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.
















