Bikinin是一种具有ATP竞争性的非甾体类植物GSK-3（糖原合酶激酶3）/Shaggy-like激酶抑制剂。
Cas No.:188011-69-0
Sample solution is provided at 25 µL, 10mM.
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Bikinin is a non-steroidal, ATP-competitive inhibitor of plant GSK-3 (glycogen synthase kinase 3)/Shaggy-like kinases. Bikinin can be used for research on plant growth and development, hormone signal transduction, and abiotic stress response mechanism[1-4].
In vitro, barley (Golden Promise and Haruna Nijo cultivars) was treated with Bikinin (10–100μM) for 0–5 days under salt stress conditions, followed by continuous stimulation with 150mM sodium chloride (NaCl) until the BBCH20 growth stage. Bikinin significantly reduced the abundance of phosphorylated HvBZR1 protein (inhibiting its phosphorylation level), while upregulating the expression of genes related to the BR signaling pathway and alleviating salt stress-induced damage to plant cells[5]. Bikinin (25–50μM) was administered to pretreat wild-type Marchantia polymorpha (Tak-1 cultivar) plants for 0–5 days, followed by normal cultivation for 5–10 days. Bikinin significantly promoted cell proliferation activity in the apical meristematic region, expanded the boundaries of this region, and simultaneously inhibited subsequent cell differentiation, leading to the loss of the typical dorsoventral structure and the accumulation of undifferentiated cell masses[6].
References:
[1] Deng XG, Zhu T, Peng XJ, 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, Wang W, Berthiller F, 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, Audenaert D, Vert G, 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.
[4] Lu Q, Houbaert A, Ma Q, et al. Adenosine monophosphate deaminase modulates BIN2 activity through hydrogen peroxide-induced oligomerization. Plant Cell. 2022 Sep 27;34(10):3844-3859.
[5] Groszyk J, Przyborowski M. Inhibition of the Glycogen Synthase Kinase 3 Family by the Bikinin Alleviates the Long-Term Effects of Salinity in Barley. Int J Mol Sci. 2022 Oct 1;23(19):11644.
[6] Furuya T, Nishihama R, Ishizaki K, et al. A glycogen synthase kinase 3-like kinase MpGSK regulates cell differentiation in Marchantia polymorpha. Plant Biotechnol (Tokyo). 2022 Mar 25;39(1):65-72.
Bikinin是一种具有ATP竞争性的非甾体类植物GSK-3（糖原合酶激酶3）/Shaggy-like激酶抑制剂。Bikinin可用于植物生长发育、激素信号转导及非生物胁迫响应机制的相关研究[1-4]。
在体外，Bikinin（10–100μM）处理大麦（Golden Promise及Haruna Nijo品系）0–5天（盐胁迫条件下），随后以150mM氯化钠（NaCl）持续刺激至BBCH20生长阶段。Bikinin显著降低了磷酸化HvBZR1蛋白的丰度（抑制其磷酸化水平），同时上调了BR信号通路相关基因的表达并缓解了盐胁迫对植物细胞的损伤[5]。Bikinin（25–50μM）预处理野生型Marchantia polymorpha（Tak-1品系）植株0–5天，随后正常培养5–10天。Bikinin显著促进了顶端分生组织区域（meristematic region）的细胞增殖活性并扩大了该区域的边界，同时抑制了细胞的后续分化进程，导致植株丧失典型的背腹结构并积累未分化细胞团（undifferentiated cell mass）[6]。
| Cell experiment [1]: | |
Cell lines | Marchantia polymorphawild-type Takaragaike-1 (Tak-1) and proMpCYCD;1:MpCYCD;1Nter-tdTomato-NLS reporter lines. |
Preparation Method | Tak-1 and reporter lines were maintained on half-strength Gamborg's B5 medium supplemented with 1% (w/v) agar and 1% (w/v) sucrose under 50–60μmol m⁻² s⁻¹ continuous white light at 22 °C. Tak-1 were treated with Bikinin at clinically relevant concentrations for indicated durations. |
Reaction Conditions | 25μM or 50μM; 5 days or 10 days |
Applications | Bikinin significantly altered the thallus morphology, resulting in abnormally small and deformed structures. Bikinin also induced the expansion of the meristematic region and enhanced cell proliferation activity, expanding the expression domain of MpCYCD;1 and increasing the area of EdU-incorporated nuclei. |
References: | |
| Cas No. | 188011-69-0 | SDF | |
| 别名 | Abrasin | ||
| 化学名 | 4-((5-bromopyridin-2-yl)amino)-4-oxobutanoic acid | ||
| Canonical SMILES | BrC1=CN=C(NC(CCC(O)=O)=O)C=C1 | ||
| 分子式 | C9H9BrN2O3 | 分子量 | 273.08 |
| 溶解度 | ≥ 13.65mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.6619 mL | 18.3097 mL | 36.6193 mL |
| 5 mM | 732.4 μL | 3.6619 mL | 7.3239 mL |
| 10 mM | 366.2 μL | 1.831 mL | 3.6619 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet