DB2313
目录号 : GC62222
DB2313是一种强效的转录因子PU.1抑制剂，IC50为14nM。
Cas No.:2170606-74-1
Sample solution is provided at 25 µL, 10mM.
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DB2313 is a potent transcription factor PU.1 inhibitor with an IC50 of 14nM[1]. DB2313 disrupts the interaction of PU.1 with target gene promoters[2]. PU.1, a critical transcription factor in the hematopoietic system, plays key roles in myeloid and lymphoid cell differentiation, maintenance of hematopoietic stem cell functions, and the development of acute myeloid leukemia (AML)[3]. DB2313 is usually used in research related to AML and inflammation[4].
In vitro, DB2313 (10μg/ml; 72h) significantly inhibited the proliferation, migration, and invasion of GBM cells (U118MG and U87MG)[5].
In vivo, DB2313 (17mg/kg; every 2 days via intraperitoneal injection for 12 days) significantly suppressed tumor growth and enhanced the recruitment of CD4+ T helper 1 (Th1) and cytotoxic T/natural killer (NK) cells into tumors in the B16-OVA melanoma mouse model[6]. DB2313 (8mg/kg; intranasal administration; 5 days/week for 3 weeks) decreased airway mucus-secreting cell numbers and small airway collagen deposition, and significantly reduced airway hyperresponsiveness in a house dust mite (HDM)-induced experimental asthma mouse model[7].
References:
[1] Antony-Debre I, Paul A, Leite J, et al. Pharmacological inhibition of the transcription factor PU.1 in leukemia. J Clin Invest. 2017;127(12):4297-4313.
[2] Tu J, Chen W, Fang Y, et al. PU.1 promotes development of rheumatoid arthritis via repressing FLT3 in macrophages and fibroblast-like synoviocytes. Ann Rheum Dis. 2023;82(2):198-211.
[3] Fisher RC, Scott EW. Role of PU.1 in hematopoiesis. Stem Cells. 1998;16(1):25-37.
[4] Tu X, Kim RY, Brown AC, et al. Airway and parenchymal transcriptomics in a novel model of asthma and COPD overlap. J Allergy Clin Immunol. 2022;150(4):817-829.e6.
[5] Zhang S, Zhao S, Qi Y, et al. SPI1-induced downregulation of FTO promotes GBM progression by regulating pri-miR-10a processing in an m6A-dependent manner. Mol Ther Nucleic Acids. 2022;27:699-717.
[6] Sleapnicov N, Ha SD, Zhong SJ, et al. Inhibition of the Transcription Factor PU.1 Suppresses Tumor Growth in Mice by Promoting the Recruitment of Cytotoxic Lymphocytes Through the CXCL9-CXCR3 Axis. Cancers (Basel). 2025;17(16):2684.
[7] Tu X, Gomez HM, Kim RY, et al. Airway and parenchyma transcriptomics in a house dust mite model of experimental asthma. Respir Res. 2023;24(1):32.
DB2313是一种强效的转录因子PU.1抑制剂，IC50为14nM[1]。DB2313能够破坏PU.1与靶基因启动子的相互作用[2]。PU.1是造血系统中一个关键的转录因子，在髓系和淋巴系细胞分化、造血干细胞功能维持以及急性髓系白血病（AML）的发展中发挥重要作用[3]。DB2313通常用于AML和炎症相关研究[4]。
在体外实验中，DB2313（10μg/ml；72小时）显著抑制了胶质母细胞瘤（GBM）细胞（U118MG和U87MG）的增殖、迁移和侵袭[5]。
在体内实验中，DB2313（17mg/kg；每2天通过腹腔注射给药一次，持续12天）显著抑制了B16-OVA黑色素瘤小鼠模型中的肿瘤生长，并增强了CD4+ T辅助1型（Th1）细胞和细胞毒性T/自然杀伤（NK）细胞向肿瘤的浸润[6]。在屋尘螨（HDM）诱导的实验性哮喘小鼠模型中，DB2313（8mg/kg；鼻内给药；每周5天，持续3周）减少了气道黏液分泌细胞数量和小气道胶原沉积，并显著降低了气道高反应性[7]。
| Cell experiment [1]: | |
Cell lines | glioma cell lines U87MG and U118MG |
Preparation Method | The glioma cell lines U87MG and U118MG were cultured in DMEM containing 10% fetal bovine serum and 1% penicillin-streptomycin. All cells were maintained in a humidified incubator with 5% CO2 at 37℃. The cells were routinely tested for mycoplasma contamination. 2000 GBM cells were seeded in 96-well plates and measured cell viability using CCK-8 assay at 0, 24, 48, and 72h. GBM cells were treated with DMSO or DB2313 (10mg/mL). EdU assays were performed using an EdU assay kit with GBM cells seeded in well plates at 2×105 cells per well. 2×104 GBM cells were used for the Transwell assay. A total of 2×105 GBM cells were cultured in spheroid formation ECM for 72h to generate tumor spheroids and used for the 3D tumor spheroid invasion assay with a 96-well 3D spheroid BME cell invasion assay kit. Images were taken at 0, 24, 48, and 72h using microscope. |
Reaction Conditions | 10μg/ml; 72h |
Applications | DB2313 significantly inhibited the proliferation, migration, and invasion of GBM cells (U118MG and U87MG). |
| Animal experiment [2]: | |
Animal models | Female wild-type BALB/c mice |
Preparation Method | Female wild-type BALB/c mice were housed under specific pathogen-free conditions and maintained on a 12-hour day-night cycle with water and regular chow available ad libitum. Mice were treated intranasally with house dust mite (HDM; Dermatophagoides pteronyssinus) extract (25µg in 30µL PBS or saline (vehicle), 5 days per week for 3 weeks. One group of HDM-treated mice were treated with DB2313 (8mg/kg in PBS). Bronchoalveolar lavage fluid was collected. Mucus-secreting cells (MSCs) were stained and counted. Collagen was stained and analyzed. Airway hyperresponsiveness was assessed using the forced oscillation technique. |
Dosage form | 8mg/kg; intranasal administration; 5 days/week for 3 weeks |
Applications | DB2313 decreased airway mucus-secreting cell numbers and small airway collagen deposition, and significantly reduced airway hyperresponsiveness in a house dust mite (HDM)-induced experimental asthma mouse model. |
References: | |
| Cas No. | 2170606-74-1 | SDF | |
| 分子式 | C42H41FN8O2 | 分子量 | 708.83 |
| 溶解度 | DMSO : 3.7 mg/mL (5.22 mM; ultrasonic and warming and heat to 70°C) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.4108 mL | 7.0539 mL | 14.1078 mL |
| 5 mM | 282.2 μL | 1.4108 mL | 2.8216 mL |
| 10 mM | 141.1 μL | 705.4 μL | 1.4108 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
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