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AKR1C3+Inhibitors

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-19903
    ASP-9521
    3 Publications Verification

    17β-HSD Cancer
    ASP-9521 is a potent, selective and orally available AKR1C3 inhibitor with an IC50 of 11 nM for human AKR1C3.
    ASP-9521
  • HY-109154

    Aldose Reductase Inflammation/Immunology
    Obafistat is a potent aldo-keto reductase AKR1C3 inhibitor with an IC50 of 1.2 nM for human AKR1C3 (patent WO2017202817A1, example 4) .
    Obafistat
  • HY-138557

    17β-HSD Cancer
    AKR1C3-IN-4 is a potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitor with an IC50 of 0.56 μM. AKR1C3-IN-4 has the potential for castrate resistant prostate cancer (CRPC) research .
    AKR1C3-IN-4
  • HY-152189

    17β-HSD Cancer
    S19-1035 is a highly potent and specific aldo-keto reductase 1C3 (AKR1C3) inhibitor. S19-1035 inhibits AKR1C3 with an IC50 value of 3.04 nM. S19-1035 can be used for the research of tumor .
    S19-1035
  • HY-176084

    Aldose Reductase Cancer
    RJG-2051 is a selective covalent aldo-keto reductase family 1 member C3 (AKR1C3) inhibitor with an IC50 value of 13 nM. RJG-2051 interferes with the metabolic process of substrates such as androgens, estrogens, and prostaglandins by AKR1C3. RJG-2051 is promising for research of cancers .
    RJG-2051
  • HY-156701

    Aldose Reductase Metabolic Disease Endocrinology
    BAY-1128688 is a potent, orally active and selective AKR1C3 inhibitor with IC50 < 2 nM. BAY-1128688 shows high selectivity over related AKR1C enzymes (1C1, 1C2, 1C4) and AKR1D1. BAY-1128688 exhibits no relevant activity at major nuclear hormone receptors. BAY-1128688 reduces endometriotic lesions in the marmoset monkey endometriosis model. BAY-1128688 can be used for endometriosis research .
    BAY-1128688
  • HY-171115

    GPR84 Aldose Reductase Metabolic Disease
    Pyrone-211 is a potent GPR84 agonist and AKR1C3 inhibitor. Pyrone-211 participates in an expanded polyamine pathway .
    Pyrone-211
  • HY-155502

    Aldose Reductase Cancer
    AKR1C3-IN-10 (compound 5r) is a selective AKR1C3 inhibitor (IC50=51 nM). AKR1C3-IN-10 shows good activity in a prostate cancer xenograft model .
    AKR1C3-IN-10
  • HY-161839

    Aldose Reductase Cancer
    AKR1C2/3-IN-1 (compound 3a) is a potent AKR1C2 and AKR1C3 inhibitor with IC50 values of 90, 50 nM, respectively. AKR1C2/3-IN-1 can be used as a radiation sensitizer and as a potentiator of chemotherapy cytotoxicity .
    AKR1C2/3-IN-1
  • HY-146573

    Aldose Reductase 17β-HSD Cancer
    AKR1C3-IN-6 (Compound 1) is a potent, selective AKR1C3 inhibitor with IC50 values of 0.31 μM and 73.23 μM against AKR1C3 and AKR1C2, respectively. AKR1C3-IN-6 shows antitumor activity .
    AKR1C3-IN-6
  • HY-163609

    PROTACs Aldose Reductase Cancer
    PROTAC AKR1C3 degrader-1 (compound 5) is a potent AKR1C3 PROTAC degrader. PROTAC AKR1C3 degrader-1 decreases the protein expression of AKR1C3, AKR1C1/2, and ARv7. PROTAC AKR1C3 degrader-1 has the potential for the research of prostate cancer. (Blue:ubiquitin E3 ligase cereblon ligand (HY-A0003), Black: linker (HY-163647); Pink: AKR1C3 inhibitor (HY-163610)) .
    PROTAC AKR1C3 degrader-1
  • HY-150646

    Aldose Reductase Cancer
    S07-2009 is a potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitor with an IC50 value of 0.20 μM .
    S07-2009
  • HY-W024692

    Indometacin methylester

    17β-HSD Cancer
    Indomethacin methylester (Compound 10; Indometacin methylester) is a potent and selective AKR1C3 inhibitor with an IC50 value of 5.67 μM. Indomethacin methylester is promising for research of postate cancer .
    Indomethacin methylester
  • HY-150648

    Aldose Reductase Cancer
    S07-2008 is a selective aldo-keto reductase family 1 member C3 (AKR1C3) inhibitor with an IC50 of 0.16 μM. S07-2008 shows anticancer activities .
    S07-2008
  • HY-19903R

    17β-HSD Reference Standards Cancer
    ASP-9521 (Standard) is the analytical standard of ASP-9521. This product is intended for research and analytical applications. ASP-9521 is a potent, selective and orally available AKR1C3 inhibitor with an IC50 of 11 nM for human AKR1C3.
    ASP-9521 (Standard)
  • HY-163610

