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AKR

" in MedChemExpress (MCE) Product Catalog:

113

Inhibitors & Agonists

2

Peptides

1

Inhibitory Antibodies

11

Natural
Products

9

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2

Isotope-Labeled Compounds

14

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1

Click Chemistry

23

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N0376
    Liquiritin
    Maximum Cited Publications
    15 Publications Verification

    Reactive Oxygen Species (ROS) 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-P99930
    Efruxifermin
    2 Publications Verification

    AKR-001; AMG-876

    FGFR Metabolic Disease
    Efruxifermin is an Fc-FGF21 fusion protein (human IgG1 Fc domain linked to a modified human FGF21). Efruxifermin has prolonged half-life and enhanced receptor affinity compared with native human FGF21. Efruxifermin can be used for the research of non-alcoholic steatohepatitis .
    Efruxifermin
  • HY-133708
    β-Glucogallin
    1 Publications Verification

    Glucogallin; 1-O-Galloyl-β-D-glucose

    Aldose Reductase Reactive Oxygen Species (ROS) NF-κB PDGFR SOD Neurological Disease Metabolic Disease
    β-Glucogallin is an orally active and selective aldose reductase (AKR1B1) inhibitor with an IC50 value of 58 μM when using Glyceraldehyde (HY-128748) as AKR1B1 substrate. β-Glucogallin reduces ROS, PDGF, RAGE, and NF-κB. β-Glucogallin increases SOD. β-Glucogallin has antioxidant and hepatoprotective effects. β-Glucogallin can be used in retinal research .
    β-Glucogallin
  • HY-105185
    Fidarestat
    3 Publications Verification

    SNK 860

    Aldose Reductase Metabolic Disease
    Fidarestat (SNK 860) is an inhibitor of aldose reductase, with IC50s of 26 nM, 33 μM, and 1.8 μM for aldose reductase, AKR1B10 and V301L AKR1B10, respectively; Fidarestat (SNK 860) has the potential to treat diabetic disease.
    Fidarestat
  • HY-113114

    Endogenous Metabolite Glucocorticoid Receptor Metabolic Disease Inflammation/Immunology
    Tetrahydrocortisone is a corticosteroid catalyzed from endogenous glucocorticoids by AKR1D1 (5β-reductase). Its formation is mediated by AKR1D1 and regulated by the glucocorticoid receptor (GR). As one of the final products of glucocorticoid inactivation metabolism, Tetrahydrocortisone participates in the maintenance of glucocorticoid metabolic homeostasis in vivo. Tetrahydrocortisone can be used for mechanistic studies of metabolic diseases such as non-alcoholic fatty liver disease (NAFLD) and type 2 diabetes, and also serves as a biomarker for in vivo AKR1D1 activity and glucocorticoid metabolic status .
    Tetrahydrocortisone
  • HY-13463
    Avatrombopag
    5 Publications Verification

    AKR-501; E5501; YM477

    Thrombopoietin Receptor Inflammation/Immunology Cancer
    Avatrombopag (AKR-501) is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag mimics the biological activities of TPO. Avatrombopag increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A .
    Avatrombopag
  • 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-114009
    AKR1C1-IN-1
    2 Publications Verification

    Aldose Reductase Neurological Disease
    AKR1C1-IN-1 is a potent and selective inhibitor of human 20α-hydroxysteroid dehydrogenase (AKR1C1), with a Ki value of 4 nM for AKR1C1 .
    AKR1C1-IN-1
  • 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-139696

    Aldose Reductase Cancer
    AKR1B10-IN-1 is a potent inhibitor of AKR1B10 (Aldo-Keto Reductase 1B10) with an IC50 of 3.5 nM. AKR1B10-IN-1 suppresses proliferation, metastasis, and Cisplatin (CDDP) resistance of lung cancer cells .
    AKR1B10-IN-1
  • HY-124573

    OBI-3424; TH-3424; (R)-AST-3424

    DNA Alkylator/Crosslinker Cancer
    (R)-Odafosfamide (OBI-3424) is a proagent that is selectively converted by AKR1C3 (aldo-keto reductase 1C3) to a potent DNA-alkylating agent. (R)-Odafosfamide can be used for hepatocellular carcinoma, castrate-resistant prostate cancer, and acute lymphoblastic leukemia (ALL) research .
    (R)-Odafosfamide
  • 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-P3333

