2. Signaling Pathways
  3. Immunology/Inflammation
  4. PSMA

PSMA

Prostate-specific membrane antigen

PSMA is a transmembrane protein that anchores to the cell membrane through its transmembrane region and is mainly expressed in prostate epithelial cells but also exists in other tissues. PSMA exhibits glutamate-preferring carboxypeptidase activity that hydrolyzes polyglutamylated folic acid to release folic acid monomers. PSMA mediates the endocytosis on the cell surface. PSMA acts as an angiogenesis marker in cancer cells. PSMA can be used as a diagnostic marker for prostate cancer, and for detection of invasiveness and metastatic ability of the tumor[1].

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-158125
    PSMA binder-2
    PSMA binder-2 is a ligand for PSMA and can be used to synthesize Ac-PSMA-trillium. Ac-PSMA-trillium is a suitable PSMA-targeting compound with improved PSMA binding properties and pharmacokinetic properties. PSMA ligands have different biological applications after being modified with different radioactive isotopes. If labeled with 111In, it can be used as DOTA chelating agent and imaging agent. Or labeled with 225Ac as a Macropa chelator for targeted radionuclide therapy (TRT) in the study of metastatic castration-resistant prostate cancer (mCRPC).
    PSMA binder-2
  • HY-163683
    EB-PSMA-617
    		Inhibitor
    EB-PSMA-617 is a modified form of PSMA-617 that has enhanced pharmacokinetic properties by conjugating it to Evans Blue (EB) to extend its circulation half-life to improve prostate tumor uptake and radiotherapy efficacy. In preclinical studies using PC3-PIP-loaded mice, EB-PSMA-617 demonstrated prolonged blood half-life, increased accumulation in PSMA-positive tumors, and successful tumor elimination with lower radioactivity.
    EB-PSMA-617
  • HY-139670
    PSMA–DA1
    PSMA–DA1 may be a useful PSMA-targeting radiotheranostic agent.
    PSMA–DA1
  • HY-P10055
    PSMA targeting peptide
    PSMA-1 is a PSMA targeting peptide (GRFLTGGTGRLLRIS) and can be used for for targeted delivery of glucose-regulated protein (GRP)-silencing siRNAs in PCa cells. PSMA-1 is selected and polyarginine sequences R6 or R9 were added at the C terminus to generate the CTPs. FITC labeling of the peptide with an aminohexanoic acid (Ahx) linker at the N terminus produced FITC-PSMA-1, to track PSMA binding on PCa cells.
    PSMA targeting peptide
  • HY-163608
    Ac-macropa
    Ac-macropa is a PSMA-targeted Actinium-225 Conjugate, and can be used for study of prostate cancer.
    Ac-macropa
  • HY-129615
    MIP-1072
    		Inhibitor
    MIP-1072 is a small molecule specific prostate-specific membrane antigen (PSMA) inhibitor. MIP-1072 inhibits the glutamate carboxypeptidase activity of PSMA with an Ki value of 4.6 nM. MIP-1072 is promising for research of prostate cancer.
    MIP-1072
  • HY-123733A
    MIP-1095 TFA
    		99.76%
    MIP-1095 (RPS-001) TFA is a potent inhibitor of PSMA with good biodistribution and efficient targeting of tumor lesions. In applications, MIP-1095 TFA will be isotopically labeled (131I labeled) as an imaging probe to indicate tumor progression. And 131I-MIP-1095 showed higher renal uptake in mice.
    MIP-1095 TFA
  • HY-P99554
    Topsalysin
    Topsalysin is a PSA-activated protoxin, a pore-forming protein (synthetic proaerolysin) fusion protein with human prostate-specific antigen. Topsalysin has tumor suppression effect in mice modle.
    Topsalysin
  • HY-123733
    MIP-1095
    		Inhibitor
    MIP-1095 potently inhibits the glutamate carboxypeptidase activity of PSMA (Ki =0.24 nM).
    MIP-1095
  • HY-163196
    PSMA-IN-4
    		Inhibitor
    PSMA-IN-4 (compound 9) is a potent inhibitor of PSMA, with the IC50 value of 1.2 μM.
