2. Apoptosis
  3. Apoptosis
  4. 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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DB1055

DB1055 Chemical Structure

CAS No. : 869767-86-2

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Description

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].

In Vitro

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.

DB1055 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: THP-1
Concentration: 10 μM
Incubation Time: days 1-4 post-treatment
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).

Apoptosis Analysis[1]

Cell Line: THP-1
Concentration: 5 μM,10 μM, 15 μM
Incubation Time: 7-day
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.

Cell Differentiation Assay[1]

Cell Line: THP-1
Concentration: 5 μM
Incubation Time: 3-day and 6-day
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.

Cell Differentiation Assay[1]

Cell Line: THP-1
Concentration: 5 μM,10 μM, 15 μM
Incubation Time: 7-day
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.
In Vivo

DB1055 (20 mg/kg; i.p.; on days 1, 3, and 5; for 3 weeks) reduces THP-1-induced splenomegaly and increases hCD11b-positive THP-1 cells in NSG mice[1].
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.

Animal Model: NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG) mice (6-8-week-old)[1]
Dosage: 20 mg/kg
Administration: i.p.; on days 1, 3, and 5; for 3 weeks
Result: Significantly decreased THP-1-induced splenomegaly. Increased hCD11b-positive human THP-1 cells in blood and peritoneal ascites.
Animal Model: NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG) mice (6-8-week-old)[1]
Dosage: 40 mg/kg
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.
Result: Markedly and significantly reduced AML-associated splenomegaly. Decreased total blast cell count in spleens, bone marrows, and blood.
Molecular Weight

354.42

Formula

C21H18N6
CAS No.
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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DB1055 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DB1055869767-86-2DB 1055DB-1055Apoptosishuman AML cellsNSG immunodeficient micemonocyte-to-macrophage differentiationAML blastsacute myeloid leukemiaHOXA9DNATHP-1patient-derived xenograftshuman CD34+ bone marrow cellsInhibitorinhibitorinhibit

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