    MHC Inflammation/Immunology Cancer
    KSPWFTTL is an immunodominant Kb-restricted epitope from the p15E transmembrane protein. KSPWFTTL can restore susceptibility of a tumor line to anti-AKR/Gross MuLV cytotoxic T lymphocytes .
    KSPWFTTL
  • HY-13463A
    Avatrombopag maleate
    5 Publications Verification

    AKR-501 maleate; E5501 maleate; YM477 maleate

    Thrombopoietin Receptor Cytochrome P450 ERK STAT Inflammation/Immunology Cancer
    Avatrombopag (AKR-501) maleate is an orally active, non-peptide thrombopoietin receptor (TPO receptor) agonist (EC50: 3.3 nM). Avatrombopag maleate mimics the biological activity of TPO. Avatrombopag maleate increases platelet production by activating intracellular signaling systems and promotes the production of platelets and megakaryocytes from hematopoietic precursor cells. Avatrombopag maleate is a substrate for cytochrome P450 (CYP) 2C9 and CYP3A .
    Avatrombopag maleate
  • HY-D1341
    Coumberone
    2 Publications Verification

    Fluorescent Dye Cancer
    Coumberone is a metabolic fluorogenic probe, and isoform-selective substrate for all AKR1C isoforms. Coumberone can be reduced by all four members of the AKR1C family to its fluorescent alcohol coumberol. Coumberone can be used for the research of AKR1C .
    Coumberone
  • HY-N2282

    Zingiberensis newsaponin

    Aldose Reductase JAK STAT Autophagy Apoptosis NF-κB SOD Reactive Oxygen Species (ROS) Cardiovascular Disease Neurological Disease Inflammation/Immunology Cancer
    Zingiberen Newsaponin (Zingiberensis newsaponin) is an orally active type of steroid saponin compound. Zingiberen Newsaponin exerts anti-hepatocellular carcinoma (HCC) effects by inhibiting autophagy and the AKR1C1/JAK2/STAT3 pathway. Zingiberen Newsaponin activates oxidative stress (upregulates ROS and MDA) and mitochondrial pathways, promoting cancer cell apoptosis. Zingiberen Newsaponin alleviates cerebral ischemia-reperfusion (I/R) injury by decreasing the concentration of pro-inflammatory cytokines and inhibits NF-κB. Zingiberen Newsaponin can enhance the activity of SOD, eliminate free radicals and protect nerve cells. Zingiberen Newsaponin induces platelet aggregation .
    Zingiberen newsaponin
  • 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-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-D1342

    Fluorescent Dye Cancer
    Coumberol is a fluorescent substrate of AKR1C3 protein. Coumberol can be used for the research of AKR1C3 .
    Coumberol
  • 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-172314

    Aldose Reductase Drug Derivative Cancer
    ACHM-025 is a prodrug, which is selectively activated by AKR1C3 to a nitrogen mustard DNA alkylating agent. ACHM-025 can be used for the research of cancer, such as leukemia .
    ACHM-025
  • 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-RS17235

    Small Interfering RNA (siRNA) Others

    Akr1b1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Akr1b1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Akr1b1 Mouse Pre-designed siRNA Set A
    Akr1b1 Mouse Pre-designed siRNA Set A
  • 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-149040

    (S)-OBI-3424; (S)-TH-3424; AST-3424

    17β-HSD Cancer
    Odafosfamide ((S)-OBI-3424) is a highly selective prodrug bis-alkylating agent activated by aldehyde-keto reductase 1C3 (AKR1C3(). Odafosfamide is highly cytotoxic to cell lines with high AKR1C3 expression. Odafosfamide exhibits antitumor activity in a variety of tumors with high AKR1C3 expression (such as liver cancer, non-small cell lung cancer, and leukemia). Odafosfamide can be used in cancer research .
    Odafosfamide
  • 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-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-118819

    Aldose Reductase Neurological Disease Cancer
    5-Bromo-3-phenyl salicylic acid is a selective inhibitor for human 20α-hydroxysteroid dehydrogenase (AKR1C1) with Ki of 140 nM .
    5-Bromo-3-phenyl salicylic acid
  • HY-N8549A

    Endogenous Metabolite Metabolic Disease
    5-Dihydrocortisone is a 5-Dihydrocortisone with mixture of isomers. 5β-Dihydrocortisone is a sterol metabolite of cortisone by 5β-reductase (AKR1D1) in liver
    5-Dihydrocortisone
  • HY-RS00532

