PSMA

Zadavotide guraxetan is a potent inhibitor of prostate-specific membrane antigen (PSMA). This compound is utilized in SPECT/CT imaging, providing valuable insights into the cellular profiles of triple-negative breast cancer and prostate cancer. Its application in radionuclide studies underscores its significance in cancer research and therapeutic development.

Tert-Butyl-DCL is a potent inhibitor of Prostate-Specific Membrane Antigen (PSMA), a crucial target in prostate cancer research. Its inhibition of PSMA activity makes Tert-Butyl-DCL a valuable tool for studying the molecular mechanisms of prostate cancer progression and therapeutic interventions. This compound is ideal for applications in cancer biology and the development of PSMA-targeted therapies.

EC0652 is a potent PSMA imaging agent designed for SPECT imaging applications. It enables the detection and visualization of prostate-specific membrane antigen (PSMA) expression, making it a valuable tool in research focused on metastatic castration-resistant prostate cancer. This compound enhances the understanding of tumor biology and may aid in the development of targeted therapeutic strategies.

Flotufolastat is a prostate-specific membrane antigen (PSMA) modulator that serves as a radiodiagnostic agent for imaging prostate cancer. This compound is instrumental in enhancing the detection and characterization of prostate cancer lesions. Flotufolastat is valuable for research applications focused on prostate cancer and other malignancies associated with PSMA expression.

PSMA binder-1 is a potent ligand targeting Prostate-Specific Membrane Antigen (PSMA). It facilitates the synthesis of PSMA-targeting molecules, such as Ac-PSMA-trillium, providing a valuable tool for research in prostate cancer diagnosis and therapy. This compound is essential for studies focused on imaging and targeted treatment strategies aimed at PSMA-expressing tumors.

Piflufolastat is a positron emission tomography (PET) imaging agent that specifically targets prostate-specific membrane antigen (PSMA). Labeled with fluorine-18, Piflufolastat F-18 serves as a diagnostic tool for the visualization of prostate cancer. Its application in molecular imaging enables enhanced detection and monitoring of prostate malignancies, supporting research and clinical decision-making in oncology.

PSMA-azide is a ligand targeting prostate-specific membrane antigen (PSMA). It effectively inhibits PSMA-dependent hydrolysis of N-acetylaspartylglutamic acid (NAAG) with an IC50 of 9 nM and a Ki of 1 nM, making it a valuable tool for studying PSMA-related pathways. Additionally, PSMA-azide features an azide moiety, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition reactions (CuAAc) with alkynyl-containing molecules, facilitating various biochemical labeling and conjugation applications in research.

Glu-urea-Glu-NHS ester is an activated N-hydroxysuccinamide (NHS) ester of the Glu-urea-Glu compound. It serves as a versatile active intermediate in the synthesis of small-molecule inhibitors targeting prostate-specific membrane antigen (PSMA). This reagent is valuable for developing imaging agents, such as PSMAi-PEG conjugates, and enhancing the efficacy of targeted drug delivery systems in research applications.

GCPII-IN-1 is a potent inhibitor of the gene carboxypeptidase II (GCPII), also recognized as prostate-specific membrane antigen (PSMA), with a Ki value of 44.3 nM. This compound is primarily utilized in the research of prostate cancer, facilitating studies aimed at understanding tumor biology and developing potential therapeutic strategies. Its mechanism of action makes it a valuable tool for elucidating the role of GCPII in cancer progression.

GCPII-IN-1 TFA is a selective inhibitor of GCPII (glutamate carboxypeptidase II), also known as prostate-specific membrane antigen (PSMA), exhibiting a Ki value of 44.3 nM. This compound is instrumental in the investigation of prostate cancer, facilitating studies on the modulation of GCPII activity and its potential therapeutic applications in oncology. Researchers can utilize GCPII-IN-1 TFA to explore mechanisms of tumor growth and treatment resistance in prostate cancer models.

Prostate Specific Antigen Substrate is a fluorescent substrate utilized for the detection of enzymatic activity associated with prostate specific antigen (PSA). This reagent enables researchers to effectively measure PSA activity, aiding in the study of prostate cancer and other related conditions. Its application in various assays facilitates enhanced understanding of PSA's role in oncology research.

EC1169 is a PSMA-targeted maytansinoid conjugate that selectively binds to prostate-specific membrane antigen (PSMA). This compound delivers the cytotoxic maytansinoid B hydrazide payload directly to PSMA-positive tumor cells, demonstrating significant antitumor activity while sparing PSMA-negative cells. In preclinical models, EC1169 promotes complete recovery in mice with PSMA-positive tumors, exhibiting a favorable safety profile without inducing body weight loss or major organ damage. This reagent is valuable for research focused on prostate cancer and other PSMA-expressing malignancies.

