Okadaic acid

- Overview
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    Background
    
    Okadaic acid is a potent inhibitor of protein phosphatase 1/2A with IC50 values of 19 nM and 0.2 nM for protein phosphatase 1 and protein phosphatase 2A, respectively [1].
    Protein phosphatase 1 (PP1) and protein phosphatase 2A (PP2A) are two major mammalian serine/threonine protein phosphatases and are activated in response to Ca2+ cascades as well as increased protein kinase A activity [2].
    In confluent rabbit lens epithelial cells (RLECs), okadaic acid (100 nM) significantly induced cell apoptosis. Also, okadaic acid induced the expression of p53 and bax, which are necessary for the apoptotic programs. In N/N1003A cells, okadaic acid (10 nM) decreased total phosphatase activity by 20% and mainly inhibited PP-2A activity, while okadaic acid (100 nM) reduced 81% total phosphatase activity and inhibited PP-1 and PP-2A activity [3].
    In the rat striatum, okadaic acid (0.005, 0.05 and 0.5 nM) increased Elk-1 and CREB phosphorylation and c-Fos immunoreactivity in a dose-dependant way. Also, okadaic acid (0.05 and 0.5 nM) increased c-fos mRNA expression in a dose-dependent way [2].
    
    [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.
- Properties
  - Alternative Name
    
    9,10-Deepithio-9,10-didehydroacanthifolicin
    
    CAS Number
    
    78111-17-8
    
    Molecular Formula
    
    C44H68O13
    
    Molecular Weight
    
    805.01
    
    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.
    
    Purity
    
    Purity ≥95.00%
    
    Solubility
    
    Soluble in DMSO
    
    Storage
    
    Desiccate at -20°C
    
    * For Research Use Only
- Reference
  - 1. Bin Chen, Bin Liu, et al. "NDR1 functions as tumor suppressor in glioblastoma by phosphoralation of YAP." Research Square. doi.org/10.21203/rs.3.rs-276613/v1.
    2. 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
    3. 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
    4. 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.
    5. 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

Okadaic acid

Background

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