DB2313 is an inhibitor of the transcription factor PU.1 (IC50 = 14 nM).[1] Long-term exposure of DB2313 (300 nM) to Kit+/Sca-1+/Lin- hematopoietic stem progenitor cells (KSL-HSPCs) reduces colony formation. DB2313 (700 nM) decreases ovalbumin-induced reprogramming of isolated mouse neutrophils into antigen-presenting cells.[2] It decreases tumor growth, weight, and volume in a U87MG glioblastoma multiforme mouse xenograft model when administered at a dose of 10 mg/kg per day.[3]
References:
[1].Antony-Debré, I., Paul, A., Leite, J., et al.Pharmacological inhibition of the transcription factor PU.1 in leukemiaJ. Clin. Invest.127(12)4297-4313(2017).
[2].Mysore, V., Cullere, X., Mears, J., et al.FcγR engagement reprograms neutrophils into antigen cross-presenting cells that elicit acquired anti-tumor immunityNat. Commun.12(1)4791(2021).
[3].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 mannerMol. Ther. Nucleic Acids27699-717(2022).