Bikinin

Bikinin is a non-steroidal, ATP-competitive inhibitor of plant GSK-3/Shaggy-like kinases and activates BR (brassinosteroids) signaling. IC50 & Target: GSK-3^[1] In Vitro: Bikinin reduces transcript levels of NbRBOHB and BR-induced NbRBOHB expression in TRV:00, TRV:NbDWARF, TRV:NbBRI1, TRV:NbBSK1, TRV:NbBAK1, TRV:NbBIK1 and TRV:NbBSU1 plants. Bikinin largely inhibits BR-increased ROS accumulation. Moreover, Bikinin decreases the transcripts of these six genes in all plants, but fails to down-regulate transcripts of these genes in NbBES1/BZR1-silenced plants. Bikinin also inhabits BR-induced up-regulation of the six genes, and the inhibition effects are compromised in NbBES1/BZR1-silenced plants^[1]. Bikinin is a potent inhibitor of group I and group II ASKs^[2]. Bikinin directly binds the GSK3 BIN2 and acts as an ATP competitor. Furthermore, bikinin inhibits the activity of six other Arabidopsis GSK3s^[3].