| Bioactivity | 2-MPPA (GPI-5693) is an orally active and selective glutamate carboxypeptidase II (GCP II; PSMA) inhibitor with an IC50 of 90 nM[1][2]. | ||||||||||||
| Target | IC50: 90 nM (GCP II) | ||||||||||||
| In Vivo | 2-MPPA (10, 30 or 100 mg/kg) significantly attenuates Dizocilpine (HY-15084B) (0.1 mg/kg)-induced prepulse inhibition (PPI) deficits in mice, in a dose dependent manner. The efficacy of 2-MPPA on dizocilpine-induced PPI deficits is significantly antagonized by pretreatment with the selective group II metabotropic glutamate receptor (mGluR) antagonist LY341495 (HY-70059) (1.0 mg/kg)[1].2-MPPA (30 mg/kg) significantly prevents the deficit in SNCV induced by both 5 and 25 mg/kg taxol by 96.3 ± 4.4% and 98.3± 11.6% respectively[2].2-MPPA (10 mg/kg) inhibits tumor growth in the high expressor PSMA model CWR22RS by 70%[2]. | ||||||||||||
| Name | 2-MPPA | ||||||||||||
| CAS | 254737-29-6 | ||||||||||||
| Formula | C8H14O4S | ||||||||||||
| Molar Mass | 206.26 | ||||||||||||
| Appearance | Oil | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Takatsu Y, et al. Orally active glutamate carboxypeptidase II inhibitor 2-MPPA attenuates dizocilpine-induced prepulse inhibition deficits in mice. Brain Res. 2011 Jan 31;1371:82-6. [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. |