| Bioactivity | Bikinin is a non-steroidal, ATP-competitive inhibitor of plant GSK-3/Shaggy-like kinases and activates BR (brassinosteroids) signaling. | ||||||||||||
| Invitro | 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]. | ||||||||||||
| Name | Bikinin | ||||||||||||
| CAS | 188011-69-0 | ||||||||||||
| Formula | C9H9BrN2O3 | ||||||||||||
| Molar Mass | 273.08 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [1]. Deng XG, et al. Role of brassinosteroid signaling in modulating Tobacco mosaic virus resistance in Nicotiana benthamiana. Sci Rep. 2016 Feb 3;6:20579. [2]. Rozhon W, et al. Bikinin-like inhibitors targeting GSK3/Shaggy-like kinases: characterisation of novel compounds and elucidation of their catabolism in planta. BMC Plant Biol. 2014 Jun 19;14:172. [3]. De Rybel B, et al. Chemical inhibition of a subset of Arabidopsis thaliana GSK3-like kinases activates brassinosteroid signaling. Chem Biol. 2009 Jun 26;16(6):594-604. |