| Field | Specification |
|---|---|
| Alternative names | GPI-5693 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C8H14O4S |
| Purity | |
| SMILES | |
| Form | Oil |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
2-MPPA, also known as GPI-5693, is an orally active, selective inhibitor of glutamate carboxypeptidase II (GCP II; PSMA), with an IC50 of 90 nM[1][2]. It is supplied as a colorless to light yellow oil (C8H14O4S, MW 206.26) at 98.0% purity.
Physical & Chemical Properties
| CAS Number | 254737-29-6 |
|---|---|
| Molecular Formula | C8H14O4S |
| Molecular Weight | 206.26 g/mol |
| Purity | 98.0% |
| Appearance | Oil |
| Color | Colorless to light yellow |
| SMILES | O=C(O)C(CCCS)CCC(O)=O |
| Signaling Pathway | Metabolic Enzyme/Protease |
| Solubility | In Vitro: DMSO: 100 mg/mL (484.82 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Pure form: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target
IC50: 90 nM (GCP II)[2]
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
[2]. She Y, et al. 2-MPPA, a selective inhibitor of PSMA, delays prostate cancer growth and attenuates taxol-induced neuropathy in mice. Journal of Clinical Oncology, 2005, 23(16_suppl): 8054-8054.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 100 mg/mL (484.82 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (12.12 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.5 mg/mL (12.12 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (12.12 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vivo
2-MPPA at 10, 30, or 100 mg/kg significantly reduces Dizocilpine (0.1 mg/kg)-induced prepulse inhibition (PPI) deficits in mice in a dose-dependent manner. Pretreatment with the antagonist LY341495 (1.0 mg/kg), which is selective for group II metabotropic glutamate receptors (mGluR), significantly counteracts the effect of 2-MPPA on dizocilpine-induced PPI deficits[1]. At 30 mg/kg, 2-MPPA significantly prevents the SNCV deficit induced by taxol at both 5 and 25 mg/kg, by 96.3 ± 4.4% and 98.3± 11.6%, respectively[2]. At 10 mg/kg, 2-MPPA suppresses tumor growth by 70% in the high expressor PSMA model CWR22RS[2].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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