SRT3025 HCl|cas 2070015-26-6

SRT3025 HCl|cas 2070015-26-6

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Product Name: SRT3025 HCl|CAS: 2070015-26-6|Cat No: DC10629|Other Names:

SRT3025 is an orally available small molecule activator of the SIRT1 enzyme.

In vitro:
SRT3025 inhibits RANKL-induced osteoclast differentiation, fusion and resorptive capacity without affecting osteoclast survival. SRT3025 inhibits RANKL-induced osteoclastogenesis in bone marrow-derived macrophages (BMMs) by activating AMPK and deacetylating RelA/p65 lysine 310, critical for activation of the NF-κB signaling pathway. SRT3025 acts faster than oxymetholone to improve hematopoiesis. It does not work by direct activation of Sirt1 in hematopoietic cells. SRT3025 might suppress p21 transcription through the down-regulation of Egr1. SRT3025 is found to activate wild-type Sirt1 protein but failed to activate the E230K mutant, an activation-resistant Sirt1 protein (due to a mutation at position 230).
In vivo: SRT3025 treatment also inhibits tumor growth in Panc-1 xenografts, even though it is not as effective in inhibiting the viability of Panc-1 cells in culture. SRT3025 is well tolerated in mice and has the potential to be used in several diseases. SRT3025 administration expands HSPCs and boosts blood counts while long term SRT3025 administration does not permanently increase or decrease HSC repopulating potential. SRT3025 reduces plasma cholesterol, inflammation, and atherosclerosis in Apoe−/− mice, and it increases hepatic Ldlr expression and Pcsk9 accumulation.