GCPII-IN-1 TFA is a peptide-like inhibitor scaffold targeting glutamate carboxypeptidase II in biochemical assays. Carboxylate and amide groups mimic key substrate interactions within the active site. Researchers assess binding constants, catalytic suppression, and structural complementarity by enzymology and docking. Applications include enzyme-mechanism elucidation, inhibitor-design research, and neurochemical pathway studies.
CAT No: R2721
CAS No:1269794-89-9
Synonyms/Alias:GCPII-IN-1 TFA;GCPII-IN-1 (TFA);1269794-89-9;(2S)-2-[[(1S)-5-amino-1-carboxypentyl]carbamoylamino]pentanedioic acid;2,2,2-trifluoroacetic acid;EX-A10938;HY-139840A;DA-73673;MS-27735;CS-0255869;E72657;(((S)-5-Amino-1-carboxypentyl)carbamoyl)-L-glutamic acid compound with 2,2,2-trifluoroacetic acid (1:1);
Gcpii-IN-1 tfa is a small-molecule biochemical inhibitor specifically designed to target glutamate carboxypeptidase II (GCPII), an enzyme also known as prostate-specific membrane antigen (PSMA) or N-acetylated-alpha-linked acidic dipeptidase (NAALADase). As a potent and selective GCPII inhibitor, this compound plays a significant role in neurochemical and cancer-related research, particularly where the modulation of glutamatergic neurotransmission or PSMA activity is of interest. Its trifluoroacetate (tfa) salt form enhances solubility and handling for laboratory applications, making it a valuable tool for probing GCPII-related pathways and mechanisms in preclinical settings.
Enzyme Inhibition Studies: GCPII-IN-1 tfa is widely utilized in biochemical assays to investigate the inhibitory kinetics and selectivity of compounds targeting GCPII. By serving as a reference inhibitor, it enables researchers to dissect the molecular interactions governing GCPII's active site and to benchmark the potency of novel analogs. Such studies are fundamental for elucidating the structure-activity relationships that underpin the design of next-generation GCPII inhibitors for research purposes.
Neurotransmitter Regulation Research: The compound is instrumental in studies examining the regulation of glutamatergic signaling, particularly through its effect on the hydrolysis of N-acetylaspartylglutamate (NAAG) to glutamate. By blocking GCPII activity, GCPII-IN-1 tfa allows researchers to modulate synaptic glutamate concentrations in experimental systems, providing insight into the enzyme's role in excitatory neurotransmission, synaptic plasticity, and neuroprotection. This capability is especially valuable in models of neurological disorders where glutamate dysregulation is implicated.
Cancer Biology Investigations: Due to the overexpression of PSMA/GCPII in prostate cancer and certain other malignancies, this inhibitor is frequently employed in oncology research to study PSMA-mediated signaling and cellular processes. By selectively inhibiting the enzyme, investigators can delineate its contributions to tumor growth, angiogenesis, and cellular uptake mechanisms. Such studies support the development of new diagnostic and research tools targeting PSMA in cancer biology.
Radioligand Binding and Imaging Probe Development: GCPII-IN-1 tfa is often used in competitive binding assays to validate the specificity and affinity of radiolabeled ligands or imaging agents designed for PSMA-targeted applications. Its high affinity for GCPII makes it an effective competitor in displacement studies, facilitating the optimization of molecular imaging probes and the interpretation of in vitro and ex vivo binding data. These applications are critical for advancing the development of research reagents for molecular imaging and tracer validation.
Drug Discovery and Lead Optimization: In the context of early-stage drug discovery, the compound provides a robust tool for screening chemical libraries and optimizing lead compounds that modulate GCPII activity. Its well-characterized inhibitory profile enables medicinal chemists to assess the efficacy, selectivity, and off-target effects of new molecules, supporting the iterative process of lead refinement. By incorporating GCPII-IN-1 tfa into screening platforms, research teams can accelerate the identification of promising candidates for further preclinical evaluation.
Through its targeted inhibition of GCPII, GCPII-IN-1 tfa offers a multifaceted platform for advancing research across enzymology, neurobiology, oncology, and chemical biology. Its application versatility and biochemical specificity make it an indispensable resource for laboratories focused on unraveling the complexities of GCPII function and its broader implications in health and disease models.
If you have any peptide synthesis requirement in mind, please do not hesitate to contact us at . We will endeavor to provide highly satisfying products and services.
Creative Peptides is a trusted CDMO partner specializing in high-quality peptide synthesis, conjugation, and manufacturing under strict cGMP compliance. With advanced technology platforms and a team of experienced scientists, we deliver tailored peptide solutions to support drug discovery, clinical development, and cosmetic innovation worldwide.
From custom peptide synthesis to complex peptide-drug conjugates, we provide flexible, end-to-end services designed to accelerate timelines and ensure regulatory excellence. Our commitment to quality, reliability, and innovation has made us a preferred partner across the pharmaceutical, biotechnology, and personal care industries.
Read More