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AKR1C3

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37

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Cat. No. Product Name Target Research Areas Chemical Structure
  • 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-RS00536

    Small Interfering RNA (siRNA) Others

    AKR1C3 Human Pre-designed siRNA Set A contains three designed siRNAs for AKR1C3 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    AKR1C3 Human Pre-designed siRNA Set A
    AKR1C3 Human Pre-designed siRNA Set A
  • 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-144749

    Aldose Reductase Cancer
    AKR1C3-IN-5 (Compound 6e) is a potent inhibitor of AKR1C3. AKR1C3 enzyme is overexpressed in hormone-dependent prostate and breast tumors. AKR1C3-IN-5 derived from drupanin, which exhibits half-maximal inhibitory concentration (IC50) of 9.6 ± 3 μM and selectivity index (SI) of 5.5 against MCF-7 cells .
    AKR1C3-IN-5
  • 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-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-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-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-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-107379
    AKR1C3-IN-1
    1 Publications Verification

    17β-HSD Others
    AKR1C3-IN-1 is a potent, highly selective inhibitor of AKR1C3, with an IC50 of 13 nM.
    AKR1C3-IN-1
  • 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-152188

    Aldose Reductase Cancer
    AKR1C3-IN-9 is a selective inhibitor of Aldo-keto Reductase 1C3 (AKR1C3) with an IC50 value of 8.92 nM. AKR1C3-IN-9 significantly reverses the Doxorubicin (HY-15142A) (DOX) resistance in a resistant breast cancer cell line .
    AKR1C3-IN-9
  • 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-D1342

    Fluorescent Dye Cancer
    Coumberol is a fluorescent substrate of AKR1C3 protein. Coumberol can be used for the research of AKR1C3 .
    Coumberol
  • HY-W008567

    Drug Metabolite Others
    N-Deschlorobenzoyl indomethacin (Compound 18), the primary metabolite of indomethacin (HY-14397), lacks the ​N-p-chlorobenzoyl group in its structure. Consequently, N-Deschlorobenzoyl indomethacin loses inhibitory activity against AKR1C2 and AKR1C3 (AKR1C2 IC50 =100 μM, AKR1C3 IC50 >100 μM), exhibiting no selectivity .
    N-Deschlorobenzoyl indomethacin
  • 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-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-19903
    ASP-9521
    2 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-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-W024692

    Indometacin methylester

    Prostaglandin Receptor 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-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-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-163940

    Aldose Reductase Androgen Receptor Cancer
    LX1 is an anti-prostate cancer compound that targets androgen receptor (AR), AR variants and steroidogenic enzyme AKR1C3. LX1 inhibits the enzymatic activity of AKR1C3, reduces the conversion of androstenedione to testosterone and reduces the expression of AR and AR-V7 and downregulates their target genes. LX1 overcomes the resistance of tumor cells to Enzalutamide (HY-70002), and the combination with Enzalutamide (HY-70002) further inhibits tumor growth .
    LX1
  • HY-116170

    Aldose Reductase Cancer
    SN34037 is a specific inhibitor of Aldo-keto reductase 1C3 (AKR1C3, EC 1.1.1.188) with the ability to inhibit the cytotoxic activity of PR-104A. SN34037-sensitive coumberone reduction provides a rapid and specific assay for AKR1C3 activity. SN34037 inhibits the aerobic cytotoxicity of PR-104A in TF1 erythroleukemia cells with high AKR1C3 expression, but not in Nalm6 pre-B acute lymphoblastic leukemia cells with low AKR1C3 expression .
    SN34037
  • HY-152189

    Others 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-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-124573

    TH-3424

    DNA Alkylator/Crosslinker Cancer
    OBI-3424 (TH-3424) is a proagent that is selectively converted by AKR1C3 (aldo-keto reductase 1C3) to a potent DNA-alkylating agent. OBI-3424 can be used for hepatocellular carcinoma, castrate-resistant prostate cancer, and acute lymphoblastic leukemia (ALL) research .
    OBI-3424
  • 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-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-N10361

    RAR/RXR PPAR Aldose Reductase Cancer
    Drupanin is an orally active and selective AKR1C3 enzyme inhibitor and an RXRα agonist with an EC50 value of 4.8 μM, which is found in green propolis. Drupanin also activates PPARγ moderately. Drupanin induces adipogenesis and elevates aP2 mRNA levels in 3T3-L1 fibroblasts Drupanin has the potential for the research of breast and prostate cancers .
    Drupanin
  • 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-163647

    E3 Ligase Ligand-Linker Conjugates Cancer
    Lenalidomide-COCH-PEG2-azido is a synthesized E3 ligase ligand-linker conjugate that incorporates the Lenalidomide (HY-A0003) based cereblon ligand and a linker. Lenalidomide-COCH-PEG2-azido can be used in the synthesis of PROTAC AKR1C3 degrader-1 (HY-163609) .
    Lenalidomide-COCH-PEG2-azido
  • HY-150644
    S07-2010
    1 Publications Verification

    Aldose Reductase Cancer
    S07-2010 is a potent pan-AKR1C (aldo-keto reductase family 1 member C) inhibitor, with IC50 values of 0.19, 0.36, 0.47, and 0.73 μM for AKR1C3, AKR1C4, AKR1C1 and AKR1C2, respectively. S07-2010 induces apoptosis in A549/DDP cells. S07-2010 strengthens the cytotoxicity of chemotherapeutic agents in drug-resistant cells. S07-2010 significantly inhibits the proliferation of drug-resistant cells .
    S07-2010
  • HY-N0376
    Liquiritin
    Maximum Cited Publications
    7 Publications Verification

    Reactive Oxygen Species Neurological Disease Inflammation/Immunology Cancer
    Liquiritin, a flavonoid isolated from Glycyrrhiza uralensis, is a potent and competitive AKR1C1 inhibitor with IC50s of 0.62 μM, 0.61 μM, and 3.72μM for AKR1C1, AKR1C2 and AKR1C3, respectively. Liquiritin efficiently inhibits progesterone metabolism mediated by AKR1C1 in vivo . Liquiritin acts as an antioxidant and has neuroprotective, anti-cancer and anti-inflammatory activity .
    Liquiritin
  • HY-N0376R

    Reactive Oxygen Species Neurological Disease Inflammation/Immunology Cancer
    Liquiritin (Standard) is the analytical standard of Liquiritin. This product is intended for research and analytical applications. Liquiritin, a flavonoid isolated from Glycyrrhiza uralensis, is a potent and competitive AKR1C1 inhibitor with IC50s of 0.62 μM, 0.61 μM, and 3.72μM for AKR1C1, AKR1C2 and AKR1C3, respectively. Liquiritin efficiently inhibits progesterone metabolism mediated by AKR1C1 in vivo . Liquiritin acts as an antioxidant and has neuroprotective, anti-cancer and anti-inflammatory activity .
    Liquiritin (Standard)
  • HY-B0398AR

    Bacterial Antibiotic Topoisomerase Infection
    Liquiritin (Standard) is the analytical standard of Liquiritin. This product is intended for research and analytical applications. Liquiritin, a flavonoid isolated from Glycyrrhiza uralensis, is a potent and competitive AKR1C1 inhibitor with IC50s of 0.62 μM, 0.61 μM, and 3.72μM for AKR1C1, AKR1C2 and AKR1C3, respectively. Liquiritin efficiently inhibits progesterone metabolism mediated by AKR1C1 in vivo . Liquiritin acts as an antioxidant and has neuroprotective, anti-cancer and anti-inflammatory activity .
    Nalidixic acid (sodium salt) (Standard)

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