PNT2001 is a potent prostate-specific membrane antigen (PSMA) ligand, exhibiting an IC50 of 3.1 nM. This compound enhances cellular internalization, making it a valuable tool for targeting PSMA in prostate cancer research. Additionally, PNT2001 can be labeled with 177Lu and 225Ac, facilitating the development of radiolabeled therapies for prostate cancer treatment and diagnostic applications.

PSMA I&S is a key precursor for the synthesis of 99mTc-labeled PSMA-targeting ligands. This compound facilitates the generation of radiolabeled agents that selectively bind to the prostate-specific membrane antigen (PSMA), making it valuable for imaging and therapeutic applications in prostate cancer research. Its role in the development of novel radiopharmaceuticals enhances the ability to study PSMA expression in various biological contexts.

Zopocianine is a near-infrared optical probe targeting prostate-specific membrane antigen (PSMA). This compound selectively binds to PSMA expressed on the surface of cancer cells, facilitating receptor-mediated endocytosis and subsequent accumulation within acidic endosomes. Zopocianine is particularly effective for visualizing small tumors, primary prostate tumors, and locoregional metastases, making it a valuable tool in fluorescence-guided surgery for achieving negative tumor margins. Its applications are primarily in the field of prostate cancer research.

PSMA binder-2 is a potent ligand targeting Prostate-Specific Membrane Antigen (PSMA), facilitating the synthesis of Ac-PSMA-trillium, which exhibits enhanced binding and pharmacokinetic properties. This versatile compound can be modified with various radioactive isotopes for different applications; when labeled with 111In, it serves effectively as a DOTA chelating and imaging agent. Alternatively, when conjugated with 225Ac, it acts as a Macropa chelator, proving valuable for targeted radionuclide therapy (TRT) in the research of metastatic castration-resistant prostate cancer (mCRPC).

PSMA–DA1 is a radioactive inhibitor targeting Prostate-Specific Membrane Antigen (PSMA). It serves as a promising radiotheranostic agent for imaging and treating PSMA-expressing tumors. Its specificity for PSMA makes it a valuable tool in the research of prostate cancer diagnosis and therapy, enabling the development of effective targeted treatment strategies.

MIP-1072 is a selective inhibitor of prostate-specific membrane antigen (PSMA) that targets the enzyme's glutamate carboxypeptidase activity. With a Ki value of 4.6 nM, MIP-1072 demonstrates significant potency in inhibiting PSMA, making it a valuable tool in prostate cancer research. Its application is particularly relevant for studies focused on the role of PSMA in tumor progression and targeted therapies.

Topsalysin is a PSA-activated protoxin that functions as a pore-forming protein, specifically a synthetic proaerolysin fusion protein modified to target human prostate-specific antigen (PSA). It demonstrates significant tumor-suppressive effects in mouse models, making it a valuable tool for studying prostate cancer biology. Its unique mechanism allows for selective targeting of PSA-expressing tissues, providing insights into therapeutic approaches for prostate cancer treatment.

PSMA Ligand 1 is a potent PSMA ligand that exhibits an IC50 of 26.74 nM. This compound has been radiolabeled with [18F], making it a suitable candidate for use as a PET tracer in imaging studies. Its primary applications include aiding in the diagnosis and monitoring of prostate cancer, facilitating innovative research in oncology and molecular imaging.

PDI2 (PSMA-DOTA-PEI2) is a prostate-specific membrane antigen (PSMA) ligand that functions as a tumor retention agent and imaging agent while reducing renal uptake. It selectively binds to PSMA on prostate cancer cells, facilitating entry through clathrin-dependent endocytosis, which results in increased tumor retention and decreased renal accumulation. PDI2 is valuable for research in prostate cancer and castration-resistant metastatic prostate cancer, particularly in the context of SPECT diagnostic imaging and radiotheranostics.

MIP-1095 is a potent inhibitor of prostate-specific membrane antigen (PSMA), specifically targeting its glutamate carboxypeptidase activity with a Ki of 0.24 nM. This compound is valuable in research applications focused on prostate cancer, facilitating studies on PSMA's role in tumor progression and its potential as a therapeutic target. MIP-1095 is essential for the development of PSMA-targeted diagnostics and therapeutics.

PSMA-IN-4 is a potent inhibitor of prostate-specific membrane antigen (PSMA), exhibiting an IC50 value of 1.2 μM. This compound effectively interferes with PSMA activity, making it a valuable tool in research focused on prostate cancer diagnostics and therapeutics. Its specificity and potency support investigations into PSMA's role in tumor biology and its potential as a therapeutic target.

