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Biochem/physiol Actions
Cell-permeable N,N′-bis(acyloxymethyl carbamate) prodrug of the anaphase-promoting complex (APC) inhibitor Nα-p-Tosyl-L-arginine methyl ester (TAME).
proTAME is a cell-permeable N,N′-bis(acyloxymethyl carbamate) prodrug of the anaphase-promoting complex (APC) inhibitor Nα-p-Tosyl-L-arginine methyl ester (TAME). Upon entering cells, proTAME (12 μM) is effectively converted by cellular esterases to TAME, which in turn inactivates the spindle assembly checkpoint (SAC) by blocking APC-dependent proteolysis, causing prolonged mitotic duration at low doses (780 nM - 3 μM in HeLa cells, 6 μM in hTERT-RPE1 cells) or mitotic arrest and cell death at high doses (12 μM in HeLa cells). Note: proTAME is not active in some cells (e.g. MCF10A, due to the lack of esterase activity required for proTAME activation.
Disclaimer
Hygroscopic
| Quality Segment | 100 |
| assay | ≥90% (HPLC) |
| form | (Powder or solid or crytals or semi-solid) |
| storage condition | desiccated |
| color | colorless to yellow |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | -10 to -25°C |
| SMILES string | O=C(CC1=CC=CC=C1)OCOC(/N=C(NC(OCOC(CC2=CC=CC=C2)=O)=O)\NCCC[C@H](NS(C3=CC=C(C=C3)C)(=O)=O)C(OC)=O)=O |
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¥ 3372.68
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¥ 8137.12
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¥ 4476.05
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¥ 75435.65
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