Okadaic acid
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Okadaic acid是一种强效的蛋白磷酸酶1/2A抑制剂，作用于蛋白质磷酸酶1和蛋白质磷酸酶2A，IC50值分别19 nM和0.2 nM [1]。
蛋白质磷酸酶1（PP1）和蛋白质磷酸酶2A（PP2A）是二个主要的哺乳动物丝氨酸/苏氨酸蛋白磷酸酶，随着Ca2+ 级联以及蛋白激酶A活性增加而被激活 [2]。
在融合兔晶状体上皮细胞（RLECs）中，Okadaic acid（100 nM）显著地诱导细胞凋亡。此外，Okadaic acid诱导细胞凋亡程序必需的p53和bax的表达。在N/N1003A 细胞中，Okadaic acid（10 nM）降低20%的总磷酸酶活性，主要抑制PP-2A的活性，而Okadaic acid（100 nM） 降低81%的总磷酸酶活性，主要抑制PP-1 和PP-2A的活性 [3] 。
在大鼠纹状体中，Okadaic acid（0.005、0.05 和0.5 nM）剂量依赖性地增加Elk-1和CREB磷酸化以及c-Fos免疫反应性。此外，Okadaic acid（0.05 和0.5 nM）剂量依赖性地增加c-fos mRNA表达 [2]。
参考文献： [1].Holmes CF. Liquid chromatography-linked protein phosphatase bioassay; a highly sensitive marine bioscreen for okadaic acid and related diarrhetic shellfish toxins. Toxicon, 1991, 29(4-5): 469-477. [2].Choe ES, Parelkar NK, Kim JY, et al. The protein phosphatase 1/2A inhibitor okadaic acid increases CREB and Elk-1 phosphorylation and c-fos expression in the rat striatum in vivo. J Neurochem, 2004, 89(2): 383-390. [3].Li DW, Fass U, Huizar I, et al. Okadaic acid-induced lens epithelial cell apoptosis requires inhibition of phosphatase-1 and is associated with induction of gene expression including p53 and bax. Eur J Biochem, 1998, 257(2): 351-361.
- 1. Chiara Balbo Pogliano, Ilaria Ceppi, et al. "The CDK1-TOPBP1-PLK1 axis regulates the Bloom's syndrome helicase BLM to suppress crossover recombination in somatic cells." Sci Adv. 2022 Feb 4;8(5):eabk0221. PMID: 35119917
- 2. Bin Chen, Bin Liu, et al. "NDR1 functions as tumor suppressor in glioblastoma by phosphoralation of YAP." Research Square. 11 Mar, 2021.
- 3. Amitha Muraleedharan, Noa Rotem-Dai, et al. "Protein kinase C eta is activated in reactive astrocytes of an Alzheimer's disease mouse model: Evidence for its immunoregulatory function in primary astrocytes." Glia. 2020 Oct 17. PMID: 33068318
- 4. Grigaitis R, Ranjha L, et al. "Phosphorylation of the RecQ Helicase Sgs1/BLM Controls Its DNA Unwinding Activity during Meiosis and Mitosis." Dev Cell. 2020;53(6):706-723.e5. PMID: 32504558
- 5. Ilaria Ceppi, Sean M. Howard, et al. "CtIP promotes the motor activity of DNA2 to accelerate long-range DNA end resection." bioRxiv. 2019 October 01.
- 6. Xu J, Zhang L, et al. "PP2A Facilitates Porcine Reproductive and Respiratory Syndrome Virus Replication by Deactivating irf3 and Limiting Type I Interferon Production." Viruses. 2019 Oct 15;11(10). pii: E948. PMID: 31618847
| Physical Appearance | A solution in ethanol. To change the solvent, simply evaporate the ethanol under a gentle stream of nitrogen and immediately add the solvent of choice. |
| Storage | Desiccate at -20°C |
| M.Wt | 805.01 |
| Cas No. | 78111-17-8 |
| Formula | C44H68O13 |
| Solubility | Soluble in DMSO |
| Chemical Name | 9,10-Deepithio-9,10-didehydroacanthifolicin |
| SDF | Download SDF |
| Canonical SMILES | CC1CCC2(CCCCO2)OC1C(C)CC(C3C(=C)C(C4C(O3)CCC5(O4)CCC(O5)C=CC(C)C6CC(=CC7(O6)C(CCC(O7)CC(C)(C(=O)O)O)O)C)O)O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验 [1]: | |
|
细胞系 |
兔晶状体上皮细胞，N/N1003A细胞 |
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溶解方法 |
该化合物在DMSO中的溶解度大于10 mM。若获取更高浓度的溶液，可在37°C下孵育10分钟，随后在超声波浴中摇匀。-20°C以下可储存数月。 |
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反应条件 |
10-100 nM，0-24 h |
|
应用 |
在融合性的兔子晶状体上皮细胞（RLECs）中，Okadaic acid（100 nM）孵育3-24 h显著诱导细胞凋亡。此外，Okadaic acid诱导凋亡程序所必需的p53和bax的表达。在N/N1003A细胞中，Okadaic acid（10 nM）将总磷酸酶的活性降低20％，主要抑制PP-2A活性，而Okadaic acid（100 nM）降低总磷酸酶活性的81％，并抑制PP-1和PP-2A活性。 |
| 动物实验 [2]: | |
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动物模型 |
成年雄性Wistar大鼠 |
|
给药剂量 |
0–10 mg/kg，30 min，注射套管 |
|
应用 |
肠内输注Okadaic acid（0.005、0.05和0.5 nmol）以剂量依赖的方式增加注射的背纹纹状体中CREB和Elk-1的磷酸化以及c-Fos的免疫反应性。Okadaic acid（0.05和0.5 nM）以剂量依赖的方式增加背侧纹状体中c-fos mRNA的表达。Okadaic acid（0.05和0.5 nmol）以剂量依赖的方式显著增加纹状体中的c-fos mRNA杂交信号。Okadaic acid (0.05 nmol)显著增加pCREB和pElk-1。Okadaic acid（10 nM）抑制PP-2A活性，Okadaic acid（100 nM）抑制PP-2A和PP-1活性。 |
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注意事项 |
由于实验环境的不同，实际溶解度可能与理论值略有不同，请测试室内所有化合物的溶解度。 |
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References: [1]. Li DW, Fass U, Huizar I, et al. Okadaic acid-induced lens epithelial cell apoptosis requires inhibition of phosphatase-1 and is associated with induction of gene expression including p53 and bax. Eur J Biochem, 1998, 257(2): 351-361. [2]. Choe ES, Parelkar NK, Kim JY, et al. The protein phosphatase 1/2A inhibitor okadaic acid increases CREB and Elk-1 phosphorylation and c-fos expression in the rat striatum in vivo. J Neurochem, 2004, 89(2): 383-390. |
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化学结构
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