Capromab is a monoclonal antibody targeting the intracellular domain of prostate-specific membrane antigen (PSMA). It exhibits specificity for necrotic cells with compromised membranes and does not undergo internalization upon binding. Capromab is utilized in research focused on prostate cancer, aiding in studies related to tumor progression and targeted therapies.

PSMA Ligand 3 is a ligand specifically targeting Prostate-Specific Membrane Antigen (PSMA). Its primary function is to bind to PSMA, facilitating the detection and imaging of prostate cancer cells. This compound is valuable in cancer research, particularly in the study of prostate cancer diagnostics and therapy.

PSMA binder-3 is a selective binder for Prostate-Specific Membrane Antigen (PSMA), a key target in prostate cancer research. This high-affinity ligand exhibits strong binding capabilities that facilitate the study of PSMA's role in tumor biology and therapeutic targeting. It is an essential tool for applications in imaging and drug development related to prostate cancer.

PSMA-trillium is a PSMA-targeting compound that features a PSMA binder, a Macropa chelating molecule, and a pharmacokinetics modifier. This non-radioactive derivative of Actinium-225-PSMA-Trillium (BAY 3563254) offers enhanced PSMA targeting and optimized pharmacokinetic properties. PSMA-trillium effectively binds to Ac via the Macropa chelator and serves as a potent inhibitor of metastatic castration-resistant prostate cancer (mCRPC). It is a valuable tool for research into targeted therapies for prostate cancer.

BQ0413 is a potent PSMA tracer with a dissociation constant (KD) of 89 pM, demonstrating strong affinity for the prostate-specific membrane antigen. This compound exhibits efficient cellular uptake and a notable internalization rate of 44% in PC3-pip cells, making it suitable for research applications in tumor imaging. When radiolabeled with 99mTc, BQ0413 serves as an effective imaging agent for prostate cancer in preclinical studies.

PSMA-N5 is a potent PSMA ligand, exhibiting a Ki value of 0.71 nM. This compound serves as a PET radiotracer specifically for imaging prostate cancer, facilitating the visualization of tumors. PSMA-N5 is valuable for research applications in prostate cancer and other malignancies associated with prostate-specific membrane antigen.

PSMA-IN-2 is a potent inhibitor of Prostate-Specific Membrane Antigen (PSMA) with a Ki value of 1.07 nM. This compound exhibits promising in vivo near-infrared (NIR) imaging properties at an emission wavelength of 1088 nm and an excitation wavelength of 808 nm. PSMA-IN-2 is particularly applicable in NIRII image-guided tumor resection surgeries in models of PSMA-positive tumors, making it a valuable tool for cancer research and therapeutic interventions.

PSMA-IN-3 is a high-affinity inhibitor of Prostate-Specific Membrane Antigen (PSMA), demonstrating an IC50 value of 13 nM. This compound is particularly relevant for the development of 18F-labeled radioligands for positron emission tomography (PET) imaging to detect PSMA expression in prostate cancer. Researchers can utilize PSMA-IN-3 for studies aimed at advancing diagnostic imaging and therapeutic strategies in oncology.

DCFBC is a potent prostate-specific membrane antigen (PSMA) inhibitor, primarily utilized for small animal positron emission tomography (PET) imaging applications. Labeled with fluorine-18, [18F]DCFBC demonstrates preferential uptake in PSMA-expressing tumors, particularly in PIP tumors, while showing minimal uptake in FLU tumors. Additionally, while high accumulation in the kidneys and bladder is observed, the washout of radioactivity is faster compared to PIP tumors. This specificity positions [18F]DCFBC as a valuable tool for studying prostate cancer and assessing PSMA-targeted therapies.

(R)-Zadavotide guraxetan is a potent inhibitor of prostate-specific membrane antigen (PSMA), exhibiting significant antitumor activity. It is primarily utilized in research focused on prostate cancer, contributing to the understanding of targeted therapeutic approaches. This compound serves as a valuable tool for investigating the role of PSMA in cancer biology and evaluating efficacy in preclinical studies.

PSMA-MAL-5 is a prostate-specific membrane antigen (PSMA) ligand that covalently binds to Cys466 of the PSMA protein. This compound demonstrates significant biological activity, including high radiostability and tumor uptake when labeled with 177Lu and 225Ac. PSMA-MAL-5 is also effective in inhibiting tumor growth, making it suitable for applications in SPECT/CT imaging and radionuclide therapy for prostate cancer.

PSMA precursor-1 is a key intermediate in the synthesis of prostate-specific membrane antigen (PSMA) ligands and fluorescent probes. It is utilized for the detection of PSMA in prostate cancer cell lines, specifically LNCaP and PC3. This compound plays a significant role in the development of targeted imaging agents and therapeutic strategies for prostate cancer research.