Bikinin is a non-steroidal, ATP-competitive inhibitor of plant GSK-3(Glycogen synthase kinase 3)/Shaggy-like kinases and activates BR (brassinosteroids) signaling. 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[3]. Bikinin directly binds the GSK3 BIN2 and acts as an ATP competitor. Furthermore, bikinin inhibits the activity of six other Arabidopsis GSK3s. Genome-wide transcript analyses demonstrate that simultaneous inhibition of seven GSK3s is sufficient to activate BR responses[4]. Bikinin, a GSK3 kinase inhibitor, inhibited the SnRK2.3 kinase activity and its T180 phosphorylation in vivo[5].
Bikinin 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Arabidopsis stomatal lineage cells
50 µM
2 hours
Single-cell RNA sequencing analysis revealed that bikinin suppressed the expression of early stomatal lineage genes (e.g., POLAR, EPF2, CYCD7;1, and ERL1) while upregulating GMC/GC marker genes (e.g., SMR4, CYCA2;3, HT1, and KAT2), leading to reduced stomatal density.
Proc Natl Acad Sci U S A. 2023 Sep 5;120(36):e2303758120.
Arabidopsis protoplast cells
20 µM
2 hours
Inhibits OsGSK2 activity, reduces cytoplasmic accumulation of OsOFP8
To assess the effect of bikinin on the thermal stability of 10 AtSKs, showing Tm shifts for AtSK11, AtSK12, AtSK13, BIN2/AtSK21, AtSK22, and AtSK41, but no effect on AtSK23, AtSK31, AtSK32, and AtSK42.
Proc Natl Acad Sci U S A. 2022 Mar 15;119(11):e2118220119.
Arabidopsis cell suspension cultures
50 µM
30 minutes
To examine the effect of bikinin on the thermal stability of AtSKs, finding that bikinin stabilized AtSK13 with a Tm shift of 5.94°C but had no effect on AtSK12.
Proc Natl Acad Sci U S A. 2022 Mar 15;119(11):e2118220119.
Arabidopsis seedlings
50 µM
5 days
Assess the effect of bikinin on hypocotyl elongation in Arabidopsis seedlings; bres1 and bres2 mutants showed reduced sensitivity to bikinin
Plant Cell. 2022 Sep 27;34(10):3844-3859.
Arabidopsis seedlings
30 µM
7 days
To evaluate the effect of Bikinin on Arabidopsis seedling growth, results showed that Bikinin partially rescued the dwarf phenotype of TaSK1.2-1 and TaSK2.2-1 transgenic Arabidopsis.
BMC Plant Biol. 2015 Oct 13;15:247.
Wheat embryos
2-30 µM
7-8 days
To investigate the effect of Bikinin on wheat embryo development, results showed that Bikinin treatment impaired embryonic axis and scutellum differentiation.
BMC Plant Biol. 2015 Oct 13;15:247.
Nicotiana benthamiana plants
50 µM
Bikinin treatment increased virus susceptibility and inhibited BR-induced TMV resistance.
Sci Rep. 2016 Feb 3;6:20579.
Bikinin 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Barley
Golden Promise and Haruna Nijo cultivars
Foliar spray
10 µM, 50 µM, and 100 µM
Single treatment, continued until the 5th leaf growth stage
To investigate the effects of Bikinin on barley growth under salt stress, results showed that Bikinin treatment alleviated the long-term effects of salinity on barley growth, with more significant effects observed in the Haruna Nijo cultivar.
Int J Mol Sci. 2022 Oct 1;23(19):11644
Barley
Barley seedlings
Hydroponic treatment
10 and 50 µM
5 days
To investigate the regulatory effect of bikinin on the BR signaling pathway and its impact on barley seedling growth. Results showed that bikinin treatment reduced the phosphorylated forms of HvBZR1 and detected a tiny band of dephosphorylated form in the shoots of Haruna Nijo cultivar.
Int J Mol Sci. 2021 Dec 17;22(24):13572
Arabidopsis
Transgenic Arabidopsis
Medium treatment
30 μM
7-8 days
To investigate the rescue effect of Bikinin on the dwarf phenotype of transgenic Arabidopsis, results showed that Bikinin partially rescued the dwarf phenotype of TaSK1.2-1 and TaSK2.2-1 transgenic Arabidopsis.
BMC Plant Biol. 2015 Oct 13;15:247.
Arabidopsis thaliana
BR biosynthesis mutant cpd and signaling mutant bri1-1
Medium treatment
30 μM
7 days
Compounds 10 and 15 partially rescued the phenotype of BR mutants, including expanded leaves, increased hypocotyl lengths and light green leaves
BMC Plant Biol. 2014 Jun 19;14:172
Arabidopsis
Bin2-3 bil1 bil2 mutant
Medium treatment
5 μM
10 days
Bikinin significantly inhibited the activity of SnRK2.3-MYC on phosphorylating ABF fragment and reduced the phosphorylation level of T180.
Proc Natl Acad Sci U S A. 2014 Jul 1;111(26):9651-6
Arabidopsis thaliana
Wild-type Arabidopsis
Liquid medium treatment
50 µM
Single treatment, lasting 2 hours
Treatment of Arabidopsis seedlings with bikinin in liquid medium significantly reduced stomatal density, primarily by decreasing the density of small non-stomatal cells and the stomatal index. Additionally, bikinin suppressed the expression of early stomatal lineage genes while upregulating GMC/GC marker genes, leading to inhibited stomatal development.
Proc Natl Acad Sci U S A. 2023 Sep 5;120(36):e2303758120.
Arabidopsis
Wild-type Arabidopsis and atskquad and atsksext mutants
Treatment in liquid medium
50 μM
12 hours
To investigate the effect of bikinin on PIN1 polarity and leaf venation, showing that bikinin treatment led to loss of PIN1 polarity and abnormal leaf venation.
Proc Natl Acad Sci U S A. 2022 Mar 15;119(11):e2118220119.
Arabidopsis thaliana
Wild-type and transgenic plants
Medium treatment
50 μM
1 hour
Bikinin inhibits BIN2 kinase and enhances nuclear localization of BIL7
Plant J. 2025 Jan;121(2):e17212
Arabidopsis thaliana
Bres1 and bres2 mutants
Agar medium
50 μM bikinin
5 days
Evaluate the effect of bikinin on Arabidopsis seedling growth; bres1 and bres2 mutants exhibited reduced sensitivity to bikinin
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