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  3. Bikinin

Bikinin (Synonyms: Abrasin)

Cat. No.: HY-12524 Purity: 99.94%
Handling Instructions

Bikinin is a non-steroidal, ATP-competitive inhibitor of plant GSK-3/Shaggy-like kinases and activates BR (brassinosteroids) signaling.

For research use only. We do not sell to patients.

Bikinin Chemical Structure

Bikinin Chemical Structure

CAS No. : 188011-69-0

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 82 In-stock
Estimated Time of Arrival: December 31
50 mg USD 216 In-stock
Estimated Time of Arrival: December 31
100 mg USD 372 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Bikinin is a non-steroidal, ATP-competitive inhibitor of plant GSK-3/Shaggy-like kinases and activates BR (brassinosteroids) signaling.

IC50 & Target[1]

GSK-3

 

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].

Molecular Weight

273.08

Formula

C₉H₉BrN₂O₃

CAS No.

188011-69-0

SMILES

O=C(O)CCC(NC1=NC=C(Br)C=C1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 42 mg/mL (153.80 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.6619 mL 18.3097 mL 36.6193 mL
5 mM 0.7324 mL 3.6619 mL 7.3239 mL
10 mM 0.3662 mL 1.8310 mL 3.6619 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (9.15 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (9.15 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[2]

ASKs are expressed as GST-fusion proteins in Escherichia coli BL21. In vitro kinase assays are performed by incubating 50 ng GST-fusion protein, 10 μg myelin basic protein (MBP) as a substrate and 0.15 MBq γ-[32P]-ATP as co-substrate at 25°C for 30 min. The reaction buffer consists of 20 mM HEPES/KOH pH 7.4, 15 mM MgCl2, 5 mM EGTA, 1 mM dithiothreitol and 1 μM cold ATP. The reaction products are separated by SDS-PAGE and the amount of radioactivity incorporated into MBP quantified using an Amersham storage phosphor imager screen and a Biorad Molecular Imager FX[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

BikininAbrasinGSK-3Glycogen synthase kinase-3Glycogen synthase kinase 3Inhibitorinhibitorinhibit

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Bikinin
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