DB1055
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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- No. CAS: 869767-86-2
- Fòrmula: C21H18N6
- Peso molecular:354.42
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Almacenamiento:
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
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| 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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No. CAS 869767-86-2
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Peso molecular 354.42
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Fòrmula C21H18N6
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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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DB1055 Related Classifications
HY-124693 Related Classifications
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