    Ligands for Target Protein for PROTAC Aldose Reductase Cancer
    AKR1C3-IN-13 (Compound 4) is an AKR1C3 inhibitor. AKR1C3-IN-13 degrades AKR1C3 in prostate cancer cells .
    AKR1C3-IN-13
  • HY-146574

    Aldose Reductase 17β-HSD Cancer
    AKR1C3-IN-7 (Compound 13) is a potent, selective AKR1C3 inhibitor with an IC50 of 0.19 μM. AKR1C3-IN-7 shows antitumor activity .
    AKR1C3-IN-7
  • HY-146575

    Aldose Reductase 17β-HSD Cancer
    AKR1C3-IN-8 (Compound 5) is a potent, selective AKR1C3 inhibitor with an IC50 of 0.069 μM. AKR1C3-IN-8 shows antitumor activity .
    AKR1C3-IN-8
  • HY-163323

    Aldose Reductase Cancer
    AKR1C3-IN-12 (compound 2j) is an aldo-keto reductase 1C3 (AKR1C3) inhibitor with an IC50 of 27 nM. AKR1C3-IN-12 enhances the efficacy of Gemcitabine and Cisplatin in bladder cancer .
    AKR1C3-IN-12
  • HY-150650

    Aldose Reductase Cancer
    S07-2001 is a potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitor with an IC50 value of 2.08 μM. S07-2001 enhances the activity of Doxorubicin against cancer cells. S07-2001 has potential as a chemotherapeutic potentiator for cancer agent resistance .
    S07-2001
  • HY-155035

    17β-HSD Cancer
    S07-1066 is an aldo-keto reductase 1C3 (AKR1C3) inhibitor, synergizing doxorubicin (DOX) cytotoxicity. S07-1066 selectively blocks AKR1C3-mediated reduction of DOX, and reverses the DOX resistance in overexpressing AKR1C3 cells .
    S07-1066
  • HY-150649

    17β-HSD Cancer
    S07-2005 racemic is a potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitor with an IC50 value of 0.13 μM and 0.75 μM for AKR1C3 and AKR1C4, respectively. S07-2005 racemic has potential as a chemotherapeutic potentiator for cancer agent resistance .
    S07-2005 (racemic)
  • HY-173453

    Aldose Reductase Apoptosis Cancer
    AKR1C3-IN-15 (compound 30) is a potent and selective AKR1C3 inhibitor with an IC50 of 5 nM. AKR1C3-IN-15 enhances Sorafenib (HY-10201)-induced ROS generation, promoted apoptosis, and restored sorafenib sensitivity in HCC models both in vitro and in vivo .
    AKR1C3-IN-15
  • HY-157810

    Aldose Reductase Cancer
    AKR1C3-IN-11 (Compound 6e) is a Aldo-keto reductase 1C3 (AKR1C3) inhibitor with an IC50 of 2.0 μM. AKR1C3-IN-11 inhibit cell proliferation in combination with abiraterone (HY-70013). AKR1C3-IN-11 can be used for the research of prostate cancer .
    AKR1C3-IN-11
  • HY-163784

    Aldose Reductase Cancer
    AKR1C3-IN-14 (compound 4) is an AKR1C3 inhibitor (IC50=0.122 μM) that reduces the overproduction of androgens by inhibiting the activity of the AKR1C3 enzyme, thereby regulating hormone-mediated signaling. AKR1C3-IN-14 also plays a role in the biosynthesis of the prostaglandin PGF2α, regulating cell proliferation by affecting this pathway. AKR1C3-IN-14 can be used in the study of prostate cancer .
    AKR1C3-IN-14
  • HY-121656

    Endogenous Metabolite Cancer
    AKR1C2/3-IN-2 is a potential AKR1C3 inhibitor with selective AKR1C3 activity. AKR1C2/3-IN-2 is able to block AKR1C3-mediated testosterone (T) production and PSA induction, affecting the endocrine activity of prostate cancer cells. AKR1C2/3-IN-2 shows selectivity over other AKR1C enzymes, indicating its potential application in inhibiting drug-resistant prostate cancer. AKR1C2/3-IN-2 has no inhibitory activity against COX isomerases, further emphasizing its specificity as a prostate cancer inhibitory compound .
    AKR1C2/3-IN-2
  • HY-181542

    Aldose Reductase Cancer
    SG-55 is a selective, noncompetitive and orally active AKR1C3 inhibitor with an IC50 of 5 nM and a Ki of 10 nM. SG-55 shows >2000-fold selectivity for AKR1C3 over AKR1C1, AKR1C2, and AKR1C4 (> 10 μM). SG-55 increases the ratio of reduced/oxidized nicotinamide adenine dinucleotide phosphate (NADPH/NADP +), decreases the ratio of reduced/oxidized glutathione (GSH/GSSG), and induces DNA double-strand breaks. SG-55 can overcome Osimertinib (HY-15772) resistance mediated by EGFR C797S triple mutation in non-small cell lung cancer (NSCLC) .
    SG-55

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