SI-113

SI-113 is a serum/glucocorticoid-regulated kinase 1 (SGK1) inhibitor (IC₅₀ = 600 nM).¹ It is selective for SGK1 over c-Src and Abl kinases at 12.5 µM.² SI-113 (12.5 µM) is cytotoxic to MCF-7 breast cancer, A172 glioblastoma multiforme, and RKO colorectal adenocarcinoma cell lines. In vivo, SI-113, in combination with paclitaxel, reduces tumor volume, tumor weight, and SGK1 protein levels in a patient-derived xenograft (PDX) mouse model of ovarian cancer when administered at a dose of 9.3 mg/kg.³. SI-113 (100 µg/ml) is also active against S. aureus and E. coli.⁴

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1. Greco, C., Taresco, V., Pearce, A.K., et al. Development of pyrazolo[3,4-d]pyrimidine kinase inhibitors as potential clinical candidates for glioblastoma multiforme. ACS Med. Chem. Lett. 11(5), 657-663 (2020).

2. D'Antona, L., Amato, R., Talarico, C., et al. SI113, a specific inhibitor of the Sgk1 kinase activity that counteracts cancer cell proliferation. Cell. Physiol. Biochem. 35(5), 2006-2018 (2015).

3. D'Antona, L., Dattilo, V., Catalogna, G., et al. In preclinical model of ovarian cancer, the SGK1 inhibitor SI113 counteracts the development of paclitaxel resistance and restores drug sensitivity. Transl. Oncol. 12(8), 1045-1055 (2019).

4. Greco, C., Catania, R., Balcco, D.L., et al. Synthesis and antibacterial evaluation of new pyrazolo[3,4-d]pyrimidines kinase inhibitors. Molecules 25(22), 5354 (2020).