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Okadaic acidProtein phosphatase 1 inhibitor

Okadaic acid

Catalog No. A4540
Size Price Stock Qty
50μg $56.00 In stock
100μg $107.00 In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & MSDS

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Chemical structure

Okadaic acid

Protocol

Cell experiment [1]:

Cell lines

Rabbit lens epithelial cells, N/N1003A cells

Preparation method

The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

10-100 nM, 0-24 h,

Applications

In confluent rabbit lens epithelial cells (RLECs), okadaic acid (100 nM) within 3 to 24 h significantly induced cell apoptosis. Also, okadaic acid induced the expression of p53 and bax, which were 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.

Animal experiment [2]:

Animal models

Adult male Wistar rats

Dosage form

0-10 mg/kg, 30 min, injection cannula

Application

Intrastriatal infusion of okadaic acid (0.005, 0.05 and 0.5 nmol) increased CREB and Elk-1 phosphorylation and c-Fos immunoreactivity in the injected dorsal striatum in a dose-dependent manner. Okadaic acid (0.05 and 0.5 nM) increased c-fos mRNA expression in the dorsal striatum in a dose-dependent manner. Okadaic acid (0.05 and 0.5 nmol) at a survival time of 30 min significantly increased c-fos mRNA hybridization signals in the striatum in a dose-dependent manner. Okadaic acid at 0.05 nmol significantly increased pCREB and pElk-1. Okadaic acid (10 nM) inhibited PP-2A activity and okadaic acid (100 nM) inhibited both PP-2A and PP-1 activity.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

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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Chemical Properties

Cas No. 78111-17-8 SDF Download SDF
Chemical Name 9,10-Deepithio-9,10-didehydroacanthifolicin
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
Formula C44H68O13 M.Wt 805.01
Solubility Soluble in DMSO > 10 mM Storage Desiccate at -20°C
General tips N/A
Shipping Condition N/A

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].

References:
[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.