PFI-2 HCl is an a first-in-class, potent, highly selective, and cell-active inhibitor of the methyltransferase activity of SETD7 with IC50 of 2 nM, 500 fold active than (S)-PFI-2.
PFI-2 ((R)-PFI-2 hydrochloride) hydrochloride serves as a highly potent and specific inhibitor of the SET domain-containing lysine methyltransferase 7 (SETD7), with (R)-PFI-2 exhibiting an IC50 value of 2.0 nM, indicating strong inhibitory efficacy, while (S)-PFI-2 displays an IC50 value of 1.0 μM. This compound is utilized in the study of chronic kidney disease and the inflammatory responses that contribute to the development of renal fibrosis.
体内研究
When administered intraperitoneally (i.p.) at a concentration of 200 μM twice weekly, PFI-2 hydrochloride attenuates the progression of renal fibrosis and preserves renal function in FA nephropathy and reduces ECM accumulation and fibroblasts activation after FA injury. Otherwise, at the same concentratiom, PFI-2 hydrochloride impedes Th2 cytokine signaling activation and M2 macrophage polarization and suppresses M2 macrophages-myofibroblasts transition and myeloid myofibroblasts accumulation in the FA-treated kidneys[2].
体外研究
Both enantiomers of PFI-2 show distinct inhibitory activities, with (R)-PFI-2 being notably potent at a 2.0 nM IC50 value, and (S)-PFI-2 demonstrating inhibitory capacity at a 1.0 μM IC50 value.
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