191089-60-8

K-7174, a GATA-specific inhibitor, is a putative antiinflammatory agent that attenuates effects of inflammatory cytokines in certain cell types.

K-7174 is a homopiperazine with dual GATA and proteasome inhibitory activtiy. K-7174 selective inhibts GATA-mediated gene regulations in cultures (10-30 μM; VCAM-1 expression in HUVECs or Epo suppression in Hep3B cells) and in vivo (30 mg/kg in mice via i.p. against IL-1beta- or TNF-alpha-induced anemia). K-7174 exhibits anti-myeloma activity in vitro (10-25 μM) and in vivo (50 mg/kg/day p.o. in mice) by targeting the active pockets of β1β2 and β5 subunits of proteasome along hydrophobic grooves in the direction of the β7β1 and β4 subunits in a manner distinct from th at of bortezomib.

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