from moisture and light). 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 | 2.8215 mL | 14.1076 mL | 28.2151 mL | 70.5378 mL |
| 5 mM | 0.5643 mL | 2.8215 mL | 5.6430 mL | 14.1076 mL | |
| 10 mM | 0.2822 mL | 1.4108 mL | 2.8215 mL | 7.0538 mL | |
| 15 mM | 0.1881 mL | 0.9405 mL | 1.8810 mL | 4.7025 mL | |
| 20 mM | 0.1411 mL | 0.7054 mL | 1.4108 mL | 3.5269 mL | |
| 25 mM | 0.1129 mL | 0.5643 mL | 1.1286 mL | 2.8215 mL | |
| 30 mM | 0.0941 mL | 0.4703 mL | 0.9405 mL | 2.3513 mL | |
| 40 mM | 0.0705 mL | 0.3527 mL | 0.7054 mL | 1.7634 mL | |
| 50 mM | 0.0564 mL | 0.2822 mL | 0.5643 mL | 1.4108 mL | |
| 60 mM | 0.0470 mL | 0.2351 mL | 0.4703 mL | 1.1756 mL | |
| 80 mM | 0.0353 mL | 0.1763 mL | 0.3527 mL | 0.8817 mL | |
| 100 mM | 0.0282 mL | 0.1411 mL | 0.2822 mL | 0.7054 mL |
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