| Name | EIPA |
| Description | EIPA (L593754) is a TRPP3 channel inhibitor (IC50=10.5 μM) and an inhibitor of Na+/H+ exchange (NHE). EIPA inhibits megacytosis, promotes autophagy, and can be used in inflammation and tumor studies. |
| Cell Research | The effect of EIPA alone (without alanine or proline) is also examined in both control (DMEM cultured cells) and amino acid-starved cells. The cells are incubated for 6 h in DMEM containing 5% FBS and either 0 or 0.3 mM EIPA (labeled QNN and QNE, respectively), HBSS containing either 0 or 0.3 mM EIPA (labeled HNN and HNE, respectively), HBSS with 1.0 mM alanine (labeled HAN) or 0.5 mM proline (labeled HPN), HBSS with 1.0 mM alanine and 0.3 mM EIPA (labeled HAE), and HBSS with 0.5 mM proline and 0.3 mM EIPA (labeled HPE) [2]. |
| In vitro | METHODS: Ten cells were pretreated with EIPA (50 µM) for 1.5 h. Dextran index was measured by Dextran uptake assay.
RESULTS: Immortalized but untransformed hTERT-HME1 mammary epithelial cells and MCF10A cells did not exhibit megacellular drinking in complete medium, but stimulated dextran uptake by nutrient deprivation. Although PIK3CB was found to be required for growth factor-stimulated macrocytosis, oncogenic mutations in PIK3CA were sufficient to induce constitutive macrocytosis in mouse embryonic fibroblast MEFs and untransformed MCF10A cells. [1]
METHODS: MKN28 cells were treated with EIPA (5-100 µM) for 48 h. Cell proliferation was detected by cell count.
RESULTS: Cell exposure to EIPA inhibited the proliferation of MKN28 cells in a dose- and time-dependent manner. [2] |
| In vivo | METHODS: To assay in vivo activity, EIPA (10 mg/kg) was injected intraperitoneally into BALB/c mice bearing 4T1 xenografts, and 70 kD FITC-Ficoll was injected into the tumors 1 h later. The mice were necropsied 1 h after Ficoll injection, and the tumors were excised and frozen in OCT.
RESULTS: EIPA-sensitive 70 kD FITC-Ficoll uptake was observed in in situ homozygous 4T1 tumors of BALB/c mice, suggesting that AMPK activation or other signals are sufficient to trigger the formation of large fusions in vivo. [1] |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 135 mg/mL (450.36 mM), Sonication is recommended.
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| Keywords | colon carcinoma | IEC-18 | NHE3 | renal failure | IBDs | Cation channel | ddY strain mice | MKN28 | L-593754 | Autophagy | gastric cancer | Inhibitor | neuron | pancreatic carcinoma | EIPA | inhibit | IECs | TRP Channel | L 593754 | Sodium-hydrogen Exchanger | Prostaglandin Receptor | Cyclooxygenase | COX | Na+/H+ Exchanger (NHE) | zinc | Transient receptor potential channels | calcium | kainite | Sodium/hydrogen Exchanger |
| Inhibitors Related | Phenytoin sodium | Lidocaine Hydrochloride hydrate | Lidocaine | Camphor | Lidocaine hydrochloride | L-Aspartic aicd sodium | 1,4-Cineole | Mebeverine hydrochloride | Amitriptyline hydrochloride | Riluzole | Benzocaine | Nefopam hydrochloride |
| Related Compound Libraries | 经典已知活性库 | 疼痛相关化合物库 | 神经信号分子库 | 膜蛋白靶向化合物库 | 神经保护化合物库 | 抑制剂库 | 抗心血管疾病化合物库 | 已知活性化合物库 | 离子通道库 | 抗癌化合物库 |
United States
