Name | 4-[(5-bromopyridin-2-yl)amino]-4-oxobutanoic acid |
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Synonyms |
4-[(5-bromopyridin-2-yl)amino]-4-oxobutanoic acid
4-[(5-bromo-2-pyridyl)amino]-4-oxobutanoic acid 4-[(5-Bromo-2-pyridinyl)amino]-4-oxobutanoic acid Butanoic acid, 4-[(5-bromo-2-pyridinyl)amino]-4-oxo- Butanoic acid,4-[(5-bromo-2-pyridinyl)amino]-4-oxo- Bikinin |
Description | Bikinin is a non-steroidal, ATP-competitive inhibitor of plant GSK-3/Shaggy-like kinases and activates BR (brassinosteroids) signaling. |
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Related Catalog | |
Target |
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]. |
Kinase Assay | 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]. |
References |
Density | 1.7±0.1 g/cm3 |
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Boiling Point | 521.6±45.0 °C at 760 mmHg |
Melting Point | 144°C(lit.) |
Molecular Formula | C9H9BrN2O3 |
Molecular Weight | 273.083 |
Flash Point | 269.2±28.7 °C |
Exact Mass | 271.979645 |
PSA | 79.29000 |
LogP | 1.73 |
Appearance | white to tan |
Vapour Pressure | 0.0±1.4 mmHg at 25°C |
Index of Refraction | 1.635 |
Storage condition | 2-8°C |
Water Solubility | DMSO: ≥5mg/mL |
Symbol |
GHS07 |
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Signal Word | Warning |
Hazard Statements | H302-H319 |
Precautionary Statements | P305 + P351 + P338 |
Hazard Codes | Xn |
Risk Phrases | 22-36 |
Safety Phrases | 26 |
RIDADR | NONH for all modes of transport |
HS Code | 2933399090 |
HS Code | 2933399090 |
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Summary | 2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |