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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.
| Cell Experiment | |
|---|---|
| Cell lines | Clone 9 rat hepatocytes |
| Preparation method | Cells (40000 per well) were seeded on to 96-well plates. After 24 h, OA, MeOk, MC-LR or vehicle were added to the cells. Then, a 1:10 dilution of Alamar Blue was added. Fluorescence was measured by using a microplate fluorescence reader FL600 after 24 h of incubation with the toxins. |
| Concentrations | 1.5 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | Female CD-1 mice |
| Formulation | Saline solution containing 1.8% ethanol (v/v) |
| Dosages | 1 mg/kg/day |
| Administration | Gastric intubation |
| 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 |
| Related Phosphatase Products |
|---|
| CCT007093
CCT007093 is a potent PPM1D (WIP1) inhibitor with IC50 of 8.4 μM. |
| Microcystin-LR
Microcystin-LR is a potent protein phosphatase inhibitor with IC50 of 0.04 nM for PP2A, >40-fold selectivity over PP1. |
| Sal003
Sal003 is a potent and cell-permeable eIF-2α phosphatase inhibitor. |
| Razuprotafib
Razuprotafib (AKB-9778) is an effective selective inhibitor of VE-PTP (HPTPß) catalytic activity (IC50=17 pM). |
| β-Glycerophosphate disodium salt hydrate
β-Glycerophosphate is a classical serine-threonine phosphatase inhibitor used in kinase reaction buffers. |
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