2. Apoptosis
  3. Apoptosis
  4. DB1055

DB1055 是一种 HOXA9 抑制剂，可与 HOXA9 竞争结合 DNA (阻断其 DNA 相互作用活性)。DB1055 在体外诱导人急性髓系白血病 (AML) 细胞增殖减少、细胞凋亡 (apoptosis) 及分化。DB1055 促进单核细胞向巨噬细胞分化，并在人 THP-1 AML 异种移植体内模型中表现出抗白血病活性。DB1055 不影响人 CD34+ 骨髓细胞。DB1055 可用于急性髓系白血病研究。

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DB1055

DB1055 Chemical Structure

CAS No. : 869767-86-2

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DB1055 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

DB1055 (10 µM; 处理后第 1-4 天) 抑制 THP-1 细胞的增殖[1]。
DB1055 (1.5-5 µM; 14-day) 剂量依赖性地抑制 THP-1 细胞的集落形成[1]。
DB1055 (5-15 µM; 7-day) 以浓度依赖的方式诱导 THP-1 细胞死亡[1]。
DB1055 (5-15 µM; 7-day) 以浓度依赖的方式在 THP-1 细胞中诱导凋亡性细胞死亡 [1]。
DB1055 (5 µM; 3-day and 6-day) 诱导 THP-1 细胞出现分化的形态学特征[1]。
DB1055 (5-15 µM; 7-day) 以浓度依赖性方式诱导 THP-1 细胞的髓系分化，表现为 CD11b 和 CD14 表达增加[1]。
DB1055 (0.1-10 µM; 15 天) 对来源于正常人 CD34+ 细胞的红系、髓系和巨核系谱系表现出较低的毒性[1]。
DB1055 (0.01-10 µM) 抑制 HOXA9 与 TLR4 和 EMP1 基因启动子的结合 (IC50 = 0.28 μM (TLR4)，0.18 μM (EMP1))[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

DB1055 相关抗体:

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.
体内研究
(In Vivo)

DB1055 (20 mg/kg; i.p.; 在第 1、3 和 5 天；持续 3 周) 减少 THP-1 诱导的脾肿大，并增加在 NSG 小鼠中的 hCD11b 阳性 THP-1 细胞[1]。
DB1055 (40 mg/kg; i.p.; 在第 1、3 和 5 天给药；每 3 周一次) 减少患者来源的 AML 异种移植 NSG 小鼠的 AML 相关脾肿大，并降低原始细胞计数[1]。
DB1055 (30 mg/kg; i.p.; on days 1, 3, and 5) 在 C57BL/6 小鼠中未导致白细胞或红细胞计数显著减少，表明 DB1055 不会抑制正常的造血作用 [1]。

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.
分子量

354.42

Formula

C21H18N6
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

DB1055 相关分类

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  • 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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