    PSMA-IN-4
  • HY-P10743
    BQ7876
    BQ7876 is a probe targeting prostate-specific membrane antigen (PSMA) that contains a DOTA chelator. BQ7876, after being radiolabeled with radionuclide (177Lu), functions in both radionuclide imaging and tumor cell destruction by specifically binding to PSMA. BQ7876 shows potential for research in the field of metastatic castration-resistant prostate cancer (mCRPC). BQ7876 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
    BQ7876
  • HY-P5990
    Prostate Specific Antigen Substrate
    Prostate Specific Antigen Substrate is a prostate specific antigen (PSA) fluorescent substrate. Prostate Specific Antigen Substrate can be used for detect enzymatic activity of PSA.
    Prostate Specific Antigen Substrate
  • HY-149297
    PSMA-IN-1
    		Inhibitor
    PSMA-IN-1 (compound 23) is an inhibitor of PSMA with a Ki value of 2.49 nM. PSMA-IN-1 inhibits tumor growth with high selectivity and specificity in PSMA+ xenograft models. PSMA-IN-1 is a NIR probe (λEX: 620 nm; λEM: 670 nm) used for tumor disappearance. PSMA-IN-1 can be used for research on prostate cancer.
    PSMA-IN-1
  • HY-P10744
    BQ7859
    BQ7859 is a probe targeting PSMA that contains a NOTA chelator and demonstrates excellent imaging performance. BQ7859 can be labeled with various radionuclides, such as 68Ga, 18F, 55Co, and 111In. In a mouse prostate cancer xenograft model, BQ7859 (labeled with 111In) efficiently accumulates in tumor regions in a PSMA-dependent manner and provides high-contrast tumor imaging. BQ7859 shows potential for research in prostate cancer imaging, particularly in positron emission tomography (PET) and single-photon emission computed tomography (SPECT). BQ7859 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
    BQ7859
  • HY-161626
    PSMA binder-3
    		Chemical
    PSMA binder-3 is a binder of PSMA.
    PSMA binder-3
  • HY-148152
    PSMA I&S
    PSMA I&S is a precursor of the 99mTc-labeled PSMA-targeting ligand.
    PSMA I&S
  • HY-162779
    CDD-3290
    		Inhibitor
    CDD-3290 (Compound 20) is a prostate-specific antigen (PSA) inhibitor with a Ki value of 216 nM. CDD-3290 also inhibits α-chymotrypsin and elastase.
    CDD-3290
  • HY-158119A
    PSMA-trillium
    PSMA-trillium is a PSMA targeting compound, consisting of a PSMA targeting molecule (PSMA binder), a Macropa chelating molecule, and a group that regulates pharmacokinetics (PK modifier). PSMA-trillium is a non-radioactive form of Actinium-225-PSMA-Trillium (BAY 3563254) with improved PSMA targeting and pharmacokinetic properties. PSMA-trillium can bind Ac through the Macropa chelating molecule, or the radioactive isotope 225Actinium. Actinium-225-PSMA-Trillium is a potent inhibitor of metastatic castration-resistant prostate cancer (mCRPC).
    PSMA-trillium
  • HY-172366
    BQ0413
    BQ0413 exhibits good affinity to PSMA with a KD of 89 pM. BQ0413 exhibits good uptake and internalization property with an internalization rate of 44% in PC3-pip cell. BQ0413 can be used as tumor imaging agent when labeled with 99mTc.
    BQ0413
  • HY-16215
    Mipsagargin
    		Inhibitor
    Mipsagargin (G-202) is a novel thapsigargin-based targeted proagent consisting of a prostate-specific membrane antigen (PSMA)-specific peptide coupled to an analog of the potent sarcoplasmic/endoplasmic reticulum calcium adenosine triphosphatase (SERCA) pump inhibitor Thapsigargin (HY-13433). Mipsagargin is activated by PSMA-mediated cleavage of an inert masking peptide. Mipsagargin has the potential for refractory, advanced or metastatic solid tumours research.
    Mipsagargin
Cat. No. Product Name / Synonyms Application Reactivity