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Okadaic acid

Cat. No. M5195
Okadaic acid Structure
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25ug USD 225  USD225 In stock
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Biological Activity

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. Okadaic acid (100 nM) significantly induced cell apoptosis in confluent rabbit lens epithelial cells (RLECs). Okadaic acid also 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.

Chemical Information
Molecular Weight 805.01
Formula C44H68O13
CAS Number 78111-17-8
Solubility (25°C) DMSO 25 mg/mL
Ethanol 25 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Choe ES, et al. J Neurochem. The protein phosphatase 1/2A inhibitor okadaic acid increases CREB and Elk-1 phosphorylation and c-fos expression in the rat striatum in vivo.

[2] Nuydens R, et al. J Neurochem. Okadaic acid-induced apoptosis in neuronal cells: evidence for an abortive mitotic attempt.

[3] Holmes CF. Toxicon. Liquid chromatography-linked protein phosphatase bioassay; a highly sensitive marine bioscreen for okadaic acid and related diarrhetic shellfish toxins.

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