    Small Interfering RNA (siRNA) Others

    AKR1B1 Human Pre-designed siRNA Set A contains three designed siRNAs for AKR1B1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    AKR1B1 Human Pre-designed siRNA Set A
    AKR1B1 Human Pre-designed siRNA Set A
  • HY-RS00533

    Small Interfering RNA (siRNA) Others

    AKR1B10 Human Pre-designed siRNA Set A contains three designed siRNAs for AKR1B10 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    AKR1B10 Human Pre-designed siRNA Set A
    AKR1B10 Human Pre-designed siRNA Set A
  • HY-13463B
    Avatrombopag hydrochloride
    5 Publications Verification

    AKR-501 hydrochloride; E5501 hydrochloride; YM477 hydrochloride

    Thrombopoietin Receptor Cardiovascular Disease Cancer
    Avatrombopag (AKR-501) hydrochloride is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag hydrochloride mimics the biological activities of TPO. Avatrombopag hydrochloride increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag hydrochloride is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A .
    Avatrombopag hydrochloride
  • 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-P3333A

    MHC Inflammation/Immunology Cancer
    KSPWFTTL TFA is an immunodominant Kb-restricted epitope from the p15E transmembrane protein. KSPWFTTL TFA can restore susceptibility of a tumor line to anti-AKR/Gross MuLV cytotoxic T lymphocytes .
    KSPWFTTL TFA
  • HY-W010617

    Biochemical Assay Reagents Inflammation/Immunology
    2-Cyclohexen-1-ol is a biochemical reagent. 2-Cyclohexen-1-ol is the oxidation substrate of mouse aldo-keto reductase AKR1C12, with a Km of 1080 μM and a Kcat of 13 min -1, showing low catalytic efficiency .
    2-Cyclohexen-1-ol
  • 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-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-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-13463R

    AKR-501 (Standard); E5501 (Standard); YM477 (Standard)

    Reference Standards Thrombopoietin Receptor Inflammation/Immunology Cancer
    Avatrombopag (Standard) is the analytical standard of Avatrombopag. This product is intended for research and analytical applications. Avatrombopag (AKR-501) is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag mimics the biological activities of TPO. Avatrombopag increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A .
    Avatrombopag (Standard)
  • HY-13463BS

    AKR-501-d8 hydrochloride; E5501-d8 hydrochloride; YM477-d8 hydrochloride

    Isotope-Labeled Compounds Thrombopoietin Receptor Cardiovascular Disease
    Avatrombopag-d8 (hydrochloride) is deuterium labeled Avatrombopag (hydrochloride). Avatrombopag (AKR-501) hydrochloride is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag hydrochloride mimics the biological activities of TPO. Avatrombopag hydrochloride increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag hydrochloride is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A .
    Avatrombopag-d8 hydrochloride
  • 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-177415

    Aldose Reductase Endocrinology
    JSD26 is a selective and orally active SCoR2 (AKR1A1) inhibitor with an IC50 of 93 nM. JSD26 has 10-fold selectivity for SCoR2 versus AKR1B1. JSD26 can be used for the study acute kidney injury (AKI) .
    JSD26
  • HY-175331

    Aldose Reductase Metabolic Disease Cancer
    ALR2-IN-7 (Compound 5a) is a highly potent and selective aldose reductase (ALR2/AKR1B1) inhibitor (Ki=8.71 nM). ALR2-IN-7 is promising for research of diabetic complications (e.g., retinopathy, nephropathy) and cancers .
    ALR2-IN-7
  • 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-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-173132

    Aldose Reductase Cancer
    AKR1Cs-IN-1 (Compound 29) is a potent and broad-spectrum inhibitor targeting members of the Aldo-Keto Reductase 1C family (AKR1C1-1C4). By simultaneously occupying the SP2 and SP3 pockets, it effectively inhibits multiple isoforms and disrupts metabolic pathways associated with drug resistance. In enzymatic activity assays, AKR1Cs-IN-1 exhibited significant inhibitory potency, with IC50 values of 0.09, 0.28, 0.05, and 0.51 µM against AKR1C1, AKR1C2, AKR1C3, and AKR1C4, respectively. In the doxorubicin (DOX)-resistant breast cancer cell line MCF-7/ADR, AKR1Cs-IN-1 showed remarkable resensitization effects and significantly enhanced the cytotoxicity of DOX. AKR1Cs-IN-1 holds promise for research on overcoming drug resistance in breast cancer .
    AKR1Cs-IN-1
  • 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

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